Synthesis and structure–activity relationships of 2-amino-3-carboxy-4-phenylthiophenes as novel atypical protein kinase C inhibitors

…, HDH Showalter, JF Pons, AJ Barber, Y Jin…

Index: Titchenell, Paul M.; Hollis Showalter; Pons, Jean-Francois; Barber, Alistair J.; Jin, Yafei; Antonetti, David A. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 10 p. 3034 - 3038

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Citation Number: 4

Abstract

Recent evidence suggests atypical protein kinase C (aPKC) isoforms are required for both TNF-and VEGF-induced breakdown of the blood–retinal barrier (BRB) and endothelial permeability to 70kDa dextran or albumin. A chemical library screen revealed a series of novel small molecule phenylthiophene based inhibitors of aPKC isoforms that effectively block permeability in cell culture and in vivo. In an effort to further elucidate the structural ...