Page last updated: 2024-12-08

cilengitide

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Description

Cilengitide: an alphaVbeta3 integrin antagonist that paralyzes cancer cells [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID176873
CHEMBL ID429876
CHEBI ID177833
SCHEMBL ID34082
MeSH IDM0382698

Synonyms (55)

Synonym
2-[(2s,5r,8s,11s)-5-benzyl-11-[3-(diaminomethylideneamino)propyl]-7-methyl-3,6,9,12,15-pentaoxo-8-propan-2-yl-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid
CHEBI:177833
188968-51-6
emd-121974
cyclo(l-arginylglycyl-l-aspartyl-d-phenylalanyl-n-methyl-l-valyl)
cilengitide [usan:inn]
cyclo(l-arginylglycyl-l-alpha-aspartyl-d-phenylalanyl-n-methyl-l-valyl)
cilengitide (usan/inn)
D03497
emd 121974
cilengitide
cyclo-(arg-gly-asp-dphe-nmeval)
nsc-707544
emd121974
cyclic-arg-gly-asp-d-phe(n-methyl)val
cyclo(arginyl-glycyl-formylaspartyl-n-methylvalyl)
cyclo(l-arginylglycyl-l-a-aspartyl-d-phenylalanyl-n-methyl-l-valyl)
CHEMBL429876 ,
emd-12192
[(2s,5r,8s,11s)-5-benzyl-11-(3-guanidino-propyl)-8-isopropyl-7-methyl-3,6,9,12,15-pentaoxo-1,4,7,10,13pentaaza-cyclopentadec-2-yl]-acetic acid
c(rgdfmev)
cyclo(arg-gly-asp-d-phe-[n-me]val)
bdbm50235980
2-((2s,5r,8s,11s)-5-benzyl-11-(3-guanidinopropyl)-8-isopropyl-7-methyl-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaazacyclopentadecan-2-yl)acetic acid
unii-4edf46e4gi
4edf46e4gi ,
HY-16141
CS-1211
cilengitide [mi]
cilengitide [usan]
cyclo(l-arginylglycyl-l-.alpha.-aspartyl-d-phenylalanyl-n-methyl-l-valyl)
cilengitide [mart.]
cilengitide [inn]
cilengitide [who-dd]
S6387
gtpl6597
2-[(2s,5r,8s,11s)-11-[3-(diaminomethylideneamino)propyl]-7-methyl-3,6,9,12,15-pentaoxo-5-(phenylmethyl)-8-propan-2-yl-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid
SCHEMBL34082
DTXSID9044035
AKOS024257893
AKOS030525213
AMLYAMJWYAIXIA-VWNVYAMZSA-N
AS-72195
2-[(2s,5r,8s,11s)-5-benzyl-11-(3-carbamimidamidopropyl)-7-methyl-3,6,9,12,15-pentaoxo-8-(propan-2-yl)-1,4,7,10,13-pentaazacyclopentadecan-2-yl]acetic acid
EX-A1775
SW220134-1
DB11890
cilengitide trifluoroacetic acid salt
Q1091921
NCGC00386242-04
NCGC00386242-02
A924615
AC-35857
nsc-774651
nsc774651

Research Excerpts

Overview

Cilengitide is a cyclic RGD pentapeptide with anti-angiogenic activity. It targets the integrins known to mediate cell-ECM interactions and activate the pro-fibrotic growth factor Transforming Growth Factor beta (TGF-β)

ExcerptReferenceRelevance
"Cilengitide is a cyclic RGD pentapeptide with anti-angiogenic activity that targets αvβ3, αvβ5 and α5β1, integrins known to mediate cell-ECM interactions and activate the pro-fibrotic growth factor Transforming Growth Factor beta (TGF-β)."( The Integrin Inhibitor Cilengitide and Bleomycin-Induced Pulmonary Fibrosis : Cilengitide and Bleomycin-Induced Pulmonary Fibrosis.
Ritzenthaler, JD; Roman, J; Torres-Gonzalez, E; Zhang, M, 2020
)
1.59
"Cilengitide is a potent and selective inhibitor of the integrins αvβ3 and αvβ5. "( A phase I study of cilengitide and paclitaxel in patients with advanced solid tumors.
Eadens, M; Erlichman, C; Goetz, MP; Haddad, T; Lupu, R; Molina, J; Qin, R; Satele, D, 2017
)
2.23
"Cilengitide is a selective antagonist of αvβ3 and αvβ5 integrins, which are involved in tumor growth and development of metastasis."( Cilengitide targets pediatric glioma and neuroblastoma cells through cell detachment and anoikis induction.
Bal-Mahieu, C; Baroncini, M; Dewitte, A; Lansiaux, A; Lartigau, E; Le Tinier, F; Leblond, P; Meignan, S; Sarrazin, T, 2013
)
2.55
"Cilengitide is an RGD-peptide of sequence cyclo[RGDfNMeV] that was was developed as a highly active and selective ligand for the αvβ3 and αvβ5 integrin receptors. "( Tackling lipophilicity of peptide drugs: replacement of the backbone N-methyl group of cilengitide by N-oligoethylene glycol (N-OEG) chains.
Adan, J; Albericio, F; Fernández-Llamazares, AI; Mitjans, F; Spengler, J, 2014
)
2.07
"Cilengitide is a chemical synthesis cyclopeptide containing RGD sequence, which can be used as a small molecule antagonist targeted to integrin αν (ITGAV). "( Cilengitide, a small molecule antagonist, targeted to integrin αν inhibits proliferation and induces apoptosis of laryngeal cancer cells in vitro.
Kan, X; Liu, M; Liu, Y; Lu, JG; Wang, JT, 2014
)
3.29
"Cilengitide is an αvβ3/αvβ5-integrin inhibitor investigated as an anticancer agent. "( Population pharmacokinetics of cilengitide in adult and pediatric cancer patients from a nonlinear mixed-effects analysis.
Bhattaram, VA; Campioni, M; Derendorf, H; Kovar, A; Krösser, S; Zühlsdorf, M, 2014
)
2.13
"Cilengitide is a stable cyclic pentapeptide containing an Arg-Gly-Asp motif responsible for selective binding to αVβ3 and αVβ5 integrins. "( Time- and NADPH-dependent inhibition of cytochrome P450 3A4 by the cyclopentapeptide cilengitide: significance of the guanidine group and accompanying spectral changes.
Barbero, L; Bojić, M; Dolgos, H; Freisleben, A; Gallemann, D; Guengerich, FP; Riva, S, 2014
)
2.07
"Cilengitide is a selective αvβ3 and αvβ5 integrin inhibitor. "( Cilengitide combined with standard treatment for patients with newly diagnosed glioblastoma with methylated MGMT promoter (CENTRIC EORTC 26071-22072 study): a multicentre, randomised, open-label, phase 3 trial.
Adamska, K; Aldape, KD; Brandes, AA; Erridge, SC; Gorlia, T; Grujicic, D; Gupta, T; Hau, P; Hegi, ME; Herrlinger, U; Hicking, C; Hong, YK; Kim, CY; Kortmann, RD; Lhermitte, B; Markivskyy, A; McBain, C; Nabors, LB; Nam, DH; Perry, J; Picard, M; Pietsch, T; Rao, N; Reardon, DA; Schnell, O; Shen, CC; Steinbach, JP; Stupp, R; Taphoorn, MJ; Tarnawski, R; Thurzo, L; Tonn, JC; van den Bent, MJ; Weller, M; Weyerbrock, A; Wick, W; Wiegel, T, 2014
)
3.29
"Cilengitide (CLG) is an inhibitor of both αv β3 and αv β5 integrins, with a defined anti-tumour effect in glioblastoma. "( Cilengitide restrains the osteoclast-like bone resorbing activity of myeloma plasma cells.
Cafforio, P; Felici, C; Resta, L; Rossi, R; Silvestris, F; Stucci, S; Tucci, M, 2016
)
3.32
"Cilengitide (CGT) is a cyclic pentapeptide that demonstrated efficacy for GBM treatment by targeting the integrins avβ3 and avβ5 over-expressed on GBM cells."( Glioma-targeted therapy using Cilengitide nanoparticles combined with UTMD enhanced delivery.
Lin, Q; Lu, CT; Mao, KL; Shen, XT; Tian, FR; Wong, HL; Xiao, J; Xu, HL; Xu, J; Yang, JJ; Yang, W; Zhao, YZ, 2016
)
1.44
"Cilengitide is a potent alphavbeta3 and alphavbeta5 integrin inhibitor."( Cilengitide: an integrin-targeting arginine-glycine-aspartic acid peptide with promising activity for glioblastoma multiforme.
Mikkelsen, T; Nabors, LB; Reardon, DA; Stupp, R, 2008
)
2.51
"Cilengitide is a specific inhibitor of alphav series integrins, and acts as an antiangiogenic."( Radiation sensitization of glioblastoma by cilengitide has unanticipated schedule-dependency.
Berens, ME; Brodie, C; Brown, SL; Finniss, S; Goodman, SL; Hahn, D; Lemke, N; Mikkelsen, T; Nelson, K; Neuteboom, B; Rennert, JL, 2009
)
1.34
"Cilengitide is a high-affinity cyclic pentapeptdic alphaV integrin antagonist previously reported to suppress angiogenesis by inducing anoikis of endothelial cells adhering through alphaVbeta3/alphaVbeta5 integrins. "( The integrin antagonist cilengitide activates alphaVbeta3, disrupts VE-cadherin localization at cell junctions and enhances permeability in endothelial cells.
Alghisi, GC; Ponsonnet, L; Rüegg, C, 2009
)
2.1
"Cilengitide is a cyclic peptide antagonist of integrins alphavbeta3 and alphavbeta5 that is currently being evaluated as a novel therapeutic agent for recurrent and newly diagnosed glioblastoma. "( Cilengitide modulates attachment and viability of human glioma cells, but not sensitivity to irradiation or temozolomide in vitro.
Adams, B; Maurer, GD; Stupp, R; Tabatabai, G; Tritschler, I; Weller, M; Wick, W, 2009
)
3.24
"Cilengitide (EMD121974) is a cyclized pentapeptide that is a potent and selective integrin antagonist which has shown activity in malignant gliomas. "( A phase I study of continuous infusion cilengitide in patients with solid tumors.
Janisch, L; Karrison, TM; Nicholas, MK; O'Donnell, PH; Ratain, MJ; Stadler, WM; Undevia, SD, 2012
)
2.09
"Cilengitide is a cyclic pentapeptide that is a specific inhibitor of the αvβ3 and αvβ5 integrins. "( Cilengitide in patients with recurrent glioblastoma: the results of NABTC 03-02, a phase II trial with measures of treatment delivery.
Chang, S; Cloughesy, T; Deangelis, LM; Gilbert, MR; Kuhn, J; Lamborn, KR; Lassman, AB; Lieberman, F; Mehta, M; Prados, M; Wen, PY, 2012
)
3.26
"Cilengitide is a selective integrin inhibitor that is well tolerated and has demonstrated biologic activity in patients with recurrent malignant glioma. "( A safety run-in and randomized phase 2 study of cilengitide combined with chemoradiation for newly diagnosed glioblastoma (NABTT 0306).
Batchelor, T; Brem, S; Fisher, JD; Grossman, SA; Hegi, ME; Lesser, G; Mikkelsen, T; Nabors, LB; Olsen, J; Peereboom, D; Rosenfeld, MR; Ye, X, 2012
)
2.08
"Cilengitide (EMD 121974) is a selective inhibitor of integrins αvβ3 and αvβ5. "( A randomized phase II study of cilengitide (EMD 121974) in patients with metastatic melanoma.
Bedikian, AY; Camacho, LH; Colevas, AD; Diwan, AH; Gallick, GE; Hwu, P; Johnson, MM; Joseph, RW; Kim, KB; Ng, CS; Papadopoulos, NE; Prieto, V; Reckeweg, A; Vardeleon, A; Wei, W; Wittemer, SM, 2012
)
2.11
"Cilengitide is a well-tolerated antiangiogenic agent. "( Assessment of the biological and pharmacological effects of the alpha nu beta3 and alpha nu beta5 integrin receptor antagonist, cilengitide (EMD 121974), in patients with advanced solid tumors.
Baron, A; Basche, M; Colevas, D; Davis, D; Eckhardt, SG; Gallemann, D; Gore, L; Gustafson, D; Hariharan, S; Holden, S; McConkey, D; Morrow, M; O'Bryant, CL; Zang, C, 2007
)
1.99

