Article ID Journal Published Year Pages File Type
10757956 Biochemical and Biophysical Research Communications 2013 6 Pages PDF
Abstract

- Inhibitors against MDR HIV-1 protease were designed, synthesized and evaluated.
- Lead peptide (6a) showed potent inhibition (IC50: 4.4 nM) of MDR HIV-1 protease.
- (6a) Showed favorable binding isotherms against NL4-3 and MDR proteases.
- (6a) Induced perturbations in the 15N-HSQC spectrum of MDR HIV-1 protease.
- Molecular modeling suggested that (6a) may induce total flap closure inMDR protease.
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Life Sciences Biochemistry, Genetics and Molecular Biology Biochemistry
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