Cilengitide: an alphaVbeta3 integrin antagonist that paralyzes cancer cells
ID Source | ID |
---|---|
PubMed CID | 176873 |
CHEMBL ID | 429876 |
CHEBI ID | 177833 |
SCHEMBL ID | 34082 |
MeSH ID | M0382698 |
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 |
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)
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.
Excerpt | Reference | Relevance |
---|---|---|
"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 |
Excerpt | Reference | Relevance |
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"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 |
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.
Excerpt | Reference | Relevance |
---|---|---|
"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 |
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.
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.
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.
Class | Description |
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oligopeptide | A 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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
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AID1695459 | Antagonist 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 staini | 2020 | RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8 | Synthesis and initial pharmacology of dual-targeting ligands for putative complexes of integrin αVβ3 and PAR2. |
AID328216 | Displacement of [125I]Echistatin from human placental integrin alpha-V-beta-5 receptor | 2008 | Bioorganic & 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. |
AID780747 | Binding affinity to soluble truncated human recombinant Fc-tagged alphaVbeta3 and integrins were expressed in HEK293T cells after 2 hrs by competition ELISA-like assay | 2013 | Bioorganic & 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). |
AID101721 | Inhibition of integrin alpha-v/beta-3 mediated M21 cell adhesion to vitronectin with monoclonal antibody P1F6 | 2002 | Journal 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. |
AID730662 | Inhibition of vitronectin binding to Integrin alphaVbeta3 receptor (unknown origin) by competitive ELISA | 2013 | Journal 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. |
AID1667329 | Inhibition 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 assay | 2020 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8 | Novel cilengitide-based cyclic RGD peptides as αvβ |
AID1355339 | Allosteric 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 cytometry | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Succinimide-Based Conjugates Improve IsoDGR Cyclopeptide Affinity to α |
AID220476 | Inhibition of vitronectin binding to recombinant human alphaV-beta3 integrin | 2002 | Journal 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. |
AID1576814 | Inhibition of human vitronectin binding to human integrin alphavbeta3 receptor after 1 hr by ELISA | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Cyclization of RGD Peptides by Suzuki-Miyaura Cross-Coupling. |
AID261128 | Displacement of [125I]echistatin from AlphaV-beta-5 integrin receptor | 2006 | Journal 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. |
AID317262 | Displacement of [125I]echistatin from human integrin alpha-V-beta-3 receptor by solid phase assay | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Discovery of subnanomolar arginine-glycine-aspartate-based alphaVbeta3/alphaVbeta5 integrin binders embedding 4-aminoproline residues. |
AID1576816 | Inhibition of human fibronectin binding to human Integrin alpha2b beta3 receptor incubated for 1 hr by ELISA | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Cyclization of RGD Peptides by Suzuki-Miyaura Cross-Coupling. |
AID1159173 | Inhibition of vitronectin binding to human alphaVbeta5 integrin after 1 hr by ELISA | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides. |
AID1350426 | Inhibition of MDM2 in human U87MG cells assessed as increase in MDM2 mRNA expression at 100 nM after 8 hrs by RT-PCR method | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme. |
AID1667325 | Inhibition 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 assay | 2020 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8 | Novel cilengitide-based cyclic RGD peptides as αvβ |
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AID290110 | Binding affinity to Integrin alpha-2b-beta-3a receptor by ELISA assay | 2007 | European 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. |
AID1916146 | Inhibition of human recombinant integrin alphavbeta6 incubated for 1 hr by ELISA assay | |||
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AID1177798 | Antagonist activity at alphavbeta3 integrin receptor (unknown origin) by cell-free ELISA | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Strategies to inhibit tumor associated integrin receptors: rationale for dual and multi-antagonists. |
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AID1916149 | Inhibition of human recombinant integrin alpha5beta1 incubated for 1 hr by ELISA assay | |||
