Page last updated: 2024-12-07

arginyl-glycyl-aspartic acid

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Description

arginyl-glycyl-aspartic acid: amino acid sequence of basic unit of widespread cellular recognition system [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID104802
CHEMBL ID313763
CHEBI ID158966
SCHEMBL ID19139
MeSH IDM0138287

Synonyms (49)

Synonym
CHEMBL313763 ,
99896-85-2
rgd tripeptide
arg-gly-asp, >=97% (tlc)
l-aspartic acid, n-(n-l-arginylglycyl)-
arginyl-glycyl-asparagilin
n-(n-l-arginylglycyl)-l-aspartic acid
arginyl-glycyl-aspartic acid
rgd peptide
rgd tripeptide sequence
arg-gly-asp ,
f-336
NCGC00167210-01
CHEBI:158966
(2s)-2-[[2-[[(2s)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]acetyl]amino]butanedioic acid
(s)-2-[2-((s)-2-amino-5-guanidino-pentanoylamino)-acetylamino]-succinic acid
bdbm50107402
(s)-2-[2-((s)-2-amino-5-carbamimidoyl-pentanoylamino)-acetylamino]-succinic acid
2-[2-(2-amino-5-guanidino-pentanoylamino)-acetylamino]-succinic acid(rgd)
119865-10-0
bitiscetin
bitistatin
124123-27-9
unii-78vo7f77pn
78vo7f77pn ,
l-arginyl-glycyl-l-aspartic acid
arginylglycylaspartic acid
AKOS015854089
AKOS015902678
S8008
SCHEMBL19139
rgd ,
l-aspartic acid, l-arginylglycyl-
AC-32859
mfcd00057952
IYMAXBFPHPZYIK-BQBZGAKWSA-N
AS-61345
(2s)-2-{2-[(2s)-2-amino-5-carbamimidamidopentanamido]acetamido}butanedioic acid
HY-P0278
(s)-2-(2-((s)-2-amino-5-guanidinopentanamido)acetamido)succinic acid
DTXSID30912420
Q4068819
arginine-glycine-aspartic acid
rgd peptides
CCG-267987
H11917
arginyl-glycyl-aspartic acid; rgd peptide
A900178
l-aspartic acid,l-arginylglycyl-

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" However, intratumoral administration of AdRGD expressing tumor necrosis factor alpha (AdRGD-TNFalpha) at high dose revealed not only the dramatic reinforcement of anti-tumor effect but also serious adverse effects, such as body weight reduction and sudden death, caused by high-level TNF-alpha leakage from the tumor into circulation."( Optimization of antitumor efficacy and safety of in vivo cytokine gene therapy using RGD fiber-mutant adenovirus vector for preexisting murine melanoma.
Hayakawa, T; Mayumi, T; Mizuguchi, H; Mizuno, N; Okada, N; Okada, Y; Takahashi, K, 2004
)
0.32
" On the other hand, AdRGD-Tyr/HSVtk and AdRGD-TERT/HSVtk did not induce severe adverse effects even when they were intravenously injected into mice at 10(9) plaque-forming units (PFU), whereas mice injected with AdRGD-CMV/HSVtk at 10(8) PFU exhibited body weight reduction and serum level increase of biochemical enzymes for hepatotoxicity."( Transcriptional targeting of RGD fiber-mutant adenovirus vectors can improve the safety of suicide gene therapy for murine melanoma.
Hayakawa, T; Mayumi, T; Mizuguchi, H; Nakagawa, S; Okada, N; Okada, Y, 2005
)
0.33
" In the transplanted islets, iNOS and toxic amounts of NO are produced as a result of islets infiltration with inflammatory cells and production of proinflammatory cytokines."( Osteopontin protects the islets and beta-cells from interleukin-1 beta-mediated cytotoxicity through negative feedback regulation of nitric oxide.
Arafat, HA; Chipitsyna, G; Dafoe, DC; Gabbeta, J; Gong, Q; Katakam, AK; Vancha, AR, 2007
)
0.34
" Our results demonstrate that G4 dendrimers, which have amino functional groups, are toxic and attenuate growth and development of zebrafish embryos at sublethal concentrations; however, G3."( Developmental toxicity of low generation PAMAM dendrimers in zebrafish.
Dengler, E; Heideman, W; Heiden, TC; Kao, WJ; Peterson, RE, 2007
)
0.34
"To explore the structural dependence of the oral potency and side effect of estrogen-RGD peptide conjugates, here six novel conjugates were prepared via introducing RGD-tetrapeptides into both 3- and 17-positions of estradiol, and introducing RGD-octapeptides into 3-position of estrone."( 3D QSAR of novel estrogen-RGD peptide conjugates: getting insight into structural dependence of anti-osteoporosis activity and side effect of estrogen in ERT.
Li, C; Liu, J; Peng, L; Peng, S; Zhang, X; Zhao, M, 2009
)
0.35
"Our data demonstrate that the single and repeated intravenous injection of QD800-RGD at a dose needed for successful tumor imaging in vivo is not toxic to mice."( Toxicity assessment of repeated intravenous injections of arginine-glycine-aspartic acid peptide conjugated CdSeTe/ZnS quantum dots in mice.
Bai, YL; Chen, D; Tang, H; Wang, YW; Yang, K, 2014
)
0.4
"5 µmol/kg/d of Dex, and the conjugates, but not Dex, exhibited no toxic action."( RGD(F/S/V)-Dex: towards the development of novel, effective, and safe glucocorticoids.
Jiang, X; Peng, S; Song, Y; Wang, Y; Wu, J; Zhao, M; Zhao, S; Zhu, H, 2016
)
0.43
" The stimuli led to encapsulated DOX's initial burst release and subsequent sustained release for anti-tumor therapy which was verified to be more effective and have less adverse effects than free DOX."( Targeted and pH-facilitated theranostic of orthotopic gastric cancer via phase-transformation doxorubicin-encapsulated nanoparticles enhanced by low-intensity focused ultrasound (LIFU) with reduced side effect.
Liu, Z; Ran, H; Wang, Y; Wang, Z; Zhou, S, 2019
)
0.51

