Authentic HIV-1 Integrase Inhibitors [PDF]
Future Medicinal Chemistry, 2010 HIV-1 integrase (IN) is indispensable for HIV-1 replication and has become a validated target for developing anti-AIDS agents. In two decades of development of IN inhibition-based anti-HIV therapeutics, a significant number of compounds were identified as IN inhibitors, but only some of them showed antiviral activity.
Terrence R. Burke +4 more
openaire +3 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]
, 2014 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
Biomolecules, 2020 The search for compounds that can inhibit the interaction of certain viral proteins with their cellular partners is a promising trend in the development of antiviral drugs.
Simon Galkin +4 more
doaj +1 more source
Antimicrobial Agents and Chemotherapy, 2019 We compared the activity of the integrase inhibitor bictegravir against HIV-1 and HIV-2 using a culture-based, single-cycle assay. Values of 50% effective concentrations ranged from 1.2 to 2.5 nM for 9 HIV-1 isolates and 1.4 to 5.6 nM for 15 HIV-2 ...
Robert A. Smith +7 more
semanticscholar +1 more source
Adaptive HIV-1 evolutionary trajectories are constrained by protein stability [PDF]
, 2017 Despite the use of combination antiretroviral drugs for the treatment of HIV-1 infection, the emergence of drug resistance remains a problem. Resistance may be conferred either by a single mutation or a concerted set of mutations.
Kandathil, Shaun M. +3 more
core +1 more source
Integrase-deficient lentiviral vectors mediate efficient gene transfer to human vascular smooth muscle cells with minimal genotoxic risk [PDF]
, 2012 We have previously shown that injury-induced neointima formation was rescued by adenoviral-Nogo-B gene delivery. Integrase-competent lentiviral vectors (ICLV) are efficient at gene delivery to vascular cells but present a risk of insertional mutagenesis.
Adrian J. Thrasher +11 more
core +1 more source
ING116070: a study of the pharmacokinetics and antiviral activity of dolutegravir in cerebrospinal fluid in HIV-1-infected, antiretroviral therapy-naive subjects. [PDF]
, 2014 BackgroundDolutegravir (DTG), a once-daily, human immunodeficiency virus type 1 (HIV-1) integrase inhibitor, was evaluated for distribution and antiviral activity in cerebrospinal fluid (CSF).MethodsING116070 is an ongoing, single-arm, open-label ...
Chen, Shuguang +8 more
core +3 more sources
How developing world concerns need to be part of drug development plans: A case study of four emerging antiretrovirals [PDF]
, 2008 Clinical trials are usually designed to meet registration requirements in developed countries, and do not always address key concerns for use in developing countries.
Alexandra Calmy +22 more
core +2 more sources
7‐Step Flow Synthesis of the HIV Integrase Inhibitor Dolutegravir
Angewandte Chemie, 2018 Dolutegravir (DTG), an important active pharmaceutical ingredient (API) used in combination therapy for the treatment of HIV, has been synthesized in continuous flow. By adapting the reported GlaxoSmithKline process chemistry batch route for Cabotegravir,
Robert E. Ziegler +5 more
semanticscholar +1 more source
Elvitegravir: A New HIV Integrase Inhibitor [PDF]
Antiviral Chemistry and Chemotherapy, 2009 Integration is a distinctive and essential process in the HIV infection cycle and thus represents an attractive antiviral drug target. Integrase inhibitors combined with other classes of drug might contribute to long-lasting suppression of HIV type-1 (HIV-1) replication for many patients.
Kazuya Shimura +2 more
openaire +3 more sources