Effects

Cilengitide has been shown to inhibit alphavbeta3- and alophavbeta5-mediated cell adhesion and block in vitro endothelial cell migration. It has significantly inhibited the proliferation of HNSCC cells in a dose-dependent way.

ExcerptReferenceRelevance
"Cilengitide has significantly inhibited the proliferation of HNSCC cells in a dose-dependent way. "( A comparative assessment of the effects of integrin inhibitor cilengitide on primary culture of head and neck squamous cell carcinoma (HNSCC) and HNSCC cell lines.
Açil, Y; Gülses, A; Purcz, N; Weimer, J; Wiltfang, J; Zhang, L, 2019
)
2.2
"Cilengitide has been shown to inhibit alphavbeta3- and alphavbeta5-mediated cell adhesion and block in vitro endothelial cell migration."( Phase II evaluations of cilengitide in asymptomatic patients with androgen-independent prostate cancer: scientific rationale and study design.
Beekman, KW; Colevas, AD; Cooney, K; Dipaola, R; Dunn, RL; Gross, M; Hussain, M; Keller, ET; Pienta, KJ; Ryan, CJ; Smith, D, 2006
)
1.36

Actions

ExcerptReferenceRelevance
"Cilengitide appears to enhance radiation response in preclinical models of breast cancer. "( In vitro study of combined cilengitide and radiation treatment in breast cancer cell lines.
Chakravarti, A; Huebner, A; Ibrahim, A; Lautenschlaeger, T; Li, B; Meng, W; Peereboom, D; Perry, J; White, J, 2013
)
2.13

Treatment

Cilengitide treatment resulted in a significantly decreased diameter of the J3T-1 tumor vessel clusters and its core vessels when compared with controls. An anti-invasive effect was shown in the J 3T-2 glioma with a significant reduction of diffuse cell infiltration around the tumor center.

ExcerptReferenceRelevance
"Cilengitide treatment of cultured fibroblasts showed decreased adhesion to vitronectin and fibronectin, both integrin-dependent events. "( The Integrin Inhibitor Cilengitide and Bleomycin-Induced Pulmonary Fibrosis : Cilengitide and Bleomycin-Induced Pulmonary Fibrosis.
Ritzenthaler, JD; Roman, J; Torres-Gonzalez, E; Zhang, M, 2020
)
2.31
"Cilengitide treatment resulted in a significantly decreased diameter of the J3T-1 tumor vessel clusters and its core vessels when compared with controls, while an anti-invasive effect was shown in the J3T-2 glioma with a significant reduction of diffuse cell infiltration around the tumor center."( Bimodal anti-glioma mechanisms of cilengitide demonstrated by novel invasive glioma models.
Chiocca, EA; Date, I; Fujii, K; Ichikawa, T; Inoue, S; Kaur, B; Kurozumi, K; Michiue, H; Onishi, M; Yoshida, K, 2013
)
1.39
"Cotreatment with cilengitide and radiation dramatically amplified the effects of radiation, producing survival over 200 days and triggering an enhanced apoptotic response and suppression of tumor growth by histology at necropsy."( Radiation sensitization of glioblastoma by cilengitide has unanticipated schedule-dependency.
Berens, ME; Brodie, C; Brown, SL; Finniss, S; Goodman, SL; Hahn, D; Lemke, N; Mikkelsen, T; Nelson, K; Neuteboom, B; Rennert, JL, 2009
)
0.94

Pharmacokinetics

A single-agent dose escalating phase I and pharmacokinetic study with Cilengitide was performed to determine its safety and toxicity. A candidate pharmacodynamic biomarker, serum c-telopeptide collagen crosslinks (CTx), was also measured.

ExcerptReferenceRelevance
"A single-agent dose escalating phase I and pharmacokinetic study with Cilengitide, an inhibitor of the integrins alphavbeta3 and alphavbeta5, was performed to determine its safety and toxicity."( Phase I and pharmacokinetic study of continuous twice weekly intravenous administration of Cilengitide (EMD 121974), a novel inhibitor of the integrins alphavbeta3 and alphavbeta5 in patients with advanced solid tumours.
Böttcher, S; Brindley, C; Drevs, J; Dumez, H; Eskens, FA; Hoekstra, R; Perschl, A; van Oosterom, AT; Verweij, J; Wynendaele, W, 2003
)
0.77
" This study aimed to develop a cilengitide population pharmacokinetic model using nonlinear mixed-effects modeling of 136 adult patients with advanced solid tumors and to scale the pharmacokinetic parameters to the pediatric population."( Population pharmacokinetics of cilengitide in adult and pediatric cancer patients from a nonlinear mixed-effects analysis.
Bhattaram, VA; Campioni, M; Derendorf, H; Kovar, A; Krösser, S; Zühlsdorf, M, 2014
)
0.97
"Fit-for-purpose pharmacodynamic biomarkers could expedite development of combination antiangiogenic regimens."( Serum C-Telopeptide Collagen Crosslinks and Plasma Soluble VEGFR2 as Pharmacodynamic Biomarkers in a Trial of Sequentially Administered Sunitinib and Cilengitide.
Cohen, EE; Fleming, GF; Harris, PJ; Janisch, L; Karovic, S; Karrison, TG; Levine, MR; Maitland, ML; O'Donnell, PH; Polite, BN; Ratain, MJ, 2015
)
0.62
" A candidate pharmacodynamic biomarker of cilengitide inhibition of integrin αvβ3, serum c-telopeptide collagen crosslinks (CTx), was also measured."( Serum C-Telopeptide Collagen Crosslinks and Plasma Soluble VEGFR2 as Pharmacodynamic Biomarkers in a Trial of Sequentially Administered Sunitinib and Cilengitide.
Cohen, EE; Fleming, GF; Harris, PJ; Janisch, L; Karovic, S; Karrison, TG; Levine, MR; Maitland, ML; O'Donnell, PH; Polite, BN; Ratain, MJ, 2015
)
0.88

Compound-Compound Interactions

Cilengitide was well tolerated when combined with standard chemoradiation. It may improve survival for patients newly diagnosed with glioblastoma multiforme regardless of MGMT methylation status.