Pharmacokinetics

ExcerptReferenceRelevance
" The half-life of RGDpep-HuMab (90 min) was still considerably longer than that of free RGD peptides (<10 min)."( Targeting of RGD-modified proteins to tumor vasculature: a pharmacokinetic and cellular distribution study.
Bos, EJ; de Leij, LF; Kok, RJ; Meijer, DK; Molema, G; Moorlag, HE; Proost, JH; Schraa, AJ, 2002
)
0.31
" We studied the tumor targeting efficacy and in vivo pharmacokinetic properties of 125I-RGD-mPEG by means of direct tissue sampling and autoradiography in mice xenografted subcutaneously with U87MG glioblastoma."( Pharmacokinetics and tumor retention of 125I-labeled RGD peptide are improved by PEGylation.
Bading, JR; Chen, X; Conti, PS; Park, R; Shahinian, AH, 2004
)
0.32
" The fluorescence images were acquired using an intensified charge-coupled device system and were analyzed with a three-compartment pharmacokinetic (PK) model to determine uptake parameters in the tumor and normal tissue regions of interest as a function of administered dose."( Imaging dose-dependent pharmacokinetics of an RGD-fluorescent dye conjugate targeted to alpha v beta 3 receptor expressed in Kaposi's sarcoma.
Houston, JP; Ke, S; Kwon, S; Li, C; Sevick-Muraca, EM; Wang, W; Wu, Q,
)
0.13
" The pharmacokinetic parameters in tumor-bearing mice were analyzed by PKAnalyst."( Evaluation of pharmacokinetics of bioreducible gene delivery vectors by real-time PCR.
Manickam, DS; Oupický, D; Wu, C; Zhou, QH, 2009
)
0.35
"(18)F-FPPRGD2 has desirable pharmacokinetic and biodistribution properties."( Pilot pharmacokinetic and dosimetric studies of (18)F-FPPRGD2: a PET radiopharmaceutical agent for imaging α(v)β(3) integrin levels.
Berganos, R; Burton, L; Chang, E; Chen, X; Chin, FT; Gambhir, SS; Goris, ML; Iagaru, AH; Kardan, A; Liu, S; Mittra, ES; Shen, B, 2011
)
0.37
" However, HM-3 has relatively short half-life in vivo."( In vivo pharmacokinetics, immunogenicity and mechanism of PEGylated antitumor polypeptide.
Huang, X; Li, W; Li, Y; Liu, Z; Pan, L; Pu, C; Ren, Y; Xu, HM; Yang, Y; Zhang, C, 2012
)
0.38
" The drug concentration in plasma was determined and the pharmacokinetic behaviour was compared."( [In vivo imaging in tumor-bearing animals and pharmacokinetics of PEGylated liposomes modified with RGD cyclopeptide].
Deng, LH; Tang, CY; Tu, LX; Wu, CB; Xu, YH, 2012
)
0.38
" Doxorubicin as a model anticancer drug was loaded into liposomes using an ammonium sulfate gradient method to investigate the encapsulation efficiency, cellular uptake by the integrin-overexpressing human glioma cell line U87MG in vitro, and pharmacokinetic properties in Sprague-Dawley rats."( Cyclic RGD peptide-modified liposomal drug delivery system: enhanced cellular uptake in vitro and improved pharmacokinetics in rats.
Chen, Z; Deng, J; Tao, T; Zhao, Y, 2012
)
0.38
"64 h ng/mg; the elimination half-life (T1/2) in retina was 104."( Pharmacokinetics of HM-3 after intravitreal administration in mice.
Hu, J; Li, W; Liu, Q; Liu, X; Shen, H; Xia, X; Xie, P; Xu, H; Yuan, D; Yuan, S, 2014
)
0.4
"The pharmacokinetic profiles of intravitreal administration HM-3 provide the basis for the development of reasonable dosing regimens of clinical choroidal neovascularization (CNV) treatment."( Pharmacokinetics of HM-3 after intravitreal administration in mice.
Hu, J; Li, W; Liu, Q; Liu, X; Shen, H; Xia, X; Xie, P; Xu, H; Yuan, D; Yuan, S, 2014
)
0.4
" In the case of peptide-based radiotracers, the modification and addition of a linker or spacer functional group often offer faster in vivo pharmacokinetic behavior."( Improved Pharmacokinetics Following PEGylation and Dimerization of a c(RGD-ACH-K) Conjugate Used for Tumor Positron Emission Tomography Imaging.
Kim, BI; Kim, JY; Kim, SW; Lee, JW; Lee, KC; Lee, YJ; Park, JA; Shin, UC, 2016
)
0.43
" A drug with a short half-life in the blood is less available at a target organ."( Novel "Add-On" Molecule Based on Evans Blue Confers Superior Pharmacokinetics and Transforms Drugs to Theranostic Agents.
Chen, H; Chen, X; Jacobson, O; Kiesewetter, DO; Liu, Y; Ma, Y; Niu, G; Weiss, ID; Wu, H, 2017
)
0.46

