Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T67363 Target Info
Target Name Integrin alpha-V/beta-3 (ITGAV/B3)
Synonyms
Integrin alphaVbeta3; Integrin alpha-v beta-3; Integrin alpha V beta 3; Alpha(v)beta(3) Integrin; Alpha v beta 3 integrin
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Target Type Clinical trial Target
Gene Name ITGAV-ITGB3
Biochemical Class Integrin
UniProt ID
ITAV_HUMAN - ITB3_HUMAN
Co-Targets of This Target  Top
Co-Target Name Glycoprotein IIb/IIIa receptor (GPIIb/IIIa) Successful Target
UniProt ID ITA2B_HUMAN-ITB3_HUMAN
Gene Name ITGA2B; ITGB3
Synonyms
Platelet membrane glycoprotein IIb; Platelet membrane glycoprotein IIIa; GP
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Representative Drug(s) Cilengitide Drug Info IC50 = 590 nM [1]
Co-Target Name Integrin alpha-5/beta-1 (ITGA5/B1) Clinical trial Target
UniProt ID ITA5_HUMAN-ITB1_HUMAN
Gene Name ITGA5-ITGB1
Synonyms
alpha(5)beta(1) integrin; Alpha 5 beta 1 integrin
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Representative Drug(s) Cilengitide Drug Info IC50 = 13.2 nM [2]
Co-Target Name Integrin alpha-V/beta-6 (ITGAV/B6) Clinical trial Target
UniProt ID ITAV_HUMAN-ITB6_HUMAN
Gene Name ITGAV-ITGB6
Synonyms
alpha(V)beta(6) integrin; Alpha V beta 6 integrin
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Representative Drug(s) Cilengitide Drug Info IC50 = 470 nM [1]
Co-Target Name Integrin alpha-V/beta-5 (ITGAV/B5) Discontinued Target
UniProt ID ITAV_HUMAN-ITB5_HUMAN
Gene Name ITGAV-ITGB5
Synonyms
Integrin; Vitronectin receptor
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Representative Drug(s) Cilengitide Drug Info IC50 = 0.13 nM [3]
Co-Target Name Integrin alpha-V/alpha-5 (ITGAV/ITGA5) Co-Target
UniProt ID ITAV_HUMAN-ITA5_HUMAN
Gene Name ITGAV-ITGA5
Representative Drug(s) Cilengitide Drug Info IC50 = 0.13 nM [4]
References  Top
REF 1 Nanomolar small molecule inhibitors for alphav(beta)6, alphav(beta)5, and alphav(beta)3 integrins. J Med Chem. 2002 Feb 28;45(5):1045-51.
REF 2 Strategies to inhibit tumor associated integrin receptors: rationale for dual and multi-antagonists. J Med Chem. 2014 Aug 14;57(15):6301-15.
REF 3 Discovery of subnanomolar arginine-glycine-aspartate-based alphaVbeta3/alphaVbeta5 integrin binders embedding 4-aminoproline residues. J Med Chem. 2008 Mar 27;51(6):1771-82.
REF 4 Morpholine-based RGD-cyclopentapeptides as alphavbeta3/alphavbeta5 integrin ligands: role of configuration towards receptor binding affinity. Bioorg Med Chem. 2009 Feb 15;17(4):1542-9.

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