Kinetic and thermodynamic characterisation of HIV-protease inhibitors against E35D↑G↑S mutant in the South African HIV-1 subtype C protease.
HIV
Protease
inhibitor
mutant
thermodynamics
Journal
Journal of enzyme inhibition and medicinal chemistry
ISSN: 1475-6374
Titre abrégé: J Enzyme Inhib Med Chem
Pays: England
ID NLM: 101150203
Informations de publication
Date de publication:
Dec 2019
Dec 2019
Historique:
entrez:
15
8
2019
pubmed:
15
8
2019
medline:
27
8
2019
Statut:
ppublish
Résumé
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 inhibitors against the mutant (
Identifiants
pubmed: 31409143
doi: 10.1080/14756366.2019.1636234
pmc: PMC6713120
doi:
Substances chimiques
HIV Protease Inhibitors
0
HIV Protease
EC 3.4.23.-
p16 protease, Human immunodeficiency virus 1
EC 3.4.23.-
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
1451-1456Références
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