Structural optimization of a CXCR2-directed antagonist that indirectly inhibits γ-secretase and reduces Aβ

P Bakshi, C Jin, P Broutin, B Berhane, J Reed…

Index: Bakshi, Pancham; Jin, Chao; Broutin, Pierre; Berhane, Beniam; Reed, Jon; Mullan, Michael Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 23 p. 8102 - 8112

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Citation Number: 8

Abstract

Amyloid β (Aβ), a key molecule in the pathogenesis of Alzheimer's disease (AD), is derived from the amyloid precursor protein (APP) by sequential proteolysis via β-and γ-secretases. Because of their role in generation of Aβ, these enzymes have emerged as important therapeutic targets for AD. In the case of γ-secretase, progress has been made towards designing potent inhibitors with suitable pharmacological profiles. Direct γ-secretase ...