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
This chapter presents the discovery, development and evolution of integrase strand transfer inhibitors. A brief overview of the first‐generation inhibitors raltegravir and elvitegravir serves to describe their landmark advancement of the field and also outline areas for further improvement.
Mathieu Métifiot +2 more
openaire +3 more sources
Screening of the NIH Clinical Collection for inhibitors of HIV-1 integrase activity
Drug repurposing offers a validated approach to reduce drug attrition within the drug discovery and development pipeline through the application of known drugs and drug candidates to treat new indications.
Shaakira Abrahams +4 more
doaj +1 more source
Protein expression from unintegrated HIV-1 DNA introduces bias in primary in vitro post-integration latency models [PDF]
To understand the persistence of latently HIV-1 infected cells in virally suppressed infected patients, a number of in vitro models of HIV latency have been developed.
Bonczkowski, Pawel +7 more
core +1 more source
CoMFA and CoMSIA Studies on Inhibitors of HIV-1 Integrase - Bicyclic Pyrimidinones
To understand the structural requirements of HIV-1 integrase inhibitors and to design new ligands against human HIV-1 integrase with enhanced inhibitory potency, a 3D QSAR (quantitative structure-activity relationship) study with comparative molecular ...
V. Radhika, S. Sree Kanth, M. Vijjulatha
doaj +1 more source
Mathematical model of a serine integrase-controlled toggle switch with a single input [PDF]
Dual-state genetic switches that can change their state in response to input signals can be used in synthetic biology to encode memory and control gene expression.
Colloms, Sean D. +3 more
core +1 more source
Effectiveness of dolutegravir-based regimens as either first-line or switch antiretroviral therapy: data from the Icona cohort [PDF]
Introduction: Concerns about dolutegravir (DTG) tolerability in the real-life setting have recently arisen. We aimed to estimate the risk of treatment discontinuation and virological failure of DTG-based regimens from a large cohort of HIV-infected ...
Abeli C. +155 more
core +4 more sources
Urinary eicosanoid metabolites in HIV-infected women with central obesity switching to raltegravir: an analysis from the women, integrase, and fat accumulation trial. [PDF]
Chronic inflammation is a hallmark of HIV infection. Eicosanoids reflect inflammation, oxidant stress, and vascular health and vary by sex and metabolic parameters. Raltegravir (RAL) is an HIV-1 integrase inhibitor that may have limited metabolic effects.
Boger, M Sean +11 more
core +3 more sources
HIV-1 resistance towards integrase inhibitors is a potential threat of the success of HIV-1 combination treatment. G118R is a rare drug resistance mutation conferring pan-integrase resistance.
Helene Mens +3 more
doaj +1 more source
Dynein Regulators Are Important for Ecotropic Murine Leukemia Virus Infection [PDF]
Indexación: Web of Science.During the early steps of infection, retroviruses must direct the movement of the viral genome into the nucleus to complete their replication cycle.
Arriagada, Gloria +4 more
core +1 more source

