Journal article

SB-267268, a nonpeptidic antagonist of alpha(v)beta(3) and alpha(v)beta(5) integrins, reduces angiogenesis and VEGF expression in a mouse model of retinopathy of prematurity

JL Wilkinson-Berka, D Jones, G Taylor, K Jaworski, DJ Kelly, SB Ludbrook, RN Willette, SJ Kumar, RE Gilbert

INVESTIGATIVE OPHTHALMOLOGY & VISUAL SCIENCE | ASSOC RESEARCH VISION OPHTHALMOLOGY INC | Published : 2006

Abstract

PURPOSE: To determine whether SB-267268, a nonpeptidic antagonist of the alpha(v)beta3 and alpha(v)beta5 integrins, attenuates angiogenesis in a murine model of retinopathy of prematurity (ROP) and alters the expression of vascular endothelial growth factor (VEGF) and its second receptor (VEGF-R2). METHODS: In receptor binding, SB-267268 exhibited nanomolar potency for human, monkey, and murine alpha(v)beta3 and alpha(v)beta5. SB-267268 inhibited the attachment of alpha(v)beta3-transfected HEK293 cells to microtiter plate wells precoated with RGD-containing matrix proteins, and vitronectin-mediated human and rat aortic smooth-muscle-cell migration. At postnatal day (P)12, C57BL/6 mice were e..

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