| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T01851 | ||||
| Target Name | Integrin beta-1 | ||||
| Target Type | Clinical Trial |
||||
| Drug Potency against Target | C(-GRGDfL-) | Drug Info | IC50 = 740 nM | [529125] | |
| SB-265123 | Drug Info | Ki = 18000 nM | [525536] | ||
| JSM 6427 | Drug Info | IC50 = 0.55 nM | [552709] | ||
| MK-0668 | Drug Info | IC50 = 0.15 nM | [530343] | ||
| TR-14035 | Drug Info | IC50 = 414 nM | [528475] | ||
| R411 | Drug Info | IC50 = 12 nM | |||
| Action against Disease Model | JSM 6427 | JSM6427 provided a dose-dependent blockade of ARPE-19 cell adhesion to fibronectin (IC(50), 7.1 +/- 2.5 microM) and inhibition of migration (IC(50), 6.0 +/- 4.5 microM). In the rabbit model, intravitreal injection of JSM6427 provided significant inhibition of proliferation of retinal cells (M?1ller cells, microglia, and macrophages) | [552988] | Drug Info | |
| The Effect of Target Knockout, Knockdown or Genetic Variations | Itga1-/- normal vascular development; reduced adult angiogenesis | [529125] | |||
| References | |||||
| Ref 529125 | J Med Chem. 2007 Nov 29;50(24):5878-81. Epub 2007 Nov 1.Multiple N-methylation by a designed approach enhances receptor selectivity. | ||||
| Ref 525536 | Bioorg Med Chem Lett. 1999 Jul 5;9(13):1807-12.Orally bioavailable nonpeptide vitronectin receptor antagonists with efficacy in an osteoporosis model. | ||||
| Ref 552988 | Assessment of the integrin alpha5beta1 antagonist JSM6427 in proliferative vitreoretinopathy using in vitro assays and a rabbit model of retinal detachment. Invest Ophthalmol Vis Sci. 2010 Feb;51(2):1028-35. doi: 10.1167/iovs.09-3575. Epub 2009 Oct 8. | ||||
| Ref 552709 | Inhibition of inflammatory lymphangiogenesis by integrin alpha5 blockade. Am J Pathol. 2007 Jul;171(1):361-72. | ||||
| Ref 530343 | Bioorg Med Chem Lett. 2009 Oct 1;19(19):5803-6. Epub 2009 Jul 28.Discovery of N-{N-[(3-cyanobenzene) sulfonyl]-4(R)-(3,3-difluoropiperidin-1-yl)-(l)-prolyl}-4-[(3',5'-dichloro-isonicotinoyl) amino]-(l)-phenylalanine (MK-0617), a highly potent and orally active VLA-4 antagonist. | ||||
| Ref 528475 | Bioorg Med Chem Lett. 2007 Jan 1;17(1):142-6. Epub 2006 Oct 10.2,6-Quinolinyl derivatives as potent VLA-4 antagonists. | ||||
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