Compound-Compound Interactions

ExcerptReferenceRelevance
"RGD, either alone or in combination with CDDP."( A novel CRAd in combination with cisplatin enhanced the antitumor efficacy in ovarian cancer.
Liu, Y; Wei, Y; Yin, X; Zhang, B; Zhang, P; Zheng, J, 2011
)
0.37
"RGD in combination with CDDP was a potential therapeutic modality for the therapy in ovarian cancer."( A novel CRAd in combination with cisplatin enhanced the antitumor efficacy in ovarian cancer.
Liu, Y; Wei, Y; Yin, X; Zhang, B; Zhang, P; Zheng, J, 2011
)
0.37
" Our purpose was to elucidate whether the use of the oncolytic adenovirus Δ24-RGD alone or in combination with standard chemotherapy would be effective, in vitro and in vivo, against osteosarcoma."( The oncolytic adenovirus Δ24-RGD in combination with cisplatin exerts a potent anti-osteosarcoma activity.
Alonso, MM; Fueyo, J; Gomez-Manzano, C; Jauregui, P; Julián, MS; Lecanda, F; Marrodan, L; Martinez-Velez, N; Patiño-García, A; Sierrasesúmaga, L; Toledo, G; Torre, W; Urquiza, L; Vera, B; Xipell, E; Zalacain, M; Zandueta, C, 2014
)
0.4
" Polymeric nanoparticles combined with ultrasound (US) are widely applied in cancer treatment due to their time applications, low cost, simplicity, and safety."( Prevention of Oxidized Low Density Lipoprotein-Induced Endothelial Cell Injury by DA-PLGA-PEG-cRGD Nanoparticles Combined with Ultrasound.
Du, L; Duan, Y; Huang, H; Huang, L; Li, Z; Sun, Y, 2017
)
0.46