ExcerptReferenceRelevance
" The primary objectives of this randomized phase 2 trial were to determine the safety and efficacy of cilengitide when combined with radiation and temozolomide for patients with newly diagnosed glioblastoma multiforme and to select a dose for comparative clinical testing."( A safety run-in and randomized phase 2 study of cilengitide combined with chemoradiation for newly diagnosed glioblastoma (NABTT 0306).
Batchelor, T; Brem, S; Fisher, JD; Grossman, SA; Hegi, ME; Lesser, G; Mikkelsen, T; Nabors, LB; Olsen, J; Peereboom, D; Rosenfeld, MR; Ye, X, 2012
)
0.85
"Cilengitide was well tolerated when combined with standard chemoradiation and may improve survival for patients newly diagnosed with glioblastoma multiforme regardless of MGMT methylation status."( A safety run-in and randomized phase 2 study of cilengitide combined with chemoradiation for newly diagnosed glioblastoma (NABTT 0306).
Batchelor, T; Brem, S; Fisher, JD; Grossman, SA; Hegi, ME; Lesser, G; Mikkelsen, T; Nabors, LB; Olsen, J; Peereboom, D; Rosenfeld, MR; Ye, X, 2012
)
2.08
" However, little is known about the cellular processes induced during cilengitide therapy in combination with irradiation and cisplatin in head and neck squamous cell carcinoma (HNSCC)."( The effect of cilengitide in combination with irradiation and chemotherapy in head and neck squamous cell carcinoma cell lines.
Heiduschka, G; Kornek, G; Kotowski, U; Lill, C; Schmid, R; Schneider, S; Seemann, R; Thurnher, D, 2014
)
1
" However, combination with cisplatin resulted in synergistic growth inhibition in all three cell lines."( The effect of cilengitide in combination with irradiation and chemotherapy in head and neck squamous cell carcinoma cell lines.
Heiduschka, G; Kornek, G; Kotowski, U; Lill, C; Schmid, R; Schneider, S; Seemann, R; Thurnher, D, 2014
)
0.76
"Cilengitide in combination with cisplatin and irradiation may be a feasible option for the treatment of patients with head and neck cancer."( The effect of cilengitide in combination with irradiation and chemotherapy in head and neck squamous cell carcinoma cell lines.
Heiduschka, G; Kornek, G; Kotowski, U; Lill, C; Schmid, R; Schneider, S; Seemann, R; Thurnher, D, 2014
)
2.21
" Data from phase 2 trials suggest that it has antitumour activity as a single agent in recurrent glioblastoma and in combination with standard temozolomide chemoradiotherapy in newly diagnosed glioblastoma (particularly in tumours with methylated MGMT promoter)."( Cilengitide combined with standard treatment for patients with newly diagnosed glioblastoma with methylated MGMT promoter (CENTRIC EORTC 26071-22072 study): a multicentre, randomised, open-label, phase 3 trial.
Adamska, K; Aldape, KD; Brandes, AA; Erridge, SC; Gorlia, T; Grujicic, D; Gupta, T; Hau, P; Hegi, ME; Herrlinger, U; Hicking, C; Hong, YK; Kim, CY; Kortmann, RD; Lhermitte, B; Markivskyy, A; McBain, C; Nabors, LB; Nam, DH; Perry, J; Picard, M; Pietsch, T; Rao, N; Reardon, DA; Schnell, O; Shen, CC; Steinbach, JP; Stupp, R; Taphoorn, MJ; Tarnawski, R; Thurzo, L; Tonn, JC; van den Bent, MJ; Weller, M; Weyerbrock, A; Wick, W; Wiegel, T, 2014
)
1.85
" This phase II, randomized, open-label, multicenter trial investigated the efficacy and safety of 2 dose regimens of the selective integrin inhibitor cilengitide combined with standard chemoradiotherapy in patients with newly diagnosed glioblastoma and an unmethylated MGMT promoter."( Two cilengitide regimens in combination with standard treatment for patients with newly diagnosed glioblastoma and unmethylated MGMT gene promoter: results of the open-label, controlled, randomized phase II CORE study.
Ashby, L; Depenni, R; Fink, KL; Grujicic, D; Hegi, ME; Hicking, C; Lhermitte, B; Mazurkiewicz, M; Mikkelsen, T; Nabors, LB; Nam, DH; Perry, JR; Picard, M; Reardon, DA; Salacz, M; Tarnawski, R; Zagonel, V, 2015
)
1.17
" Cilengitide was administered intravenously in combination with daily temozolomide (TMZ) and concomitant radiotherapy (RT; wk 1-6), followed by TMZ maintenance therapy (TMZ/RT→TMZ)."( Two cilengitide regimens in combination with standard treatment for patients with newly diagnosed glioblastoma and unmethylated MGMT gene promoter: results of the open-label, controlled, randomized phase II CORE study.
Ashby, L; Depenni, R; Fink, KL; Grujicic, D; Hegi, ME; Hicking, C; Lhermitte, B; Mazurkiewicz, M; Mikkelsen, T; Nabors, LB; Nam, DH; Perry, JR; Picard, M; Reardon, DA; Salacz, M; Tarnawski, R; Zagonel, V, 2015
)
1.89
"Standard and intensive cilengitide dose regimens were well tolerated in combination with TMZ/RT→TMZ."( Two cilengitide regimens in combination with standard treatment for patients with newly diagnosed glioblastoma and unmethylated MGMT gene promoter: results of the open-label, controlled, randomized phase II CORE study.
Ashby, L; Depenni, R; Fink, KL; Grujicic, D; Hegi, ME; Hicking, C; Lhermitte, B; Mazurkiewicz, M; Mikkelsen, T; Nabors, LB; Nam, DH; Perry, JR; Picard, M; Reardon, DA; Salacz, M; Tarnawski, R; Zagonel, V, 2015
)
1.29
"This multicentre, open-label, randomized, controlled phase II study evaluated cilengitide in combination with cetuximab and platinum-based chemotherapy, compared with cetuximab and chemotherapy alone, as first-line treatment of patients with advanced non-small-cell lung cancer (NSCLC)."( Cilengitide combined with cetuximab and platinum-based chemotherapy as first-line treatment in advanced non-small-cell lung cancer (NSCLC) patients: results of an open-label, randomized, controlled phase II study (CERTO).
Atanackovic, D; Barlesi, F; Bennouna, J; Feurer, M; Germonpre, P; Goekkurt, E; Gridelli, C; Hicking, C; Krzakowski, M; Lena, H; Milanowski, J; O'Byrne, K; Picard, M; Schuette, W; Straub, J; Szczesna, A; Vansteenkiste, J; Verhoeven, D; Waller, CF, 2015
)
2.09
" We designed a study of cediranib, a vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitor, combined with cilengitide, an integrin inhibitor."( A phase I study of cediranib in combination with cilengitide in patients with recurrent glioblastoma.
Ahluwalia, MS; Batchelor, TT; Duda, DG; Gerstner, ER; Grossman, S; Jain, RK; Kaley, TJ; Levine, MA; Mikkelsen, T; Nabors, BL; Olson, JJ; Wen, PY; Ye, X, 2015
)
0.88

Dosage Studied

Cilengitide was detected in all tumor specimens with higher levels in the group receiving 2000 mg dosing. So far, inhibition of angiogenesis by compounds such as bevacizumab, cediranib and enzastaurin did not prolong survival.

ExcerptRelevanceReference
"The phase II dosage of intravenous cilengitide in children with refractory brain tumors is 1,800 mg/m(2)."( Phase I clinical trial of cilengitide in children with refractory brain tumors: Pediatric Brain Tumor Consortium Study PBTC-012.
Boyett, JM; Ellenbogen, RG; Goldman, S; Kieran, MW; Kocak, M; Kun, LE; Lafond, D; MacDonald, TJ; Phillips, P; Poussaint, TY; Stewart, CF, 2008
)
0.92
" Cilengitide was detected in all tumor specimens with higher levels in the group receiving 2000 mg dosing while corresponding plasma concentrations were low, often below the lower limit of detection."( Cilengitide in patients with recurrent glioblastoma: the results of NABTC 03-02, a phase II trial with measures of treatment delivery.
Chang, S; Cloughesy, T; Deangelis, LM; Gilbert, MR; Kuhn, J; Lamborn, KR; Lassman, AB; Lieberman, F; Mehta, M; Prados, M; Wen, PY, 2012
)
2.73
" This was achieved with low CGT dosing level (2mg/kg twice weekly)."( Glioma-targeted therapy using Cilengitide nanoparticles combined with UTMD enhanced delivery.
Lin, Q; Lu, CT; Mao, KL; Shen, XT; Tian, FR; Wong, HL; Xiao, J; Xu, HL; Xu, J; Yang, JJ; Yang, W; Zhao, YZ, 2016
)
0.72
" So far, inhibition of angiogenesis by compounds such as bevacizumab, cediranib, enzastaurin or cilengitide as well as alternative dosing schedules of temozolomide did not prolong survival, neither at primary diagnosis nor at recurrent disease."( Pharmacotherapies for the treatment of glioblastoma - current evidence and perspectives.
Gramatzki, D; Roth, P; Seystahl, K; Weller, M, 2016
)
0.65
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
oligopeptideA peptide containing a relatively small number of amino acids.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (11)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Integrin beta-3Homo sapiens (human)IC50 (µMol)14.37350.00010.632310.0000AID101721; AID1125597; AID1125599; AID1159172; AID1159175; AID1159177; AID1159180; AID1177798; AID1272590; AID1273112; AID1350411; AID1447361; AID1447362; AID1576814; AID1624883; AID1667325; AID1744034; AID1850995; AID1850996; AID1916148; AID220476; AID220873; AID256968; AID261127; AID290107; AID317262; AID328215; AID393161; AID482478; AID730659; AID730662; AID780747
Integrin beta-3Homo sapiens (human)Ki0.00100.00100.98459.1400AID1355334
Integrin beta-1Homo sapiens (human)IC50 (µMol)4.02050.00010.72528.0000AID1125598; AID1159174; AID1159179; AID1177802; AID1350410; AID1576815; AID1667329; AID1744035; AID1916149; AID730663
Integrin alpha-V Homo sapiens (human)IC50 (µMol)1.05820.00010.625610.0000AID101721; AID1125597; AID1159172; AID1159173; AID1159177; AID1159178; AID1177798; AID1177801; AID1272590; AID1273112; AID1350411; AID1447361; AID1447362; AID1447363; AID1576814; AID1624883; AID1667325; AID1667326; AID1744034; AID1850995; AID1850996; AID1850997; AID1916148; AID214933; AID214935; AID220476; AID220623; AID220626; AID256968; AID256969; AID261127; AID261128; AID290107; AID290108; AID317262; AID317263; AID328215; AID328216; AID393160; AID393161; AID482478; AID730660; AID730661; AID730662; AID780747
Integrin alpha-V Homo sapiens (human)Ki0.00100.00100.00210.0035AID1355334
Integrin alpha-IIbHomo sapiens (human)IC50 (µMol)91.15960.00010.730910.0000AID1125599; AID1159175; AID1159180; AID220873; AID730659
Integrin alpha-5Homo sapiens (human)IC50 (µMol)3.65500.00011.40828.0000AID1125598; AID1159174; AID1159179; AID1177802; AID1350410; AID1576815; AID1667329; AID1744035; AID1916149; AID393160; AID730663
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00050.00021.874210.0000AID780747
Integrin beta-5Homo sapiens (human)IC50 (µMol)2.11380.00010.33725.4000AID1159173; AID1159178; AID1177801; AID1447362; AID1447363; AID1667326; AID1850997; AID214935; AID220623; AID256969; AID261128; AID290108; AID317263; AID328216; AID730661
Integrin beta-6Homo sapiens (human)IC50 (µMol)4.04200.47003.955510.0000AID214933; AID220626; AID730660
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00050.00021.270410.0000AID780747
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00050.00001.819410.0000AID780747
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (161)

