Article
Modeling, analysis, and validation of a novel HIV integrase structure provide insights into the binding modes of potent integrase inhibitors.
Journal of molecular biology - 11 Jul 2008
Chen X, Tsiang M, Yu F, Hung M, Jones G S, Zeynalzadegan A, Qi X, Jin H, Kim C U, Swaminathan S, Chen J M
Abstract excerpt
It has been shown that L-731988, a potent integrase inhibitor, targets a conformation of the integrase enzyme formed when complexed to viral DNA, with the 3'-end dinucleotide already cleaved. It has also been shown that diketo acid inhibitors bind to the strand transfer complex of integrase and are competitive with the host target DNA. However, published X-ray structures of HIV integrase do not include the DNA;...
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