Bioavailability

ExcerptReferenceRelevance
"Endotoxemia, in man, has been associated with an autooxidative reduction in the bioavailability of polymorphonuclear leukocyte receptors."( Regulation of intracellular polymorphonuclear leukocyte Fc receptors by lipopolysaccharide.
D'Amico, R; Simms, HH, 1994
)
0.29
" It also appears to have a greater association with resting platelets in the blood, which may increase bioavailability and delay metabolic breakdown."( In vitro platelet binding compared with in vivo thrombus imaging using alpha(IIb)beta3-targeted radioligands.
Knight, LC; Maurer, AH; Romano, JE, 1998
)
0.3
" However, the clinical development of orally active RGD analogs has been hindered by the low oral bioavailability of many such RGD analogs."( A coumarin-based prodrug strategy to improve the oral absorption of RGD peptidomimetics.
Borchardt, RT; Camenisch, G; Hugger, E; Sane, DC; Wang, B; Wang, W; Wheeler, GL; Zhang, H, 2000
)
0.31
" However, the low oral bioavailability for this class of compounds has been hindering their clinical development."( Orally active peptidomimetic RGD analogs that are glycoprotein IIb/IIIa antagonists.
Borchardt, RT; Wang, B; Wang, W, 2000
)
0.31
" Modification of the beta-alanine 3-substituents alters the potency and physicochemical properties of these receptor antagonists and in some cases provides orally bioavailable alpha(v)beta(3) inhibitors."( Non-peptide alpha(v)beta(3) antagonists. Part 3: identification of potent RGD mimetics incorporating novel beta-amino acids as aspartic acid replacements.
Askew, BC; Brashear, KM; Breslin, MJ; Coleman, PJ; Duggan, ME; Fernandez-Metzler, C; Hartman, GD; Hoffman, WF; Hunt, CA; Hutchinson, JH; Leu, CT; Libby, LA; Lynch, JJ; Lynch, R; Ma, B; McVean, CA; Merkle, KM; Prueksaritanont, T; Rodan, GA; Rodan, SB; Stump, GL; Wallace, AA, 2002
)
0.31
" One explanation may be the large complex size, which serves to decrease the bioavailability of the trimeric sCAR-adenovirus complexes."( Targeting adenoviral vectors by using the extracellular domain of the coxsackie-adenovirus receptor: improved potency via trimerization.
Idamakanti, N; Kaleko, M; Kaloss, M; Kim, J; Kylefjord, H; Mulgrew, K; Ryan, PC; Smith, T; Stevenson, SC, 2002
)
0.31
" In vivo biodistribution studies of (76)Br-labeled dendritic nanoprobes showed excellent bioavailability for the targeted and nontargeted nanoprobes."( Biodegradable dendritic positron-emitting nanoprobes for the noninvasive imaging of angiogenesis.
Abendschein, D; Almutairi, A; Ananth, A; Anderson, CJ; Capoccia, B; Fréchet, JM; Guillaudeu, S; Hagooly, A; Rossin, R; Shokeen, M; Welch, MJ, 2009
)
0.35
" Its water absorption rate and water retention rate were 772% and 206% respectively."( [Preparation and characterization of an extracellular matrix of artificial tendon tissue from natural macromolecules].
Wan, L; Xiong, Y, 2008
)
0.35
" In addition to their drug targeting application and their ability to improve bioavailability of drugs, nanoparticles can be designed to allow their detection with a variety of imaging methodologies."( Multifunctional nanoemulsion platform for imaging guided therapy evaluated in experimental cancer.
Calcagno, C; Dijk, WJ; Fayad, ZA; Gianella, A; Griffioen, AW; Jarzyna, PA; Kann, B; Mani, V; Mulder, WJ; Ramachandran, S; Storm, G; Tang, J; Thijssen, VL, 2011
)
0.37
" Despite significant anti-tumor efficacies and bio-safety profiles of curcumin, poor systemic bioavailability is retarding its clinical success."( Tumor growth inhibition through targeting liposomally bound curcumin to tumor vasculature.
Barui, S; Chaudhuri, A; Mondal, G; Saha, S, 2013
)
0.39
"The poor aqueous solubility and low bioavailability of curcumin restrict its clinical application for cancer treatment."( Novel tumor-targeting, self-assembling peptide nanofiber as a carrier for effective curcumin delivery.
Chu, L; Liu, J; Liu, Q; Song, N; Xu, H; Yang, C; Zhang, Y, 2014
)
0.4
"Adequate retention in systemic circulation is the preliminary requirement for systemic gene delivery to afford high bioavailability into the targeted site."( Targeted gene delivery by polyplex micelles with crowded PEG palisade and cRGD moiety for systemic treatment of pancreatic tumors.
Chen, Q; Dirisala, A; Ge, Z; Ishii, T; Itaka, K; Kano, MR; Kataoka, K; Liu, X; Matsumoto, Y; Nomoto, T; Oba, M; Osada, K; Tockary, TA; Toh, K; Uchida, S, 2014
)
0.4
" As we expected, these tri-component polynorbornenes exhibit significant enhancement in anti-thrombotic efficacy and bioavailability in vivo."( A modular designed copolymer with anti-thrombotic activity and imaging capability.
Chen, B; Feng, K; Peng, S; Tung, CH; Wu, LZ; Xie, N; Zhang, LP; Zhao, M, 2014
)
0.4
" Suramin bioavailability and function were demonstrated by attenuated M1 polarization of THP-1 cells compared to positive control."( Drug-triggered and cross-linked self-assembling nanofibrous hydrogels.
Hartgerink, JD; Jalan, AA; Kumar, VA; Li, IC; Sarkar, B; Shi, S; Wang, BK; Wickremasinghe, NC, 2015
)
0.42
" However, poor water solubility and low bioavailability limit its wide application in clinical practice."( Anticancer Efficacy of Targeted Shikonin Liposomes Modified with RGD in Breast Cancer Cells.
Cai, D; Fan, L; Li, J; Sun, J; Wang, Q; Wen, X; Wu, Y; Yue, L; Zhou, L, 2018
)
0.48
" This study aimed to prepare arginyl-glycyl-aspartic acid (RGD) containing nanostructured lipid carrier (NLC-RGD) to improve the bioavailability of galangin and explore its ability in improving the cytotoxic effects of doxorubicin (DOX)."( Targeted nanostructured lipid carrier containing galangin as a promising adjuvant for improving cytotoxic effects of chemotherapeutic agents.
Bahramifar, A; Emameh, RZ; Ghorbani, M; Hajipour, H; Nouri, M; Taheri, RA, 2021
)
0.91
" Therefore, a drug discovery programme to identify an orally bioavailable small molecule αvβ6 arginyl-glycinyl-aspartic acid (RGD)-mimetic was initiated."( Pharmacological characterisation of GSK3335103, an oral αvβ6 integrin small molecule RGD-mimetic inhibitor for the treatment of fibrotic disease.
Barksby, BS; Barnes, R; Barrett, JW; Barrett, TN; Borthwick, LA; Burgoyne, RA; Fisher, AJ; Gower, E; Hatley, RJD; Jenkins, RG; John, AE; Luckett, JC; Macdonald, SJF; Man, Y; Marshall, RP; Morrison, VS; Procopiou, PA; Pun, KT; Roper, JA; Slack, RJ; Wilkinson, AL, 2021
)
0.62