Processvia Protein(s)Taxonomy
negative regulation of low-density lipoprotein receptor activityIntegrin beta-3Homo sapiens (human)
positive regulation of protein phosphorylationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
cell-substrate junction assemblyIntegrin beta-3Homo sapiens (human)
cell adhesionIntegrin beta-3Homo sapiens (human)
cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
embryo implantationIntegrin beta-3Homo sapiens (human)
blood coagulationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of gene expressionIntegrin beta-3Homo sapiens (human)
negative regulation of macrophage derived foam cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast migrationIntegrin beta-3Homo sapiens (human)
negative regulation of lipid storageIntegrin beta-3Homo sapiens (human)
response to activityIntegrin beta-3Homo sapiens (human)
smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
platelet activationIntegrin beta-3Homo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
cell-substrate adhesionIntegrin beta-3Homo sapiens (human)
activation of protein kinase activityIntegrin beta-3Homo sapiens (human)
negative regulation of lipid transportIntegrin beta-3Homo sapiens (human)
regulation of protein localizationIntegrin beta-3Homo sapiens (human)
regulation of actin cytoskeleton organizationIntegrin beta-3Homo sapiens (human)
cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of osteoblast proliferationIntegrin beta-3Homo sapiens (human)
heterotypic cell-cell adhesionIntegrin beta-3Homo sapiens (human)
substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
tube developmentIntegrin beta-3Homo sapiens (human)
wound healing, spreading of epidermal cellsIntegrin beta-3Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusIntegrin beta-3Homo sapiens (human)
apolipoprotein A-I-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
wound healingIntegrin beta-3Homo sapiens (human)
apoptotic cell clearanceIntegrin beta-3Homo sapiens (human)
regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
positive regulation of angiogenesisIntegrin beta-3Homo sapiens (human)
positive regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
symbiont entry into host cellIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast proliferationIntegrin beta-3Homo sapiens (human)
mesodermal cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationIntegrin beta-3Homo sapiens (human)
negative regulation of lipoprotein metabolic processIntegrin beta-3Homo sapiens (human)
negative chemotaxisIntegrin beta-3Homo sapiens (human)
regulation of release of sequestered calcium ion into cytosolIntegrin beta-3Homo sapiens (human)
regulation of serotonin uptakeIntegrin beta-3Homo sapiens (human)
angiogenesis involved in wound healingIntegrin beta-3Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeIntegrin beta-3Homo sapiens (human)
platelet aggregationIntegrin beta-3Homo sapiens (human)
cellular response to mechanical stimulusIntegrin beta-3Homo sapiens (human)
cellular response to xenobiotic stimulusIntegrin beta-3Homo sapiens (human)
positive regulation of glomerular mesangial cell proliferationIntegrin beta-3Homo sapiens (human)
blood coagulation, fibrin clot formationIntegrin beta-3Homo sapiens (human)
maintenance of postsynaptic specialization structureIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor diffusion trappingIntegrin beta-3Homo sapiens (human)
positive regulation of substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
positive regulation of adenylate cyclase-inhibiting opioid receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
regulation of trophoblast cell migrationIntegrin beta-3Homo sapiens (human)
regulation of extracellular matrix organizationIntegrin beta-3Homo sapiens (human)
cellular response to insulin-like growth factor stimulusIntegrin beta-3Homo sapiens (human)
negative regulation of endothelial cell apoptotic processIntegrin beta-3Homo sapiens (human)
positive regulation of T cell migrationIntegrin beta-3Homo sapiens (human)
cell migrationIntegrin beta-3Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayIntegrin beta-1Homo sapiens (human)
stress fiber assemblyIntegrin beta-1Homo sapiens (human)
calcium-independent cell-matrix adhesionIntegrin beta-1Homo sapiens (human)
positive regulation of apoptotic processIntegrin beta-1Homo sapiens (human)
positive regulation of glutamate uptake involved in transmission of nerve impulseIntegrin beta-1Homo sapiens (human)
regulation of inward rectifier potassium channel activityIntegrin beta-1Homo sapiens (human)
regulation of spontaneous synaptic transmissionIntegrin beta-1Homo sapiens (human)
reactive gliosisIntegrin beta-1Homo sapiens (human)
G1/S transition of mitotic cell cycleIntegrin beta-1Homo sapiens (human)
establishment of mitotic spindle orientationIntegrin beta-1Homo sapiens (human)
in utero embryonic developmentIntegrin beta-1Homo sapiens (human)
cell migration involved in sprouting angiogenesisIntegrin beta-1Homo sapiens (human)
positive regulation of neuroblast proliferationIntegrin beta-1Homo sapiens (human)
phagocytosisIntegrin beta-1Homo sapiens (human)
cellular defense responseIntegrin beta-1Homo sapiens (human)
cell adhesionIntegrin beta-1Homo sapiens (human)
homophilic cell adhesion via plasma membrane adhesion moleculesIntegrin beta-1Homo sapiens (human)
leukocyte cell-cell adhesionIntegrin beta-1Homo sapiens (human)
cell-matrix adhesionIntegrin beta-1Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin beta-1Homo sapiens (human)
neuroblast proliferationIntegrin beta-1Homo sapiens (human)
muscle organ developmentIntegrin beta-1Homo sapiens (human)
myoblast fusionIntegrin beta-1Homo sapiens (human)
germ cell migrationIntegrin beta-1Homo sapiens (human)
visual learningIntegrin beta-1Homo sapiens (human)
regulation of collagen catabolic processIntegrin beta-1Homo sapiens (human)
positive regulation of fibroblast migrationIntegrin beta-1Homo sapiens (human)
cell migrationIntegrin beta-1Homo sapiens (human)
formation of radial glial scaffoldsIntegrin beta-1Homo sapiens (human)
CD40 signaling pathwayIntegrin beta-1Homo sapiens (human)
cell projection organizationIntegrin beta-1Homo sapiens (human)
lamellipodium assemblyIntegrin beta-1Homo sapiens (human)
B cell differentiationIntegrin beta-1Homo sapiens (human)
extracellular matrix organizationIntegrin beta-1Homo sapiens (human)
positive regulation of cell migrationIntegrin beta-1Homo sapiens (human)
cell-substrate adhesionIntegrin beta-1Homo sapiens (human)
receptor internalizationIntegrin beta-1Homo sapiens (human)
cell adhesion mediated by integrinIntegrin beta-1Homo sapiens (human)
cell-cell adhesion mediated by integrinIntegrin beta-1Homo sapiens (human)
heterotypic cell-cell adhesionIntegrin beta-1Homo sapiens (human)
negative regulation of Rho protein signal transductionIntegrin beta-1Homo sapiens (human)
wound healing, spreading of epidermal cellsIntegrin beta-1Homo sapiens (human)
maintenance of blood-brain barrierIntegrin beta-1Homo sapiens (human)
positive regulation of GTPase activityIntegrin beta-1Homo sapiens (human)
sarcomere organizationIntegrin beta-1Homo sapiens (human)
myoblast differentiationIntegrin beta-1Homo sapiens (human)
negative regulation of neuron differentiationIntegrin beta-1Homo sapiens (human)
positive regulation of fibroblast growth factor receptor signaling pathwayIntegrin beta-1Homo sapiens (human)
positive regulation of angiogenesisIntegrin beta-1Homo sapiens (human)
negative regulation of vasoconstrictionIntegrin beta-1Homo sapiens (human)
symbiont entry into host cellIntegrin beta-1Homo sapiens (human)
mesodermal cell differentiationIntegrin beta-1Homo sapiens (human)
myoblast fate specificationIntegrin beta-1Homo sapiens (human)
axon extensionIntegrin beta-1Homo sapiens (human)
dendrite morphogenesisIntegrin beta-1Homo sapiens (human)
leukocyte tethering or rollingIntegrin beta-1Homo sapiens (human)
regulation of cell cycleIntegrin beta-1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionIntegrin beta-1Homo sapiens (human)
cardiac muscle cell differentiationIntegrin beta-1Homo sapiens (human)
cardiac muscle cell myoblast differentiationIntegrin beta-1Homo sapiens (human)
cardiac cell fate specificationIntegrin beta-1Homo sapiens (human)
cellular response to low-density lipoprotein particle stimulusIntegrin beta-1Homo sapiens (human)
basement membrane organizationIntegrin beta-1Homo sapiens (human)
positive regulation of wound healingIntegrin beta-1Homo sapiens (human)
positive regulation of vascular endothelial growth factor signaling pathwayIntegrin beta-1Homo sapiens (human)
positive regulation of protein localization to plasma membraneIntegrin beta-1Homo sapiens (human)
regulation of synapse pruningIntegrin beta-1Homo sapiens (human)
negative regulation of anoikisIntegrin beta-1Homo sapiens (human)
cell-cell adhesionIntegrin beta-1Homo sapiens (human)
negative regulation of low-density lipoprotein receptor activityIntegrin alpha-V Homo sapiens (human)
angiogenesisIntegrin alpha-V Homo sapiens (human)
vasculogenesisIntegrin alpha-V Homo sapiens (human)
cell adhesionIntegrin alpha-V Homo sapiens (human)
cell-matrix adhesionIntegrin alpha-V Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationIntegrin alpha-V Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin alpha-V Homo sapiens (human)
positive regulation of cell population proliferationIntegrin alpha-V Homo sapiens (human)
negative regulation of macrophage derived foam cell differentiationIntegrin alpha-V Homo sapiens (human)
negative regulation of lipid storageIntegrin alpha-V Homo sapiens (human)
cell migrationIntegrin alpha-V Homo sapiens (human)
positive regulation of cell migrationIntegrin alpha-V Homo sapiens (human)
cell-substrate adhesionIntegrin alpha-V Homo sapiens (human)
negative regulation of lipid transportIntegrin alpha-V Homo sapiens (human)
cell adhesion mediated by integrinIntegrin alpha-V Homo sapiens (human)
positive regulation of osteoblast proliferationIntegrin alpha-V Homo sapiens (human)
heterotypic cell-cell adhesionIntegrin alpha-V Homo sapiens (human)
substrate adhesion-dependent cell spreadingIntegrin alpha-V Homo sapiens (human)
wound healing, spreading of epidermal cellsIntegrin alpha-V Homo sapiens (human)
endodermal cell differentiationIntegrin alpha-V Homo sapiens (human)
apolipoprotein A-I-mediated signaling pathwayIntegrin alpha-V Homo sapiens (human)
apoptotic cell clearanceIntegrin alpha-V Homo sapiens (human)
positive regulation of cell adhesionIntegrin alpha-V Homo sapiens (human)
symbiont entry into host cellIntegrin alpha-V Homo sapiens (human)
negative regulation of lipoprotein metabolic processIntegrin alpha-V Homo sapiens (human)
regulation of phagocytosisIntegrin alpha-V Homo sapiens (human)
negative chemotaxisIntegrin alpha-V Homo sapiens (human)
positive regulation of small GTPase mediated signal transductionIntegrin alpha-V Homo sapiens (human)
ERK1 and ERK2 cascadeIntegrin alpha-V Homo sapiens (human)
calcium ion transmembrane transportIntegrin alpha-V Homo sapiens (human)
transforming growth factor beta productionIntegrin alpha-V Homo sapiens (human)
entry into host cell by a symbiont-containing vacuoleIntegrin alpha-V Homo sapiens (human)
extrinsic apoptotic signaling pathway in absence of ligandIntegrin alpha-V Homo sapiens (human)
positive regulation of intracellular signal transductionIntegrin alpha-V Homo sapiens (human)
negative regulation of entry of bacterium into host cellIntegrin alpha-V Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathwayIntegrin alpha-V Homo sapiens (human)
cell-cell adhesionIntegrin alpha-V Homo sapiens (human)
positive regulation of leukocyte migrationIntegrin alpha-IIbHomo sapiens (human)
cell-matrix adhesionIntegrin alpha-IIbHomo sapiens (human)
integrin-mediated signaling pathwayIntegrin alpha-IIbHomo sapiens (human)
angiogenesisIntegrin alpha-IIbHomo sapiens (human)
cell-cell adhesionIntegrin alpha-IIbHomo sapiens (human)
cell adhesion mediated by integrinIntegrin alpha-IIbHomo sapiens (human)
angiogenesisIntegrin alpha-5Homo sapiens (human)
cell-substrate junction assemblyIntegrin alpha-5Homo sapiens (human)
cell adhesionIntegrin alpha-5Homo sapiens (human)
heterophilic cell-cell adhesion via plasma membrane cell adhesion moleculesIntegrin alpha-5Homo sapiens (human)
leukocyte cell-cell adhesionIntegrin alpha-5Homo sapiens (human)
cell-matrix adhesionIntegrin alpha-5Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin alpha-5Homo sapiens (human)
female pregnancyIntegrin alpha-5Homo sapiens (human)
memoryIntegrin alpha-5Homo sapiens (human)
positive regulation of cell-substrate adhesionIntegrin alpha-5Homo sapiens (human)
CD40 signaling pathwayIntegrin alpha-5Homo sapiens (human)
positive regulation of cell migrationIntegrin alpha-5Homo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathwayIntegrin alpha-5Homo sapiens (human)
cell-substrate adhesionIntegrin alpha-5Homo sapiens (human)
cell adhesion mediated by integrinIntegrin alpha-5Homo sapiens (human)
cell-cell adhesion mediated by integrinIntegrin alpha-5Homo sapiens (human)
heterotypic cell-cell adhesionIntegrin alpha-5Homo sapiens (human)
wound healing, spreading of epidermal cellsIntegrin alpha-5Homo sapiens (human)
endodermal cell differentiationIntegrin alpha-5Homo sapiens (human)
symbiont entry into host cellIntegrin alpha-5Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationIntegrin alpha-5Homo sapiens (human)
positive regulation of sprouting angiogenesisIntegrin alpha-5Homo sapiens (human)
negative regulation of anoikisIntegrin alpha-5Homo sapiens (human)
cell-cell adhesionIntegrin alpha-5Homo sapiens (human)
cell-matrix adhesionIntegrin beta-5Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayIntegrin beta-5Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin beta-5Homo sapiens (human)
cell migrationIntegrin beta-5Homo sapiens (human)
wound healing, spreading of epidermal cellsIntegrin beta-5Homo sapiens (human)
endodermal cell differentiationIntegrin beta-5Homo sapiens (human)
stress fiber assemblyIntegrin beta-5Homo sapiens (human)
symbiont entry into host cellIntegrin beta-5Homo sapiens (human)
epithelial cell-cell adhesionIntegrin beta-5Homo sapiens (human)
cell adhesion mediated by integrinIntegrin beta-5Homo sapiens (human)
cell-cell adhesionIntegrin beta-5Homo sapiens (human)
cell morphogenesisIntegrin beta-6Homo sapiens (human)
inflammatory responseIntegrin beta-6Homo sapiens (human)
immune responseIntegrin beta-6Homo sapiens (human)
cell adhesionIntegrin beta-6Homo sapiens (human)
cell-matrix adhesionIntegrin beta-6Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayIntegrin beta-6Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin beta-6Homo sapiens (human)
response to virusIntegrin beta-6Homo sapiens (human)
cell adhesion mediated by integrinIntegrin beta-6Homo sapiens (human)
wound healingIntegrin beta-6Homo sapiens (human)
surfactant homeostasisIntegrin beta-6Homo sapiens (human)
skin developmentIntegrin beta-6Homo sapiens (human)
symbiont entry into host cellIntegrin beta-6Homo sapiens (human)
lung alveolus developmentIntegrin beta-6Homo sapiens (human)
phospholipid homeostasisIntegrin beta-6Homo sapiens (human)
hard palate developmentIntegrin beta-6Homo sapiens (human)
bone developmentIntegrin beta-6Homo sapiens (human)
bronchiole developmentIntegrin beta-6Homo sapiens (human)
Langerhans cell differentiationIntegrin beta-6Homo sapiens (human)
enamel mineralizationIntegrin beta-6Homo sapiens (human)
cellular response to ionizing radiationIntegrin beta-6Homo sapiens (human)
transforming growth factor beta productionIntegrin beta-6Homo sapiens (human)
cell migrationIntegrin beta-6Homo sapiens (human)
cell-cell adhesionIntegrin beta-6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (37)

