HIV-1 drug resistance and resistance testing

DS Clutter, MR Jordan, S Bertagnolio… - Infection, Genetics and …, 2016 - Elsevier
The global scale-up of antiretroviral (ARV) therapy (ART) has led to dramatic reductions in
HIV-1 mortality and incidence. However, HIV drug resistance (HIVDR) poses a potential …

Drug design strategies to avoid resistance in direct-acting antivirals and beyond

AN Matthew, F Leidner, GJ Lockbaum, M Henes… - Chemical …, 2021 - ACS Publications
Drug resistance is prevalent across many diseases, rendering therapies ineffective with
severe financial and health consequences. Rather than accepting resistance after the fact …

A copper (I)-catalyzed 1, 2, 3-triazole azide− alkyne click compound is a potent inhibitor of a multidrug-resistant HIV-1 protease variant

MJ Giffin, H Heaslet, A Brik, YC Lin… - Journal of medicinal …, 2008 - ACS Publications
Treatment with HIV-1 protease inhibitors, a component of highly active antiretroviral therapy
(HAART), often results in viral resistance. Structural and biochemical characterization of a …

Cellulose microfibril crystallinity is reduced by mutating C-terminal transmembrane region residues CESA1A903V and CESA3T942I of cellulose synthase

DM Harris, K Corbin, T Wang… - Proceedings of the …, 2012 - National Acad Sciences
The mechanisms underlying the biosynthesis of cellulose in plants are complex and still
poorly understood. A central question concerns the mechanism of microfibril structure and …

Molecular basis for drug resistance in HIV-1 protease

A Ali, RM Bandaranayake, Y Cai, NM King, M Kolli… - Viruses, 2010 - mdpi.com
HIV-1 protease is one of the major antiviral targets in the treatment of patients infected with
HIV-1. The nine FDA approved HIV-1 protease inhibitors were developed with extensive use …

[HTML][HTML] HIV and drug-resistant subtypes

BM Nastri, P Pagliano, C Zannella, V Folliero… - Microorganisms, 2023 - mdpi.com
Acquired Immunodeficiency Syndrome (AIDS) is a human viral infectious disease caused by
the positive-sense single-stranded (ss) RNA Human Immunodeficiency Virus …

Amprenavir complexes with HIV‐1 protease and its drug‐resistant mutants altering hydrophobic clusters

CH Shen, YF Wang, AY Kovalevsky… - The FEBS …, 2010 - Wiley Online Library
The structural and kinetic effects of amprenavir (APV), a clinical HIV protease (PR) inhibitor,
were analyzed with wild‐type enzyme and mutants with single substitutions of V32I, I50V …

Drug resistance conferred by mutations outside the active site through alterations in the dynamic and structural ensemble of HIV-1 protease

DA Ragland, EA Nalivaika, MNL Nalam… - Journal of the …, 2014 - ACS Publications
HIV-1 protease inhibitors are part of the highly active antiretroviral therapy effectively used in
the treatment of HIV infection and AIDS. Darunavir (DRV) is the most potent of these …

Improving viral protease inhibitors to counter drug resistance

NK Yilmaz, R Swanstrom, CA Schiffer - Trends in microbiology, 2016 - cell.com
Drug resistance is a major problem in health care, undermining therapy outcomes and
necessitating novel approaches to drug design. Extensive studies on resistance to viral …

Picomolar to micromolar: elucidating the role of distal mutations in HIV-1 protease in conferring drug resistance

M Henes, GJ Lockbaum, K Kosovrasti… - ACS chemical …, 2019 - ACS Publications
Drug resistance continues to be a growing global problem. The efficacy of small molecule
inhibitors is threatened by pools of genetic diversity in all systems, including antibacterials …