Proposal of pharmacophore model for HIV reverse transcriptase inhibitors: Combined mutational effect analysis, molecular dynamics, molecular docking and …

A Annan, N Raiss, S Lemrabet… - International …, 2024 - journals.sagepub.com
Objectives: Antiretroviral therapy (ART) efficacy is jeopardized by the emergence of drug
resistance mutations in HIV, compromising treatment effectiveness. This study aims to …

Genetic diversity and antiretroviral resistance-associated mutation profile of treated and naive HIV-1 infected patients from the Northwest and Southwest regions of …

HD Meriki, KA Tufon, DN Anong, PN Atanga… - PLoS …, 2019 - journals.plos.org
Background Antiretroviral therapy (ART) has improved the survival of HIV infected persons.
However, rapid scale-up of ART and the high HIV-1 genetic variability, has greatly …

Preclinical characterization of a non-peptidomimetic HIV protease inhibitor with improved metabolic stability

A Mulato, E Lansdon, R Aoyama, J Voigt… - Antimicrobial Agents …, 2024 - Am Soc Microbiol
Protease inhibitors (PIs) remain an important component of antiretroviral therapy for the
treatment of HIV-1 infection due to their high genetic barrier to resistance development …

Halogen bond interactions of novel HIV-1 protease inhibitors (PI)(GRL-001-15 and GRL-003-15) with the flap of protease are critical for their potent activity against …

S Hattori, H Hayashi, H Bulut, KV Rao… - Antimicrobial Agents …, 2019 - Am Soc Microbiol
We generated two novel nonpeptidic HIV-1 protease inhibitors (PIs), GRL-001-15 and GRL-
003-15, which contain unique crown-like tetrahydropyranofuran (Crn-THF) and P2 …

Premature Activation of the HIV-1 Protease Is Influenced by Polymorphisms in the Hinge Region

CO Tabler, SJ Wegman, N Alhusaini, NF Lee, JC Tilton - Viruses, 2024 - mdpi.com
HIV-1 protease inhibitors are an essential component of antiretroviral therapy. However,
drug resistance is a pervasive issue motivating a persistent search for novel therapies …

Natural Polymorphisms D60E and I62V Stabilize a Closed Conformation in HIV-1 Protease in the Absence of an Inhibitor or Substrate

TT Tran, GE Fanucci - Viruses, 2024 - mdpi.com
HIV infection remains a global health issue plagued by drug resistance and virological
failure. Natural polymorphisms (NPs) contained within several African and Brazilian …

Potential immune escape mutations under inferred selection pressure in HIV-1 strains circulating in Medellín, Colombia

D Arcia, R Ochoa, JC Hernández, CM Álvarez… - Infection, Genetics and …, 2019 - Elsevier
The introduction of highly active antiretroviral therapy (HAART) has significantly improved
life expectancy of HIV-infected patients; nevertheless, it does not eliminate the virus from …

Potential Associations of Mutations within the HIV-1 Env and Gag Genes Conferring Protease Inhibitor (PI) Drug Resistance

NF Maphumulo, ML Gordon - Microbiology Research, 2021 - mdpi.com
An increasing number of patients in Africa are experiencing virological failure on a second-
line antiretroviral protease inhibitor (PI)-containing regimen, even without resistance …

Impact of antiretroviral resistance and virological failure on HIV-1 informational entropy

ENC Lima, JRC Piqueira, M Camargo… - Journal of …, 2018 - academic.oup.com
Objectives The present study investigated the relationship between genomic variability and
resistance of HIV-1 sequences in protease (PR) and reverse transcriptase (RT) regions of …

HIV drug resistance in antiretroviral-naive patients in Mexico after 10 years: is there a difference?

M Escoto-Delgadillo, BM Torres-Mendoza… - AIDS research and …, 2016 - liebertpub.com
The aim of this study was to compare the extent of resistance to antiretroviral (ARV) drugs
among the population in Mexico before and after 2005. The mutations and drug resistance …