Processvia Protein(s)Taxonomy
fibroblast growth factor bindingIntegrin beta-3Homo sapiens (human)
C-X3-C chemokine bindingIntegrin beta-3Homo sapiens (human)
insulin-like growth factor I bindingIntegrin beta-3Homo sapiens (human)
neuregulin bindingIntegrin beta-3Homo sapiens (human)
virus receptor activityIntegrin beta-3Homo sapiens (human)
fibronectin bindingIntegrin beta-3Homo sapiens (human)
protease bindingIntegrin beta-3Homo sapiens (human)
protein disulfide isomerase activityIntegrin beta-3Homo sapiens (human)
protein kinase C bindingIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor bindingIntegrin beta-3Homo sapiens (human)
integrin bindingIntegrin beta-3Homo sapiens (human)
protein bindingIntegrin beta-3Homo sapiens (human)
coreceptor activityIntegrin beta-3Homo sapiens (human)
enzyme bindingIntegrin beta-3Homo sapiens (human)
identical protein bindingIntegrin beta-3Homo sapiens (human)
vascular endothelial growth factor receptor 2 bindingIntegrin beta-3Homo sapiens (human)
metal ion bindingIntegrin beta-3Homo sapiens (human)
cell adhesion molecule bindingIntegrin beta-3Homo sapiens (human)
extracellular matrix bindingIntegrin beta-3Homo sapiens (human)
fibrinogen bindingIntegrin beta-3Homo sapiens (human)
C-X3-C chemokine bindingIntegrin beta-1Homo sapiens (human)
magnesium ion bindingIntegrin beta-1Homo sapiens (human)
virus receptor activityIntegrin beta-1Homo sapiens (human)
fibronectin bindingIntegrin beta-1Homo sapiens (human)
protease bindingIntegrin beta-1Homo sapiens (human)
actin bindingIntegrin beta-1Homo sapiens (human)
integrin bindingIntegrin beta-1Homo sapiens (human)
calcium ion bindingIntegrin beta-1Homo sapiens (human)
protein bindingIntegrin beta-1Homo sapiens (human)
coreceptor activityIntegrin beta-1Homo sapiens (human)
protein-containing complex bindingIntegrin beta-1Homo sapiens (human)
cadherin bindingIntegrin beta-1Homo sapiens (human)
protein heterodimerization activityIntegrin beta-1Homo sapiens (human)
cell adhesion molecule bindingIntegrin beta-1Homo sapiens (human)
collagen binding involved in cell-matrix adhesionIntegrin beta-1Homo sapiens (human)
integrin binding involved in cell-matrix adhesionIntegrin beta-1Homo sapiens (human)
protein tyrosine kinase bindingIntegrin beta-1Homo sapiens (human)
protein kinase bindingIntegrin beta-1Homo sapiens (human)
laminin bindingIntegrin beta-1Homo sapiens (human)
opsonin bindingIntegrin alpha-V Homo sapiens (human)
protein kinase C bindingIntegrin alpha-V Homo sapiens (human)
fibroblast growth factor bindingIntegrin alpha-V Homo sapiens (human)
C-X3-C chemokine bindingIntegrin alpha-V Homo sapiens (human)
insulin-like growth factor I bindingIntegrin alpha-V Homo sapiens (human)
neuregulin bindingIntegrin alpha-V Homo sapiens (human)
virus receptor activityIntegrin alpha-V Homo sapiens (human)
fibronectin bindingIntegrin alpha-V Homo sapiens (human)
protease bindingIntegrin alpha-V Homo sapiens (human)
integrin bindingIntegrin alpha-V Homo sapiens (human)
voltage-gated calcium channel activityIntegrin alpha-V Homo sapiens (human)
protein bindingIntegrin alpha-V Homo sapiens (human)
coreceptor activityIntegrin alpha-V Homo sapiens (human)
metal ion bindingIntegrin alpha-V Homo sapiens (human)
transforming growth factor beta bindingIntegrin alpha-V Homo sapiens (human)
extracellular matrix bindingIntegrin alpha-V Homo sapiens (human)
extracellular matrix protein bindingIntegrin alpha-V Homo sapiens (human)
protein bindingIntegrin alpha-IIbHomo sapiens (human)
identical protein bindingIntegrin alpha-IIbHomo sapiens (human)
metal ion bindingIntegrin alpha-IIbHomo sapiens (human)
extracellular matrix bindingIntegrin alpha-IIbHomo sapiens (human)
molecular adaptor activityIntegrin alpha-IIbHomo sapiens (human)
fibrinogen bindingIntegrin alpha-IIbHomo sapiens (human)
integrin bindingIntegrin alpha-IIbHomo sapiens (human)
virus receptor activityIntegrin alpha-5Homo sapiens (human)
epidermal growth factor receptor bindingIntegrin alpha-5Homo sapiens (human)
platelet-derived growth factor receptor bindingIntegrin alpha-5Homo sapiens (human)
calcium ion bindingIntegrin alpha-5Homo sapiens (human)
protein bindingIntegrin alpha-5Homo sapiens (human)
vascular endothelial growth factor receptor 2 bindingIntegrin alpha-5Homo sapiens (human)
integrin bindingIntegrin alpha-5Homo sapiens (human)
virus receptor activityIntegrin beta-5Homo sapiens (human)
protein bindingIntegrin beta-5Homo sapiens (human)
metal ion bindingIntegrin beta-5Homo sapiens (human)
integrin bindingIntegrin beta-5Homo sapiens (human)
virus receptor activityIntegrin beta-6Homo sapiens (human)
protein bindingIntegrin beta-6Homo sapiens (human)
metal ion bindingIntegrin beta-6Homo sapiens (human)
integrin bindingIntegrin beta-6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (73)