AID290109 | Binding affinity to Integrin alpha-5-beta-5 receptor by ELISA assay | 2007 | European 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. |
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AID1576813 | Binding affinity to integrin alphavbeta3 receptor in human WM115 cells assessed as inhibition of cell adhesion to vitronectin after 0.5 hr by fluorescence assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Cyclization of RGD Peptides by Suzuki-Miyaura Cross-Coupling. |
AID1850997 | Inhibition of alphavbeta5 integrin receptor-mediated cell adhesion to vitronectin in human HT-29 cells | 2022 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 73 | Sortase A-mediated cyclization of novel polycyclic RGD peptides for α |
AID1350414 | Displacement of p53 from MDM2 in human U87MG cells at 100 uM incubated for 10 mins by sandwich ELISA method relative to control | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme. |
AID1159177 | Binding affinity to alphaVbeta3 integrin (unknown origin) | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides. |
AID393160 | Displacement of [125I]echistatin from integrin alphaVbeta5 receptor in human placenta by microplate scintillation counter | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4 | Morpholine-based RGD-cyclopentapeptides as alphavbeta3/alphavbeta5 integrin ligands: role of configuration towards receptor binding affinity. |
AID1576815 | Inhibition of human fibronectin binding to human integrin alpha5beta1 incubated for 1 hr by ELISA | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Cyclization of RGD Peptides by Suzuki-Miyaura Cross-Coupling. |
AID1125599 | Inhibition of fibrinogen binding to alpha2bbeta3 integrin receptor (unknown origin) after 1 hr by competitive solid-phase binding ELISA | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8 | Pharmacophoric modifications lead to superpotent αvβ3 integrin ligands with suppressed α5β1 activity. |
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AID261127 | Displacement of [125I]echistatin from AlphaV-beta-3 integrin receptor | 2006 | Journal 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. |
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AID1350449 | Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in p21 mRNA expression at 100 nM after 24 hrs by RT-PCR method | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme. |
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AID730660 | Inhibition of latency-associated peptide binding to Integrin alphaVbeta6 receptor (unknown origin) by competitive ELISA | 2013 | Journal 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. |
AID214935 | Inhibition of integrin alpha-v/beta-5 mediated UCLAP-3 cell adhesion on vitronectin | 2002 | Journal 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. |
AID730661 | Inhibition of vitronectin binding to Integrin alphaVbeta5 receptor (unknown origin) by competitive ELISA | 2013 | Journal 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. |
AID1350421 | Inhibition 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 method | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme. |
AID256968 | Displacement of [125I]-echistatin from alphavbeta3 integrin receptor | 2005 | Journal 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. |
AID220626 | Inhibition of fibronectin binding to recombinant human alphaV-beta6 integrin | 2002 | Journal 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. |
AID1350463 | Cell cycle arrest in human U87MG cells assessed as accumulation at G0/G1 phase at 100 nM after 24 hrs | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme. |
AID1916153 | Antiviral 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 | |||
AID1447361 | Antagonist activity at integrin alphaVbeta3 (unknown origin) expressed in HEK293 cells assessed as reduction in cell adhesion to fibrinogen after 2 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9 | New potent and selective αvβ |
AID256969 | Displacement of [125I]-echistatin from alpha-v-beta-5 integrin receptor | 2005 | Journal 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. |
AID1159172 | Inhibition of vitronectin binding to human alphaVbeta3 integrin after 2 hrs by ELISA | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides. |
AID730659 | Inhibition of fibrinogen binding to Integrin alpha2bbeta3 receptor (unknown origin) by competitive ELISA | 2013 | Journal 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. |
AID220873 | Inhibition of fibrinogen binding to recombinant human platelet glycoprotein alpha IIb beta3 integrin | 2002 | Journal 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. |
AID328215 | Displacement of [125I]echistatin from human placental integrin alphaVbeta3 receptor | 2008 | Bioorganic & 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. |
AID220623 | Inhibition of vitronectin binding to recombinant human alphaV-beta5 integrin | 2002 | Journal 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. |
