Pyrone-based inhibitors of metalloproteinase types 2 and 3 may work as conformation-selective inhibitors. [PDF]
Matrix metalloproteinases are zinc-containing enzymes capable of degrading all components of the extracellular matrix. Owing to their role in human disease, matrix metalloproteinase have been the subject of extensive study.
de Oliveira, César AF+2 more
core +1 more source
Abstract Introduction Data on drug resistance, viral outcomes and guidelines compliance following protease inhibitor (PI)‐based second‐line failure in low‐ and middle‐income countries are limited, particularly in the era of dolutegravir‐containing antiretroviral therapy (ART). Methods We conducted a retrospective cohort study of people living with HIV (
John M. Humphrey+11 more
wiley +1 more source
Styrylquinoline derivatives are demonstrated to be HIV-1 integrase inhibitors. On the basis of our previous CoMFA analysis of a series of styrylquinoline derivatives, N-[(2-substituted-styryl)-5-chloro-8-hydroxyquinolin-7-yl]-benzenesulfonamide ...
Li-Ming Hu+5 more
doaj +1 more source
Abstract Introduction Black and Hispanic/Latine people are disproportionately affected by HIV‐1 and may have a greater risk of comorbidities than non‐Black and non‐Hispanic/Latine people with HIV. However, they have historically been underrepresented in HIV clinical studies.
C. Martorell+14 more
wiley +1 more source
First report of computational protein-ligand docking to evaluate susceptibility to HIV integrase inhibitors in HIV-infected Iranian patients. [PDF]
Ghasabi F+6 more
europepmc +1 more source
A rapid and convergent synthesis of the integrastatin core [PDF]
The tetracyclic core of the integrastatin natural products has been prepared in a convergent and rapidmanner. Our strategy relies upon a palladium(II)-catalyzed oxidative cyclization to form the central [3.3.1]-dioxabicycle of the natural product ...
Bugga, Pradeep+2 more
core +2 more sources
The mechanism of H171T resistance reveals the importance of Nδ-protonated His171 for the binding of allosteric inhibitor BI-D to HIV-1 integrase [PDF]
Background: Allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) are an important new class of anti-HIV-1 agents. ALLINIs bind at the IN catalytic core domain (CCD) dimer interface occupying the principal binding pocket of its cellular cofactor LEDGF/p75.
Deng, Nanjie+14 more
core +1 more source
Rethinking HIV treatment: How non‐integrase strand regimens may hold the key to better immune health
Abstract Purpose HIV outcome changed drastically with antiretroviral (ARV) therapy, especially after the introduction of second‐generation integrase strand transfer inhibitors (INSTIs). Despite these advances, however, chronic immune activation and exhaustion, marked by programmed cell death 1 (PD‐1) and programmed death ligand 1 (PD‐L1) upregulation ...
Bogusz Aksak‐Wąs+8 more
wiley +1 more source
With the widespread use of integrase inhibitors and the expanding use of long-acting cabotegravir in both pre-exposure prophylaxis and antiretroviral treatment, molecular surveillance on the transmission of integrase resistance has regained clinical ...
Kaja Mielczak+14 more
doaj +1 more source
Inhibition of Adipose Tissue Beiging by HIV Integrase Inhibitors, Dolutegravir and Bictegravir, Is Associated with Adipocyte Hypertrophy, Hypoxia, Elevated Fibrosis, and Insulin Resistance in Simian Adipose Tissue and Human Adipocytes. [PDF]
Ngono Ayissi K+16 more
europepmc +1 more source