Dosage Studied

ExcerptRelevanceReference
" RGDS was a weaker inhibitor, and produced a biphasic dose-response curve; SDRG was inactive."( Inhibition of platelet adhesion to fibrin(ogen) in flowing whole blood by Arg-Gly-Asp and fibrinogen gamma-chain carboxy terminal peptides.
Cavero, I; de Groot, PG; Endenburg, SC; Hantgan, RR; Marguerie, G; Sixma, JJ; Uzan, A, 1992
)
0.28
" Infused RGDV decreased the accumulation of both platelets and fibrin on the collagen substrate in a dose-response manner."( RGDV peptide selectively inhibits platelet-dependent thrombus formation in vivo. Studies using a baboon model.
Cadroy, Y; Hanson, SR; Houghten, RA, 1989
)
0.28
" Four ester prodrug/acid active metabolite pairs (2a/2e, 60a/60e, 62a/62e, 63a/63e) from the ABAS series which varied in their 3-substituent on the beta-amino ester "aspartate mimetic" were prepared in enantiomerically enriched form (> 95:5), and they were evaluated in canine studies for their ability to block collagen-induced aggregation in platelet-rich plasma, the elimination profile (t1/2 beta-phase), repeated oral dosing studies, and oral systemic availability."( Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor antagonists.
Bovy, PR; Garland, RB; Lindmark, RJ; Rao, SA; Rico, JG; Rogers, TE; Schretzman, LA; Tjoeng, FS; Williams, K; Zablocki, JA, 1995
)
0.29
" Like all GPIIb/IIIa antagonists, DMP 728 has a steep dose-response relationship in inhibiting platelet aggregation."( Platelet GPIIb/IIIa receptor occupancy studies using a novel fluoresceinated cyclic Arg-Gly-Asp peptide.
Bozarth, JM; Flint, SK; Forsythe, MS; Jackson, SA; Mousa, SA; Tsao, PW, 1995
)
0.29
" However, the clinical development of oral dosage forms of these RGD analogs has been hindered by their low intestinal mucosal permeability."( Synthesis and evaluation of novel coumarin-based esterase-sensitive cyclic prodrugs of peptidomimetic RGD analogs with improved membrane permeability.
Borchardt, RT; Camenisch, GP; Elmo, J; Wang, B; Wang, W; Zhang, H, 1999
)
0.3
" Treatment with a pharmacologic dosage of retinoic acid altered the TSP-1 cell adhesion mechanism in both cell lines in that neither heparin nor micromolar concentrations of the RGD peptide inhibited attachment; after treatment, attachment was inhibited by the CSVTCG peptide located in the type I repeat domain of TSP-1 and a recombinant adhesion domain (CLESH-1) from CD36."( Retinoic acid alters the mechanism of attachment of malignant astrocytoma and neuroblastoma cells to thrombospondin-1.
Gladson, CL; Grammer, JR; Murphy-Ullrich, JE; Pearce, SF; Pijuan-Thompson, V; Silverstein, RL; Stewart, J; Tuszynski, GP, 1999
)
0.3
", Whitehouse Station, New Jersey]) all sought to identify dosing regimens that would establish and maintain >80 % inhibition of ex vivo platelet aggregation throughout the duration of intravenous infusion."( Platelet aggregation inhibition with glycoprotein IIb--IIIa inhibitors.
Proimos, G, 2001
)
0.31
" The authors currently are conducting a dose deescalation study to determine the threshold dosage required for RGD mimetic binding to radiation activated receptor."( Radiation-mediated control of drug delivery.
Chakravarthy, A; Cmelak, A; Geng, L; Giorgio, T; Hallahan, DE; Martin, W; Qu, S; Scarfone, C, 2001
)
0.31
" In addition, Ad-RGD-TNFalpha required about one-tenth the dosage of Ad-TNFalpha for induction of equal therapeutic effects upon intratumoral injection into established B16 BL6 tumors."( Fiber-mutant technique can augment gene transduction efficacy and anti-tumor effects against established murine melanoma by cytokine-gene therapy using adenovirus vectors.
Hayakawa, T; Kanehira, M; Mayumi, T; Mizuguchi, H; Mizuno, N; Nakagawa, S; Nishino, N; Okada, N; Okada, Y; Takahashi, K, 2002
)
0.31
" A dose-response relation in NOS activity was observed in either Fn treated or RGD treated group."( [Fibronectin or RGD peptide promotes nitric oxide synthesis of rabbit bronchial epithelial cells].
Luo, ZQ; Qin, XQ; Sun, XH; Xiang, Y; Zhang, CQ, 2000
)
0.31
" Ad-RGD-TNFalpha required one-tenth the dosage of Ad-TNFalpha to induce an equal therapeutic effect."( Tumor necrosis factor alpha-gene therapy for an established murine melanoma using RGD (Arg-Gly-Asp) fiber-mutant adenovirus vectors.
