Identification of 4-hydroxyquinolines inhibitors of p300/CBP histone acetyltransferases

…, D Rotili, D Tarantino, A Nebbioso, S Castellano…

Index: Mai, Antonello; Rotili, Dante; Tarantino, Domenico; Nebbioso, Angela; Castellano, Sabrina; Sbardella, Gianluca; Tini, Marc; Altucci, Lucia Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 4 p. 1132 - 1135

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Citation Number: 42

Abstract

We identified a series of 4-hydroxyquinolines bearing a C1 to C15 alkyl chain at the C2 position and a carbethoxy/carboxy group at the C3 position of the quinoline nucleus (MC compounds), endowed with selective inhibitory activity against the p300/CBP HAT enzymes. Enzyme inhibition was investigated using in vitro HAT assays and by western blot analysis of cellular lysates to examine the acetylation levels of histone H3 and α-tubulin. When ...