| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T29879 | ||||
| Target Name | Integrin alpha-5 (ITGA5) | ||||
| Type of Target |
Clinical trial |
||||
| Drug Potency against Target | JSM 6427 | Drug Info | IC50 = 0.55 nM | [2] | |
| C(-GRGDfL-) | Drug Info | IC50 = 740 nM | [1] | ||
| Action against Disease Model | JSM 6427 | Drug Info | 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) on days 3 and 7 after detachment and inhibition of inflammatory response and retinal scarring on day 7 after detachmen | [3] | |
| References | |||||
| REF 1 | Multiple N-methylation by a designed approach enhances receptor selectivity. J Med Chem. 2007 Nov 29;50(24):5878-81. | ||||
| REF 2 | Inhibition of inflammatory lymphangiogenesis by integrin alpha5 blockade. Am J Pathol. 2007 Jul;171(1):361-72. | ||||
| REF 3 | 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. | ||||
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