Fujita, T; Hayakawa, T; Mayumi, T; Mizuguchi, H; Mizuno, N; Nakagawa, S; Okada, N; Okada, Y; Takahashi, K; Yamamoto, A, 2002
)
0.31
" The results of this pilot study thus provide only weak evidence that coating of titanium implants with RGD peptides in the present form and dosage may increase periimplant bone formation in the alveolar process."( Effect of RGD peptide coating of titanium implants on periimplant bone formation in the alveolar crest. An experimental pilot study in dogs.
Dard, M; Hoogestraat, D; Meyer, J; Rössler, S; Scharnweber, D; Schliephake, H; Sewing, A, 2002
)
0.31
" To achieve this goal, a frequently used cell adhesion peptide Arg-Gly-Asp (RGD) was covalently incorporated into poly(ethylene glycol) diacrylate (PEODA) hydrogel and its dosage effect (0."( The effect of incorporating RGD adhesive peptide in polyethylene glycol diacrylate hydrogel on osteogenesis of bone marrow stromal cells.
Elisseeff, J; Lee, H; Manson, PN; Wang, DA; Williams, CG; Yang, F, 2005
)
0.33
" It was concluded that the targeting properties of the prepared delivery system would potentially improve the therapeutic benefits of combretastatin A4 compared with nontargeted liposomes or solution dosage forms."( A tumor vasculature targeted liposome delivery system for combretastatin A4: design, characterization, and in vitro evaluation.
Kiani, MF; Moore, BM; Nallamothu, R; Pattillo, CB; Scott, RC; Thoma, LA; Wood, GC, 2006
)
0.33
"These studies provide critical insights regarding Ad5-delta24-RGD dosing and anticipated toxicity for a planned clinical trial for ovarian cancer."( Identifying the safety profile of a novel infectivity-enhanced conditionally replicative adenovirus, Ad5-delta24-RGD, in anticipation of a phase I trial for recurrent ovarian cancer.
Alvarez, RD; Aurigemma, R; Broadt, T; Curiel, DT; Harris, R; Makhija, S; Noker, PE; Page, JG; Polley-Nelson, J; Schweikart, K; Tian, B; Tomaszewski, J; Wang, M, 2007
)
0.34
" Brain targeted delivery was achieved and a reduction in dosage might be allowed."( Body distributioin of RGD-mediated liposome in brain-targeting drug delivery.
Chen, B; Chen, D; Hu, H; Qiao, M; Qin, J; Zhao, X, 2007
)
0.34
" In an ovariectomized mouse osteoporotic model, at an oral dosage of 110."( Synthesis, evaluation and 3D QSAR analysis of novel estradiol-RGD octapeptide conjugates with oral anti-osteoporosis activity.
Liu, J; Peng, S; Zhang, X; Zhao, M, 2009
)
0.35
" RDF migration on and within collagen was increased with RDG-grafted collagen and decreased with RGD-grafted collagen, and dose-response experiments indicated a biphasic response of RDF migration to adhesion."( Positively and negatively modulating cell adhesion to type I collagen via peptide grafting.
Fernandes, AV; Monteiro, GA; Shreiber, DI; Sundararaghavan, HG, 2011
)
0.37
" Repetitive dosing in a cohort of 14 dogs, at the defined optimal dose, was well tolerated and led to objective tumor regression in two dogs (14%), stable disease in six (43%), and disease progression in six (43%) via Response Evaluation Criteria in Solid Tumors (RECIST)."( Launching a novel preclinical infrastructure: comparative oncology trials consortium directed therapeutic targeting of TNFalpha to cancer vasculature.
Arap, W; Hajitou, A; Hanna, E; Henry, C; Kachala, S; Khanna, C; Leblanc, A; Libutti, SK; Mazcko, C; Newman, S; Paoloni, MC; Pasqualini, R; Sorenmo, K; Tandle, A; Thamm, D; Vail, D, 2009
)
0.35
" Because endostatin has relatively shorter serum half-life, frequent dosing was required for inhibiting tumor growth."( Inhibition of ovarian cancer by RGD-P125A-endostatin-Fc fusion proteins.
Jing, Y; Lu, H; Ramakrishnan, S; Subramanian, IV; Wu, K, 2011
)
0.37
" In due course, the strategy embodied in conjugate 1 could allow for more precise monitoring of dosage levels, as well as an improved understanding of cellular uptake and release mechanisms."( Direct fluorescence monitoring of the delivery and cellular uptake of a cancer-targeted RGD peptide-appended naphthalimide theragnostic prodrug.
Bhuniya, S; Han, JH; Kang, C; Kim, JS; Kim, JY; Lee, MH; Sessler, JL, 2012
