Kinetic and thermodynamic characterisation of HIV-protease inhibitors against E35D↑G↑S mutant in the South African HIV-1 subtype C protease

Autor:	Sibusiso Maseko, Eden Padayachee, Siyabonga Maphumulo, Thavendran Govender, Yasien Sayed, Glenn Maguire, Johnson Lin, Tricia Naicker, Sooraj Baijnath, Kruger Hendrik Gerhardus
Jazyk:	angličtina
Rok vydání:	2019
Předmět:	protease hiv mutant inhibitor thermodynamics Therapeutics. Pharmacology RM1-950
Zdroj:	Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 34, Iss 1, Pp 1451-1456 (2019)
Druh dokumentu:	article
ISSN:	1475-6366 1475-6374 14756366
DOI:	10.1080/14756366.2019.1636234
Popis:	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 (p
Databáze:	Directory of Open Access Journals
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