Processvia Protein(s)Taxonomy
glutamatergic synapseIntegrin beta-3Homo sapiens (human)
nucleusIntegrin beta-3Homo sapiens (human)
nucleoplasmIntegrin beta-3Homo sapiens (human)
plasma membraneIntegrin beta-3Homo sapiens (human)
cell-cell junctionIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
external side of plasma membraneIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
apical plasma membraneIntegrin beta-3Homo sapiens (human)
platelet alpha granule membraneIntegrin beta-3Homo sapiens (human)
lamellipodium membraneIntegrin beta-3Homo sapiens (human)
filopodium membraneIntegrin beta-3Homo sapiens (human)
microvillus membraneIntegrin beta-3Homo sapiens (human)
ruffle membraneIntegrin beta-3Homo sapiens (human)
integrin alphav-beta3 complexIntegrin beta-3Homo sapiens (human)
melanosomeIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
postsynaptic membraneIntegrin beta-3Homo sapiens (human)
extracellular exosomeIntegrin beta-3Homo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin beta-3Homo sapiens (human)
glycinergic synapseIntegrin beta-3Homo sapiens (human)
integrin complexIntegrin beta-3Homo sapiens (human)
protein-containing complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-PKCalpha complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-IGF-1-IGF1R complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-HMGB1 complexIntegrin beta-3Homo sapiens (human)
receptor complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-vitronectin complexIntegrin beta-3Homo sapiens (human)
alpha9-beta1 integrin-ADAM8 complexIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-1Homo sapiens (human)
ruffle membraneIntegrin beta-1Homo sapiens (human)
ruffleIntegrin beta-1Homo sapiens (human)
cytoplasmIntegrin beta-1Homo sapiens (human)
plasma membraneIntegrin beta-1Homo sapiens (human)
focal adhesionIntegrin beta-1Homo sapiens (human)
external side of plasma membraneIntegrin beta-1Homo sapiens (human)
cell surfaceIntegrin beta-1Homo sapiens (human)
endosome membraneIntegrin beta-1Homo sapiens (human)
intercalated discIntegrin beta-1Homo sapiens (human)
membraneIntegrin beta-1Homo sapiens (human)
lamellipodiumIntegrin beta-1Homo sapiens (human)
filopodiumIntegrin beta-1Homo sapiens (human)
neuromuscular junctionIntegrin beta-1Homo sapiens (human)
cleavage furrowIntegrin beta-1Homo sapiens (human)
ruffle membraneIntegrin beta-1Homo sapiens (human)
integrin alpha1-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alpha2-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alpha4-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alpha5-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alpha6-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alpha9-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alpha10-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alphav-beta1 complexIntegrin beta-1Homo sapiens (human)
myelin sheath abaxonal regionIntegrin beta-1Homo sapiens (human)
sarcolemmaIntegrin beta-1Homo sapiens (human)
melanosomeIntegrin beta-1Homo sapiens (human)
dendritic spineIntegrin beta-1Homo sapiens (human)
membrane raftIntegrin beta-1Homo sapiens (human)
perinuclear region of cytoplasmIntegrin beta-1Homo sapiens (human)
recycling endosomeIntegrin beta-1Homo sapiens (human)
extracellular exosomeIntegrin beta-1Homo sapiens (human)
synaptic membraneIntegrin beta-1Homo sapiens (human)
glial cell projectionIntegrin beta-1Homo sapiens (human)
Schaffer collateral - CA1 synapseIntegrin beta-1Homo sapiens (human)
cerebellar climbing fiber to Purkinje cell synapseIntegrin beta-1Homo sapiens (human)
integrin alpha3-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alpha7-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alpha8-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alpha11-beta1 complexIntegrin beta-1Homo sapiens (human)
receptor complexIntegrin beta-1Homo sapiens (human)
focal adhesionIntegrin beta-1Homo sapiens (human)
synapseIntegrin beta-1Homo sapiens (human)
integrin complexIntegrin beta-1Homo sapiens (human)
cell surfaceIntegrin beta-1Homo sapiens (human)
cytosolIntegrin alpha-V Homo sapiens (human)
plasma membraneIntegrin alpha-V Homo sapiens (human)
focal adhesionIntegrin alpha-V Homo sapiens (human)
cell surfaceIntegrin alpha-V Homo sapiens (human)
membraneIntegrin alpha-V Homo sapiens (human)
lamellipodium membraneIntegrin alpha-V Homo sapiens (human)
filopodium membraneIntegrin alpha-V Homo sapiens (human)
microvillus membraneIntegrin alpha-V Homo sapiens (human)
ruffle membraneIntegrin alpha-V Homo sapiens (human)
integrin alphav-beta1 complexIntegrin alpha-V Homo sapiens (human)
integrin alphav-beta3 complexIntegrin alpha-V Homo sapiens (human)
integrin alphav-beta5 complexIntegrin alpha-V Homo sapiens (human)
integrin alphav-beta6 complexIntegrin alpha-V Homo sapiens (human)
integrin alphav-beta8 complexIntegrin alpha-V Homo sapiens (human)
specific granule membraneIntegrin alpha-V Homo sapiens (human)
phagocytic vesicleIntegrin alpha-V Homo sapiens (human)
extracellular exosomeIntegrin alpha-V Homo sapiens (human)
integrin complexIntegrin alpha-V Homo sapiens (human)
alphav-beta3 integrin-PKCalpha complexIntegrin alpha-V Homo sapiens (human)
alphav-beta3 integrin-IGF-1-IGF1R complexIntegrin alpha-V Homo sapiens (human)
alphav-beta3 integrin-HMGB1 complexIntegrin alpha-V Homo sapiens (human)
external side of plasma membraneIntegrin alpha-V Homo sapiens (human)
plasma membraneIntegrin alpha-IIbHomo sapiens (human)
focal adhesionIntegrin alpha-IIbHomo sapiens (human)
cell surfaceIntegrin alpha-IIbHomo sapiens (human)
platelet alpha granule membraneIntegrin alpha-IIbHomo sapiens (human)
extracellular exosomeIntegrin alpha-IIbHomo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin alpha-IIbHomo sapiens (human)
blood microparticleIntegrin alpha-IIbHomo sapiens (human)
integrin complexIntegrin alpha-IIbHomo sapiens (human)
external side of plasma membraneIntegrin alpha-IIbHomo sapiens (human)
cell-cell junctionIntegrin alpha-5Homo sapiens (human)
focal adhesionIntegrin alpha-5Homo sapiens (human)
ruffle membraneIntegrin alpha-5Homo sapiens (human)
ruffleIntegrin alpha-5Homo sapiens (human)
endoplasmic reticulumIntegrin alpha-5Homo sapiens (human)
Golgi apparatusIntegrin alpha-5Homo sapiens (human)
plasma membraneIntegrin alpha-5Homo sapiens (human)
focal adhesionIntegrin alpha-5Homo sapiens (human)
cell surfaceIntegrin alpha-5Homo sapiens (human)
cytoplasmic vesicleIntegrin alpha-5Homo sapiens (human)
integrin alpha5-beta1 complexIntegrin alpha-5Homo sapiens (human)
postsynaptic membraneIntegrin alpha-5Homo sapiens (human)
glutamatergic synapseIntegrin alpha-5Homo sapiens (human)
alphav-beta3 integrin-vitronectin complexIntegrin alpha-5Homo sapiens (human)
external side of plasma membraneIntegrin alpha-5Homo sapiens (human)
integrin complexIntegrin alpha-5Homo sapiens (human)
plasma membraneIntegrin beta-5Homo sapiens (human)
focal adhesionIntegrin beta-5Homo sapiens (human)
cell surfaceIntegrin beta-5Homo sapiens (human)
integrin alphav-beta5 complexIntegrin beta-5Homo sapiens (human)
phagocytic vesicleIntegrin beta-5Homo sapiens (human)
extracellular exosomeIntegrin beta-5Homo sapiens (human)
receptor complexIntegrin beta-5Homo sapiens (human)
focal adhesionIntegrin beta-5Homo sapiens (human)
integrin complexIntegrin beta-5Homo sapiens (human)
cell surfaceIntegrin beta-5Homo sapiens (human)
nucleoplasmIntegrin beta-6Homo sapiens (human)
centrosomeIntegrin beta-6Homo sapiens (human)
plasma membraneIntegrin beta-6Homo sapiens (human)
focal adhesionIntegrin beta-6Homo sapiens (human)
external side of plasma membraneIntegrin beta-6Homo sapiens (human)
cell junctionIntegrin beta-6Homo sapiens (human)
integrin alphav-beta6 complexIntegrin beta-6Homo sapiens (human)
integrin complexIntegrin beta-6Homo sapiens (human)
receptor complexIntegrin beta-6Homo sapiens (human)
focal adhesionIntegrin beta-6Homo sapiens (human)
cell surfaceIntegrin beta-6Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (101)