)
0.38
"To mimic the clinic dosing pattern, initially administering high loading dose and then low maintenance dose, we designed a novel poly(2-(pyridin-2-yldisulfanyl)ethyl acrylate) (PDS) based nanoparticle delivery system."( pH and redox dual responsive nanoparticle for nuclear targeted drug delivery.
K C, RB; Thapa, B; Xu, P, 2012
)
0.38
" In tumor-targeting experiments against the IGROV-1/Pt1 human ovarian carcinoma xenotransplanted in nude mice, compound 11 exhibited a superior activity compared with paclitaxel, despite the lower (about half) molar dosage used."( Synthesis and biological evaluation (in vitro and in vivo) of cyclic arginine-glycine-aspartate (RGD) peptidomimetic-paclitaxel conjugates targeting integrin αVβ3.
Arosio, D; Belvisi, L; Carenini, N; Castiglioni, V; Colombo, R; De Cesare, M; Gennari, C; Mingozzi, M; Perego, P; Piarulli, U; Scanziani, E; Zaffaroni, N, 2012
)
0.38
"The pharmacokinetic profiles of intravitreal administration HM-3 provide the basis for the development of reasonable dosing regimens of clinical choroidal neovascularization (CNV) treatment."( Pharmacokinetics of HM-3 after intravitreal administration in mice.
Hu, J; Li, W; Liu, Q; Liu, X; Shen, H; Xia, X; Xie, P; Xu, H; Yuan, D; Yuan, S, 2014
)
0.4
" Finally, no significant cytotoxicity of the blood system or major organs of the drug-loaded liposomes was observed under treatment dosage in the safety evaluation."( Multifunctional Tandem Peptide Modified Paclitaxel-Loaded Liposomes for the Treatment of Vasculogenic Mimicry and Cancer Stem Cells in Malignant Glioma.
Gao, H; He, Q; Liu, Y; Mei, L; Qiu, Y; Shi, K; Xu, C; Yang, Y; Yu, Q; Zhang, Q; Zhang, Z, 2015
)
0.42
"879) with the dosage within a certain range."( Inhibitory Effects of PEI-RGD/125I-(αv) ASODN on Growth and Invasion of HepG2 Cells.
Cai, H; Luo, Q; Lv, Z; Qiao, Y; Sun, M; Yang, Y; Yuan, S; Yuan, X, 2015
)
0.42
" The substrate coupling strength of the RGD peptides, which is dependent on the electrostatic interactions between the APTES-treated glass substrate and the cit-AuNPs, is simply tuned by changing the APTES dosage and, hence, the resultant positive charge density on the surface."( Substrate Coupling Strength of Integrin-Binding Ligands Modulates Adhesion, Spreading, and Differentiation of Human Mesenchymal Stem Cells.
Bian, L; Choi, CK; Wang, B; Xu, YJ; Zhang, L; Zhu, M, 2015
)
0.42
" Because of the enhanced biocompatibility resulting from the glycine modification, over 80% of the cells survived, even though the dosage of glycine-modified polymeric nanobubbles was up to 5 mg/mL."( Targeted Soft Biodegradable Glycine/PEG/RGD-Modified Poly(methacrylic acid) Nanobubbles as Intelligent Theranostic Vehicles for Drug Delivery.
Guo, J; Li, Y; Wan, J; Wang, C; Zhang, Z, 2017
)
0.46
" We then demonstrate the feasibility of analyzing the response of hMSCs to a stable concentration gradient of soluble factors such as inflammatory stimuli for potential future use in potency analyses, minimizing the amount of sample required for dose-response testing."( Enabling mesenchymal stromal cell immunomodulatory analysis using scalable platforms.
García, AJ; García, JR; Lam, WA; Mannino, RG; Schneider, RS; Williams, EK, 2019
)
0.51
[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 (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
DNA polymerase kappa isoform 1Homo sapiens (human)Potency18.88760.031622.3146100.0000AID588579
[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)168.85710.00010.632310.0000AID1159172; AID1159175; AID217306; AID220467; AID32990; AID91595; AID92813
Integrin beta-1Homo sapiens (human)IC50 (µMol)830.00000.00010.72528.0000AID1159174
Integrin alpha-V Homo sapiens (human)IC50 (µMol)17.50000.00010.625610.0000AID1159172; AID1159173; AID217306; AID220467
Integrin alpha-IIbHomo sapiens (human)IC50 (µMol)287.50000.00010.730910.0000AID1159175; AID32990; AID91595; AID92813
Integrin alpha-5Homo sapiens (human)IC50 (µMol)830.00000.00011.40828.0000AID1159174
Integrin beta-5Homo sapiens (human)IC50 (µMol)38.00000.00010.33725.4000AID1159173
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (147)

