Design, synthesis and evaluation of a potent substrate analog inhibitor identified by scanning Ala/Phe mutagenesis, mimicking substrate co-evolution, against multidrug-resistant HIV-1 protease

Multidrug-resistant (MDR) clinical isolate-769, human immunodeficiency virus type-1 (HIV-1) protease (PDB ID: 1TW7), was shown to exhibit wide-open flaps and an expanded active site cavity, causing loss of contacts with protease inhibitors. In the current study, the expanded active site cavity of MD...

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Bibliografiske detaljer
Udgivet i:Biochem Biophys Res Commun
Main Authors: Yedidi, Ravikiran S., Muhuhi, Joseck M., Liu, Zhigang, Bencze, Krisztina Z., Koupparis, Kyriacos M., O'Connor, Carrie E., Kovari, Iulia A., Spaller, Mark R., Kovari, Ladislau C.
Format: Artigo
Sprog:Inglês
Udgivet: 2013
Fag:
Article
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4288442/
https://ncbi.nlm.nih.gov/pubmed/23921229
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bbrc.2013.07.117
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