Assay IDTitleYearJournalArticle
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1355340Allosteric activation of integrin alphaVbeta3 receptor in human MSR3 cell membranes assessed as increase in anti-beta3 LIBS integrin antibody AP5 binding at 500 uM incubated for 90 mins by flow cytometry2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Succinimide-Based Conjugates Improve IsoDGR Cyclopeptide Affinity to α
AID1624883Binding affinity to alphaVbeta3 integrin in human SKOV3 cells assessed as inhibition of cell adhesion to fibrinogen measured after 2 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 04-01, Volume: 29, Issue:7
Design and synthesis of novel dual-cyclic RGD peptides for α
AID1695459Antagonist activity at integrin alphavbeta3 receptor in HUVEC cells assessed as inhibition of cell adhesion to human vitronectin at 50 uM preincubated for 30 mins followed by transferring to vitronectin coated plates and measured after 1 hr by DAPI staini2020RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8
Synthesis and initial pharmacology of dual-targeting ligands for putative complexes of integrin αVβ3 and PAR2.
AID328216Displacement of [125I]Echistatin from human placental integrin alpha-V-beta-5 receptor2008Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
Synthesis, SAR and in vitro evaluation of new cyclic Arg-Gly-Asp pseudopentapeptides containing a s-cis peptide bond as integrin alphavbeta3 and alphavbeta5 ligands.
AID780747Binding affinity to soluble truncated human recombinant Fc-tagged alphaVbeta3 and integrins were expressed in HEK293T cells after 2 hrs by competition ELISA-like assay2013Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22
Synthesis and in vitro evaluation of a novel radioligand for αvβ3 integrin receptor imaging: [18F]FPPA-c(RGDfK).
AID101721Inhibition of integrin alpha-v/beta-3 mediated M21 cell adhesion to vitronectin with monoclonal antibody P1F62002Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5
Nanomolar small molecule inhibitors for alphav(beta)6, alphav(beta)5, and alphav(beta)3 integrins.
AID730662Inhibition of vitronectin binding to Integrin alphaVbeta3 receptor (unknown origin) by competitive ELISA2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Biselectivity of isoDGR peptides for fibronectin binding integrin subtypes α5β1 and αvβ6: conformational control through flanking amino acids.
AID1667329Inhibition of fibronectin binding to recombinant human integrin alpha5 (Phe42 to Tyr995 residues) beta1 (Gln21 to Asp728 residues) expressed in CHO cells by ELISA based solid phase binding assay2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Novel cilengitide-based cyclic RGD peptides as αvβ
AID1355339Allosteric activation of integrin alphaVbeta3 receptor in human MSR3 cell membranes assessed as increase in anti-beta3 LIBS integrin antibody AP5 binding at 5 uM incubated for 90 mins by flow cytometry2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Succinimide-Based Conjugates Improve IsoDGR Cyclopeptide Affinity to α
AID220476Inhibition of vitronectin binding to recombinant human alphaV-beta3 integrin2002Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5
Nanomolar small molecule inhibitors for alphav(beta)6, alphav(beta)5, and alphav(beta)3 integrins.
AID1576814Inhibition of human vitronectin binding to human integrin alphavbeta3 receptor after 1 hr by ELISA2019Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
Cyclization of RGD Peptides by Suzuki-Miyaura Cross-Coupling.
AID261128Displacement of [125I]echistatin from AlphaV-beta-5 integrin receptor2006Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5
Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior.
AID317262Displacement of [125I]echistatin from human integrin alpha-V-beta-3 receptor by solid phase assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Discovery of subnanomolar arginine-glycine-aspartate-based alphaVbeta3/alphaVbeta5 integrin binders embedding 4-aminoproline residues.
AID1576816Inhibition of human fibronectin binding to human Integrin alpha2b beta3 receptor incubated for 1 hr by ELISA2019Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
Cyclization of RGD Peptides by Suzuki-Miyaura Cross-Coupling.
AID1159173Inhibition of vitronectin binding to human alphaVbeta5 integrin after 1 hr by ELISA2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides.
AID1350426Inhibition of MDM2 in human U87MG cells assessed as increase in MDM2 mRNA expression at 100 nM after 8 hrs by RT-PCR method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1667325Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta3 (Gly27 to Asp718 residues) expressed in CHO cells by ELISA based solid phase binding assay2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Novel cilengitide-based cyclic RGD peptides as αvβ
AID1125598Inhibition of fibronectin binding to human alpha5beta1 integrin receptor after 1 hr by competitive solid-phase binding ELISA2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Pharmacophoric modifications lead to superpotent αvβ3 integrin ligands with suppressed α5β1 activity.
AID290110Binding affinity to Integrin alpha-2b-beta-3a receptor by ELISA assay2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
Identification of novel short chain 4-substituted indoles as potent alphavbeta3 antagonist using structure-based drug design.
AID1916146Inhibition of human recombinant integrin alphavbeta6 incubated for 1 hr by ELISA assay
AID1350411Inhibition of vitronectin binding to human alphaVbeta3 integrin after 1 hr by ELISA2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1350440Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in PUMA mRNA expression at 100 nM after 24 hrs in presence of MDM2 inhibitor nutlin-3 by RT-PCR method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1916147Inhibition of human recombinant integrin alphavbeta8 incubated for 1 hr by ELISA assay
AID1177798Antagonist activity at alphavbeta3 integrin receptor (unknown origin) by cell-free ELISA2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Strategies to inhibit tumor associated integrin receptors: rationale for dual and multi-antagonists.
AID317263Displacement of [125I]echistatin from human integrin alpha-V-beta-5 receptor by solid phase assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Discovery of subnanomolar arginine-glycine-aspartate-based alphaVbeta3/alphaVbeta5 integrin binders embedding 4-aminoproline residues.
AID1916149Inhibition of human recombinant integrin alpha5beta1 incubated for 1 hr by ELISA assay
AID290109Binding affinity to Integrin alpha-5-beta-5 receptor by ELISA assay2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
Identification of novel short chain 4-substituted indoles as potent alphavbeta3 antagonist using structure-based drug design.
AID1667326Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta5 (Gly24 to Asn719 residues) expressed in CHO cells by ELISA based solid phase binding assay2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Novel cilengitide-based cyclic RGD peptides as αvβ
AID1744035Binding affinity to human integrin alpha5beta1 incubated for 1 hr by ELISA based solid phase integrin binding assay2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Tuning the Biological Activity of RGD Peptides with Halotryptophans†.
AID1576813Binding affinity to integrin alphavbeta3 receptor in human WM115 cells assessed as inhibition of cell adhesion to vitronectin after 0.5 hr by fluorescence assay2019Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
Cyclization of RGD Peptides by Suzuki-Miyaura Cross-Coupling.
AID1850997Inhibition of alphavbeta5 integrin receptor-mediated cell adhesion to vitronectin in human HT-29 cells2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Sortase A-mediated cyclization of novel polycyclic RGD peptides for α
AID1350414Displacement of p53 from MDM2 in human U87MG cells at 100 uM incubated for 10 mins by sandwich ELISA method relative to control2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1159177Binding affinity to alphaVbeta3 integrin (unknown origin)2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides.
AID393160Displacement of [125I]echistatin from integrin alphaVbeta5 receptor in human placenta by microplate scintillation counter2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
Morpholine-based RGD-cyclopentapeptides as alphavbeta3/alphavbeta5 integrin ligands: role of configuration towards receptor binding affinity.
AID1576815Inhibition of human fibronectin binding to human integrin alpha5beta1 incubated for 1 hr by ELISA2019Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
Cyclization of RGD Peptides by Suzuki-Miyaura Cross-Coupling.
AID1125599Inhibition of fibrinogen binding to alpha2bbeta3 integrin receptor (unknown origin) after 1 hr by competitive solid-phase binding ELISA2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Pharmacophoric modifications lead to superpotent αvβ3 integrin ligands with suppressed α5β1 activity.
AID1350452Antiproliferative activity against human U87MG cells at 100 nM after 72 hrs by MTS assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1350415Displacement of p53 from MDM4 in human SHSY-5Y cells at 100 uM incubated for 10 mins by sandwich ELISA method relative to control2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID261127Displacement of [125I]echistatin from AlphaV-beta-3 integrin receptor2006Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5
Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior.
AID1272590Binding affinity to integrin alphav/beta3 heterodimer in human M21 cells assessed as inhibition of integrin-mediated human M21 cell adhesion to vitronectin after 1 hr in presence of MnCl22016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Cyclic RGD peptidomimetics containing 4- and 5-amino-cyclopropane pipecolic acid (CPA) templates as dual αVβ3 and α5β1 integrin ligands.
AID1159181Inhibition of alphavbeta3 integrin-mediated capillary tube formation in HUVEC after 16 hrs by matrigel assay2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides.
AID1177801Antagonist activity at alphavbeta5 integrin receptor (unknown origin) by cell-free ELISA2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Strategies to inhibit tumor associated integrin receptors: rationale for dual and multi-antagonists.
AID1916148Inhibition of human recombinant integrin alphavbeta3 incubated for 1 hr by ELISA assay
AID1350419Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in p53 accumulation at 100 nM after 24 hrs by Western blot method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1350449Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in p21 mRNA expression at 100 nM after 24 hrs by RT-PCR method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1850995Inhibition of alphavbeta3 integrin receptor-mediated cell adhesion to fibrinogen in human SK-OV-3 cells expressing alphavbeta5 integrin receptor2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Sortase A-mediated cyclization of novel polycyclic RGD peptides for α
AID780744Activation of alphaVbeta3 integrin in HUVEC at 10 uM by flow cytometry2013Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22
Synthesis and in vitro evaluation of a novel radioligand for αvβ3 integrin receptor imaging: [18F]FPPA-c(RGDfK).
AID1273112Displacement of biotinylated ECM from human placental integrin alphavbeta3 receptor incubated for 3 hrs2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Insight to the binding mode of triazole RGD-peptidomimetics to integrin-rich cancer cells by NMR and molecular modeling.
AID1355341Allosteric activation of integrin alphaVbeta3 receptor in human MSR3 cell membranes assessed as increase in monoclonal antibody LM609 binding at 500 uM incubated for 90 mins by flow cytometry2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Succinimide-Based Conjugates Improve IsoDGR Cyclopeptide Affinity to α
AID730663Inhibition of fibronectin binding to human Integrin alpha5beta1 receptor by competitive ELISA2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Biselectivity of isoDGR peptides for fibronectin binding integrin subtypes α5β1 and αvβ6: conformational control through flanking amino acids.