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)
[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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (70)

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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (13)

Assay IDTitleYearJournalArticle
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.
AID91595Inhibition of integrin alphaIIb-beta3 binding2001Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19
Determination of the binding specificity of an integral membrane protein by saturation transfer difference NMR: RGD peptide ligands binding to integrin alphaIIbbeta3.
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.
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.
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.
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.
AID217306Inhibition of binding to human Vitronectin receptor (integrin alphaV-beta3)2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Molecular model of the alpha(IIb)beta(3) integrin.
AID220467Displacement of a non-peptide radioligand from human recombinant alphaV-beta3 integrin2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Nonpeptide alpha(v)beta(3) antagonists. Part 2: constrained glycyl amides derived from the RGD tripeptide.
AID1174048Antiplatelet activity in citrated human platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation incubated for 10 mins at 37 degC by light transmission aggregometry2014Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
'Click' glycosylation of peptides through cysteine propargylation and CuAAC.
AID32990Inhibition of human alphaIIb-beta3 integrin in platelet aggregation assay2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Molecular model of the alpha(IIb)beta(3) integrin.
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.
AID92813Inhibition of rate of ADP-stimulated gel-filtered human platelet aggregation mediated by integrin alphaIIb beta-3 in PLAGGIN assay2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Nonpeptide alpha(v)beta(3) antagonists. Part 2: constrained glycyl amides derived from the RGD tripeptide.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (4,410)

TimeframeStudies, This Drug (%)All Drugs %
pre-199051 (1.16)18.7374
1990's964 (21.86)18.2507
2000's1429 (32.40)29.6817
2010's1742 (39.50)24.3611
2020's224 (5.08)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.77

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.77 (24.57)
Research Supply Index8.43 (2.92)
Research Growth Index6.01 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (12.77)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials17 (0.37%)5.53%
Reviews224 (4.92%)6.00%
Case Studies10 (0.22%)4.05%
Observational0 (0.00%)0.25%
Other4,305 (94.49%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (4)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
The Use of Adhesion Molecule Loaded Hydrogel With Minimally Invasive Surgical Technique in Treatment of Periodontal Intrabony Defect (Randomized Clinical and Biochemical Study) [NCT05653245]Phase 1/Phase 245 participants (Actual)Interventional2021-03-15Completed
Phase I Open Label Trial of Pharmacokinetics and Safety of 99mTc Niacinamide Polyethylene Glycol Bicyclic RGD Peptide (99mTc-3PRGD2) Injection in Healthy Volunteers [NCT03974685]Phase 110 participants (Actual)Interventional2018-12-12Completed
An Evaluation of the Efficacy and Safety of Technetium [99mTc] Hydrazinonicotinamide PEGylated Bicyclic RGD Peptide Injection in a Multicenter, Open, Self-controlled Clinical Trial for the Lymph Node Metastasis in Lung Tumors [NCT04233476]Phase 3409 participants (Actual)Interventional2019-10-12Completed
Targeted PET/CT and PET/MRI Imaging of Vascular Inflammation [NCT02995642]Phase 20 participants (Actual)Interventional2019-10-31Withdrawn(stopped due to Resources not secured)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]