Kinetic and thermodynamic characterisation of HIV-protease inhibitors against E35D?G?S mutant in the South African HIV-1 subtype C protease.
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ABSTRACT:
SUBMITTER: Maseko S
PROVIDER: S-EPMC6713120 | biostudies-literature | 2019 Dec
REPOSITORIES: biostudies-literature
Publications
Kinetic and thermodynamic characterisation of HIV-protease inhibitors against E35D↑G↑S mutant in the South African HIV-1 subtype C protease.
Maseko Sibusiso S Padayachee Eden E Maphumulo Siyabonga S Govender Thavendran T Sayed Yasien Y Maguire Glenn G Lin Johnson J Naicker Tricia T Baijnath Sooraj S Gerhardus Kruger Hendrik KH
Journal of enzyme inhibition and medicinal chemistry 20191201 1
Herein, we report the effect of nine FDA approved protease inhibitor drugs against a new HIV-1 subtype C mutant protease, E35D↑G↑S. The mutant has five mutations, E35D, two insertions, position 36 (G and S), and D60E. Kinetics, inhibition constants, vitality, Gibbs free binding energies are reported. The variant showed a decreased affinity for substrate and low catalytic efficiency compared to the wild type. There was a significant decrease in the binding of seven FDA approved protease inhibitor ...[more]
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