AID1350445Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in PUMA mRNA expression at 100 nM after 24 hrs in presence of MDM2 inhibitor nutlin-3 and MDM4 inhibitor SJ-1722550 by RT-PCR method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1350442Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in PUMA mRNA expression at 100 nM after 24 hrs in presence of MDM4 inhibitor SJ-1722550 by RT-PCR method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1355334Binding affinity to human integrin alphaVbeta3 receptor using acetyl-CisoDGRCGVRSSSRTPSDKY-bio probe and streptavidin-peroxidase conjugate incubated for 3 hrs by competitive binding assay2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Succinimide-Based Conjugates Improve IsoDGR Cyclopeptide Affinity to α
AID1159175Inhibition of fibrinogen binding to human alpha2b/beta3 integrin after 1 hr by ELISA2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides.
AID290108Binding affinity to Integrin alpha-v-beta-5 receptor by ELISA assay2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
Identification of novel short chain 4-substituted indoles as potent alphavbeta3 antagonist using structure-based drug design.
AID1159178Binding affinity to alphaVbeta5 integrin (unknown origin)2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides.
AID1850996Inhibition of alphavbeta3 integrin receptor-mediated cell adhesion to fibrinogen in human HEK293 cells2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Sortase A-mediated cyclization of novel polycyclic RGD peptides for α
AID1177802Antagonist activity at alpha5beta1 integrin receptor (unknown origin) by cell-free ELISA2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Strategies to inhibit tumor associated integrin receptors: rationale for dual and multi-antagonists.
AID1159182Inhibition of alphavbeta3 integrin-mediated cell adhesion in HUVEC after 15 mins by matrigel assay2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides.
AID1350467Anti-invasive activity in human U87MG cells at 10 uM after 24 hrs in presence of MDM2 inhibitor nutlin-3 and MDM4 inhibitor SJ-1722550 by transwell assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID730660Inhibition of latency-associated peptide binding to Integrin alphaVbeta6 receptor (unknown origin) by competitive ELISA2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Biselectivity of isoDGR peptides for fibronectin binding integrin subtypes α5β1 and αvβ6: conformational control through flanking amino acids.
AID214935Inhibition of integrin alpha-v/beta-5 mediated UCLAP-3 cell adhesion on vitronectin2002Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5
Nanomolar small molecule inhibitors for alphav(beta)6, alphav(beta)5, and alphav(beta)3 integrins.
AID730661Inhibition of vitronectin binding to Integrin alphaVbeta5 receptor (unknown origin) by competitive ELISA2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Biselectivity of isoDGR peptides for fibronectin binding integrin subtypes α5β1 and αvβ6: conformational control through flanking amino acids.
AID1350421Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in p53 accumulation at 100 nM after 24 hrs in presence of MDM2 inhibitor nutlin-3 by Western blot method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID256968Displacement of [125I]-echistatin from alphavbeta3 integrin receptor2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders.
AID220626Inhibition of fibronectin binding to recombinant human alphaV-beta6 integrin2002Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5
Nanomolar small molecule inhibitors for alphav(beta)6, alphav(beta)5, and alphav(beta)3 integrins.
AID1350463Cell cycle arrest in human U87MG cells assessed as accumulation at G0/G1 phase at 100 nM after 24 hrs2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1916153Antiviral activity against HSV-1 R8102 infected in HEK293T cells assessed as inhibition of viral replication upto 1000 uM using ONPG as substrate incubated for 1 hrs followed by viral infection measured after 90 mins by microplate reader analysis relative
AID1447361Antagonist activity at integrin alphaVbeta3 (unknown origin) expressed in HEK293 cells assessed as reduction in cell adhesion to fibrinogen after 2 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9
New potent and selective αvβ
AID256969Displacement of [125I]-echistatin from alpha-v-beta-5 integrin receptor2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders.
AID1159172Inhibition of vitronectin binding to human alphaVbeta3 integrin after 2 hrs by ELISA2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides.
AID730659Inhibition of fibrinogen binding to Integrin alpha2bbeta3 receptor (unknown origin) by competitive ELISA2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Biselectivity of isoDGR peptides for fibronectin binding integrin subtypes α5β1 and αvβ6: conformational control through flanking amino acids.
AID220873Inhibition of fibrinogen binding to recombinant human platelet glycoprotein alpha IIb beta3 integrin2002Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5
Nanomolar small molecule inhibitors for alphav(beta)6, alphav(beta)5, and alphav(beta)3 integrins.
AID328215Displacement of [125I]echistatin from human placental integrin alphaVbeta3 receptor2008Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
Synthesis, SAR and in vitro evaluation of new cyclic Arg-Gly-Asp pseudopentapeptides containing a s-cis peptide bond as integrin alphavbeta3 and alphavbeta5 ligands.
AID220623Inhibition of vitronectin binding to recombinant human alphaV-beta5 integrin2002Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5
Nanomolar small molecule inhibitors for alphav(beta)6, alphav(beta)5, and alphav(beta)3 integrins.
AID1350410Inhibition of fibronectin binding to soluble alpha5beta1 integrin (unknown origin) after 1 hr by ELISA2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1350464Anti-invasive activity in human U87MG cells at 10 uM after 24 hrs by transwell assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1850998Selectivity ratio of IC50 for alphavbeta5 integrin receptor-mediated cell adhesion to vitronectin in human HT-29 cells to IC50 for alphavbeta3 integrin receptor-mediated cell adhesion to fibrinogen in human HEK293 cells2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Sortase A-mediated cyclization of novel polycyclic RGD peptides for α
AID1159176Selectivity ratio IC50 for human alpha2b/beta3 integrin to IC50 for human alphaVbeta3 integrin2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides.
AID1916156Antiviral activity against HSV-1 K26GFP infected in J cells expressing nectin1 plus alphavbeta8 integrin at 700 uM incubated for 48 hrs followed by viral infection measured after 16 hrs by fluorescent microscopy
AID290107Binding affinity to Integrin alpha-v-beta-3 receptor by ELISA assay2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
Identification of novel short chain 4-substituted indoles as potent alphavbeta3 antagonist using structure-based drug design.
AID1916154Antiviral activity against HSV-1 K26GFP infected in J cells expressing nectin1 plus alphavbeta6/alphavbeta8 integrin at 700 uM incubated for 48 hrs followed by viral infection measured after 16 hrs by fluorescent microscopy
AID1916155Antiviral activity against HSV-1 K26GFP infected in J cells expressing nectin1 plus alphavbeta6 integrin at 700 uM incubated for 48 hrs followed by viral infection measured after 16 hrs by fluorescent microscopy
AID1159179Binding affinity to alpha5beta1 integrin (unknown origin)2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides.
AID1350454Antiproliferative activity against human U87MG cells at 100 nM after 72 hrs in presence of MDM2 inhibitor nutlin-3 by MTS assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1350436Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in PUMA mRNA expression at 100 nM after 24 hrs by RT-PCR method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1350457Antiproliferative activity against human U87MG cells at 100 nM after 72 hrs in presence of MDM2 inhibitor nutlin-3 and MDM4 inhibitor SJ-1722550 by MTS assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1744034Binding affinity to human integrin alphaVbeta3 incubated for 1 hr by ELISA based solid phase integrin binding assay2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Tuning the Biological Activity of RGD Peptides with Halotryptophans†.
AID1447363Antagonist activity at integrin alphaVbeta5 (unknown origin) expressed in HT-29 cells assessed as reduction in cell adhesion to vitronectin after 2 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9
New potent and selective αvβ
AID1125597Inhibition of vitronectin binding to human alphavbeta3 integrin receptor after 1 hr by competitive solid-phase binding ELISA2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Pharmacophoric modifications lead to superpotent αvβ3 integrin ligands with suppressed α5β1 activity.
AID214933Inhibition of integrin alpha-v/beta-6 mediated UCLAP-3 cell adhesion to fibronectin2002Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5
Nanomolar small molecule inhibitors for alphav(beta)6, alphav(beta)5, and alphav(beta)3 integrins.
AID1350431Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in MDM2 mRNA expression at 100 nM after 8 hrs in presence of MDM2 inhibitor nutlin-3 and MDM4 inhibitor SJ-1722550 by RT-PCR method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID393161Displacement of [125I]echistatin from integrin alphaVbeta3 receptor in human placenta by microplate scintillation counter2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
Morpholine-based RGD-cyclopentapeptides as alphavbeta3/alphavbeta5 integrin ligands: role of configuration towards receptor binding affinity.
AID1447362Antagonist activity at integrin alphaVbeta3alphaVbeta5 (unknown origin) expressed in SKOV3 cells assessed as reduction in cell adhesion to fibrinogen after 2 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9
New potent and selective αvβ
AID482478Inhibition of integrin alphaVbeta32010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Emerging targets in osteoporosis disease modification.
AID1350422Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in p53 accumulation at 100 nM after 24 hrs in presence of MDM2 inhibitor nutlin-3 and MDM4 inhibitor SJ-1722550 by Western blot method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1695465Inhibition of Alexa Fluor 647 labelled fibronectin binding to integrin alphavbeta3 receptor (unknown origin) expressed in HEK293FT cells at 5 to 50 uM preincubated for 10 mins followed by fibronectin addition and measured after 30 mins by flow cytometric 2020RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8
Synthesis and initial pharmacology of dual-targeting ligands for putative complexes of integrin αVβ3 and PAR2.
AID1744036Selectivity index, ratio of IC50 for binding affinity to human integrin alpha5beta1 to IC50 for binding affinity to human integrin alphaVbeta32021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Tuning the Biological Activity of RGD Peptides with Halotryptophans†.
AID1159180Binding affinity to alpha2b/beta3 integrin (unknown origin)2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides.
AID1159174Inhibition of fibronectin binding to human alpha5beta1 integrin after 1 hr by ELISA2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (191)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (1.05)18.2507
2000's49 (25.65)29.6817
2010's125 (65.45)24.3611
2020's15 (7.85)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 40.06

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index40.06 (24.57)
Research Supply Index5.41 (2.92)
Research Growth Index5.75 (4.65)
Search Engine Demand Index57.35 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (40.06)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials29 (14.95%)5.53%
Reviews22 (11.34%)6.00%
Case Studies3 (1.55%)4.05%
Observational0 (0.00%)0.25%
Other140 (72.16%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]