AID1350410 | Inhibition of fibronectin binding to soluble alpha5beta1 integrin (unknown origin) after 1 hr by ELISA | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme. |
AID1350464 | Anti-invasive activity in human U87MG cells at 10 uM after 24 hrs by transwell assay | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme. |
AID1850998 | Selectivity 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 cells | 2022 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 73 | Sortase A-mediated cyclization of novel polycyclic RGD peptides for α |
AID1159176 | Selectivity ratio IC50 for human alpha2b/beta3 integrin to IC50 for human alphaVbeta3 integrin | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides. |
AID1916156 | Antiviral 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 | |||
AID290107 | Binding affinity to Integrin alpha-v-beta-3 receptor by ELISA assay | 2007 | European 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. |
AID1916154 | Antiviral 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 | |||
AID1916155 | Antiviral 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 | |||
AID1159179 | Binding affinity to alpha5beta1 integrin (unknown origin) | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides. |
AID1350454 | Antiproliferative activity against human U87MG cells at 100 nM after 72 hrs in presence of MDM2 inhibitor nutlin-3 by MTS assay | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme. |
AID1350436 | Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in PUMA mRNA expression at 100 nM after 24 hrs by RT-PCR method | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme. |
AID1350457 | Antiproliferative 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 assay | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme. |
AID1744034 | Binding affinity to human integrin alphaVbeta3 incubated for 1 hr by ELISA based solid phase integrin binding assay | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1 | Tuning the Biological Activity of RGD Peptides with Halotryptophans†. |
AID1447363 | Antagonist activity at integrin alphaVbeta5 (unknown origin) expressed in HT-29 cells assessed as reduction in cell adhesion to vitronectin after 2 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9 | New potent and selective αvβ |
AID1125597 | Inhibition of vitronectin binding to human alphavbeta3 integrin receptor after 1 hr by competitive solid-phase binding ELISA | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8 | Pharmacophoric modifications lead to superpotent αvβ3 integrin ligands with suppressed α5β1 activity. |
AID214933 | Inhibition of integrin alpha-v/beta-6 mediated UCLAP-3 cell adhesion to fibronectin | 2002 | Journal 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. |
AID1350431 | Inhibition 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 method | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme. |
AID393161 | Displacement of [125I]echistatin from integrin alphaVbeta3 receptor in human placenta by microplate scintillation counter | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4 | Morpholine-based RGD-cyclopentapeptides as alphavbeta3/alphavbeta5 integrin ligands: role of configuration towards receptor binding affinity. |
AID1447362 | Antagonist activity at integrin alphaVbeta3alphaVbeta5 (unknown origin) expressed in SKOV3 cells assessed as reduction in cell adhesion to fibrinogen after 2 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9 | New potent and selective αvβ |
AID482478 | Inhibition of integrin alphaVbeta3 | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11 | Emerging targets in osteoporosis disease modification. |
AID1350422 | Inhibition 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 method | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme. |
AID1695465 | Inhibition 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 | 2020 | RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8 | Synthesis and initial pharmacology of dual-targeting ligands for putative complexes of integrin αVβ3 and PAR2. |
AID1744036 | Selectivity index, ratio of IC50 for binding affinity to human integrin alpha5beta1 to IC50 for binding affinity to human integrin alphaVbeta3 | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1 | Tuning the Biological Activity of RGD Peptides with Halotryptophans†. |
AID1159180 | Binding affinity to alpha2b/beta3 integrin (unknown origin) | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides. |
AID1159174 | Inhibition of fibronectin binding to human alpha5beta1 integrin after 1 hr by ELISA | 2014 | Journal 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] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 2 (1.05) | 18.2507 |
2000's | 49 (25.65) | 29.6817 |
2010's | 125 (65.45) | 24.3611 |
2020's | 15 (7.85) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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.
| This Compound (40.06) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 29 (14.95%) | 5.53% |
Reviews | 22 (11.34%) | 6.00% |
Case Studies | 3 (1.55%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 140 (72.16%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |