Article
Effect of flap mutations on structure of HIV-1 protease and inhibition by saquinavir and darunavir.
Journal of molecular biology - 1 Aug 2008
Liu Fengling, Kovalevsky Andrey Y, Tie Yunfeng, Ghosh Arun K, Harrison Robert W, Weber Irene T
Abstract excerpt
HIV-1 (human immunodeficiency virus type 1) protease (PR) and its mutants are important antiviral drug targets. The PR flap region is critical for binding substrates or inhibitors and catalytic activity. Hence, mutations of flap residues frequently contribute to reduced susceptibility to PR inhibitors in drug-resistant HIV. Structural and kinetic analyses were used to investigate the role of flap residues Gly48,...
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