Synthesis and SAR of 2-arylbenzoxazoles, benzothiazoles and benzimidazoles as inhibitors of lysophosphatidic acid acyltransferase-β

B Gong, F Hong, C Kohm, L Bonham, P Klein

Index: Gong, Baoqing; Hong, Feng; Kohm, Cory; Bonham, Lynn; Klein, Peter Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 6 p. 1455 - 1459

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Citation Number: 84

Abstract

LPAAT is an integral membrane protein that catalyzes the biosynthesis of phosphatidic acid (PA) from lysoPA (LPA). PA has been implicated in cell signaling events including Ras-associated factor (Raf) translocation to membranes, mammalian target of rapamycin (mTOR) activation, epidermal growth factor receptor (EGFR) internalization, and activation of protein kinase C-ζ (PKCζ). 1, 2, 3 and 4 LPAAT-α was shown to be uniformly expressed in all human tissues ...