Synthesis and evaluation of coumarin derivatives as potential dual-action HIV-1 protease and reverse transcriptase inhibitors
Baylis–Hillman-derived 3-(benzylaminomethyl) coumarins have been treated, sequentially,
with chloroacetyl chloride and propargylamine to afford alkynylated coumarins as substrates …
with chloroacetyl chloride and propargylamine to afford alkynylated coumarins as substrates …
Virological failure in patients with HIV-1 subtype C receiving antiretroviral therapy: an analysis of a prospective national cohort in Sweden
A Häggblom, V Svedhem, K Singh, A Sönnerborg… - The lancet HIV, 2016 - thelancet.com
Background People with HIV-1 in low-income and middle-income countries increasingly
need second-line regimens with boosted protease inhibitors. However, data are scarce for …
need second-line regimens with boosted protease inhibitors. However, data are scarce for …
Non-B HIV-1 subtypes in sub-Saharan Africa: impact of subtype on protease inhibitor efficacy
Abstract In 2012, 25 million people [71% of global human immunodeficiency virus (HIV)
infection] were estimated to be living with HIV in sub-Saharan Africa. Of these, approximately …
infection] were estimated to be living with HIV in sub-Saharan Africa. Of these, approximately …
HIV protease hinge region insertions at codon 38 affect enzyme kinetics, conformational stability and dynamics
HIV-1 protease is essential for the production of mature, infectious virions and is a major
target in antiretroviral therapy. We successfully purified a HIV-1 subtype C variant, L38↑ …
target in antiretroviral therapy. We successfully purified a HIV-1 subtype C variant, L38↑ …
Structural insights into the South African HIV-1 subtype C protease: impact of hinge region dynamics and flap flexibility in drug resistance
The HIV protease plays a major role in the life cycle of the virus and has long been a target
in antiviral therapy. Resistance of HIV protease to protease inhibitors (PIs) is problematic for …
in antiviral therapy. Resistance of HIV protease to protease inhibitors (PIs) is problematic for …
Understanding drug resistance of wild-type and L38HL insertion mutant of HIV-1 C protease to saquinavir
S Venkatachalam, N Murlidharan, SR Krishnan… - Genes, 2023 - mdpi.com
Acquired immunodeficiency syndrome (AIDS) is one of the most challenging infectious
diseases to treat on a global scale. Understanding the mechanisms underlying the …
diseases to treat on a global scale. Understanding the mechanisms underlying the …
Binding free energy calculations of nine FDA‐approved protease inhibitors against HIV‐1 subtype C I36T↑ T containing 100 amino acids per monomer
HA Lockhat, JRA Silva, CN Alves… - Chemical biology & …, 2016 - Wiley Online Library
In this work, have investigated the binding affinities of nine FDA‐approved protease inhibitor
drugs against a new HIV‐1 subtype C mutated protease, I36T↑ T. Without an X‐ray crystal …
drugs against a new HIV‐1 subtype C mutated protease, I36T↑ T. Without an X‐ray crystal …
Comparison of the molecular dynamics and calculated binding free energies for nine FDA‐approved HIV‐1 PR drugs against subtype B and C‐SA HIV PR
SM Ahmed, HG Kruger, T Govender… - Chemical biology & …, 2013 - Wiley Online Library
We report the first account of a comparative analysis of the binding affinities of nine FDA‐
approved drugs against subtype B as well as the South African subtype C HIV PR (C‐SA). A …
approved drugs against subtype B as well as the South African subtype C HIV PR (C‐SA). A …
Non-active site mutations in the HIV protease: Diminished drug binding affinity is achieved through modulating the hydrophobic sliding mechanism
The global HIV/AIDS epidemic still currently affects approximately 38 million individuals
globally. The protease enzyme of the human immunodeficiency virus is a major drug target …
globally. The protease enzyme of the human immunodeficiency virus is a major drug target …
Synthesis and structural studies of pentacycloundecane-based HIV-1 PR inhibitors: A hybrid 2D NMR and docking/QM/MM/MD approach
MM Makatini, K Petzold, SN Sriharsha, N Ndlovu… - European journal of …, 2011 - Elsevier
Pentacycloundecane (PCU) lactam-peptide based HIV protease inhibitors were synthesized
and nanomolar activity against the resistance-prone wild type C-South African HIV protease …
and nanomolar activity against the resistance-prone wild type C-South African HIV protease …