Biotinylated biphenyl ketone-containing 2, 4-dioxobutanoic acids designed as HIV-1 integrase photoaffinity ligands

…, EA Semenova, C Liao, M Nicklaus, Y Pommier…

Index: Zhao, Xue Zhi; Semenova, Elena A.; Liao, Chenzhong; Nicklaus, Marc; Pommier, Yves; Burke Jr., Terrence R. Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 23 p. 7816 - 7825

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Citation Number: 22

Abstract

The diketo acid (DKA) class of HIV-1 integrase inhibitors are thought to function by chelating divalent metal ions within the enzyme catalytic center. However, differences in mutations conferring resistance among sub-families of DKA inhibitors suggest that multiple binding orientations may exist. In order to facilitate identification of DKA-binding sites, biotin-tagged biphenyl ketone-containing 2, 4-dioxobutanoic acids were prepared as DKA photoaffinity ...