Discovery of a novel 5-carbonyl-1H-imidazole-4-carboxamide class of inhibitors of the HIV-1 integrase–LEDGF/p75 interaction

E Serrao, ZL Xu, B Debnath, F Christ, Z Debyser…

Index: Serrao, Erik; Xu, Zhong-Liang; Debnath, Bikash; Christ, Frauke; Debyser, Zeger; Long, Ya-Qiu; Neamati, Nouri Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 19 p. 5963 - 5972

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Citation Number: 10

Abstract

Abstract Though much progress has been made in the inhibition of HIV-1 integrase catalysis, clinical resistance mutations have limited the promise of long-term drug prescription. Consequently, allosteric inhibition of integrase activity has emerged as a promising approach to antiretroviral discovery and development. Specifically, inhibitors of the interaction between HIV-1 integrase and cellular cofactor LEDGF/p75 have been ...