Results 231 to 240 of about 71,892 (273)

Quinoline-based HIV integrase inhibitors.

Current Pharmaceutical Design, 2013
HIV integrase became an important target for drug development more than twenty years ago. However, progress has been hampered by the lack of assays suitable for high throughput screening, a reliable crystal structure or pharmacophore.
R. Musioł
semanticscholar   +3 more sources

Resistance to HIV integrase inhibitors

Current Opinion in HIV and AIDS, 2012
Purpose of reviewHIV integrase inhibitors are potent antiretroviral drugs that efficiently decrease viral load in patients. Emergence of resistance mutations against this new class of drugs represents a threat to their long-term efficacy.
T. Mesplède, P. Quashie, M. Wainberg
semanticscholar   +7 more sources

Tolerability of HIV integrase inhibitors

Current Opinion in HIV and AIDS, 2012
Purpose of reviewThis review discusses the available safety data for three integrase strand transfer inhibitors (INSTIs) – raltegravir, elvitegravir and dolutegravir – derived from studies in both HIV-infected and HIV-uninfected cohorts.
F. Lee, A. Carr
semanticscholar   +3 more sources

Impact of Integrase inhibitors and tenofovir alafenamide on weight gain in people with HIV

Current Opinion in HIV and AIDS, 2021
Purpose of review Obesity is increasing in people with HIV (PWH). This review aims to summarise the recent evidence investigating the associations between the use of integrase inhibitors and tenofovir alafenamide (TAF) with weight gain and the mechanisms
J. Lake, J. Trevillyan
semanticscholar   +1 more source

Novel integrase inhibitors for HIV

Expert Opinion on Investigational Drugs, 2010
Integrase inhibitors are the newest class of antiretroviral agents developed to treat HIV-1 infection. Raltegravir (RAL), the only integrase inhibitor (INI) currently approved for the treatment of HIV-infected patients, has proven to be a potent and well-tolerated antiretroviral (ARV) agent.
Martin Markowitz, Nicole Prada
openaire   +3 more sources

Investigational HIV integrase inhibitors in phase I and phase II clinical trials

Expert Opinion on Investigational Drugs, 2017
Introduction: To date, three HIV integrase strand transfer inhibitors (INSTIs), i.e. raltegravir, elvitegravir and dolutegravir, have been approved for clinical use.
Yingshan Han, T. Mesplède, M. Wainberg
semanticscholar   +1 more source

ChemInform Abstract: Potential Inhibitors of HIV Integrase

ChemInform, 1999
AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Vasu Nair, Christophe Mathe
openaire   +3 more sources

Thiazolothiazepine Inhibitors of HIV-1 Integrase

Journal of Medicinal Chemistry, 1999
A series of thiazolothiazepines were prepared and tested against purified human immunodeficiency virus type-1 integrase (HIV-1 IN) and viral replication. Structure-activity studies reveal that the compounds possessing the pentatomic moiety SC(O)CNC(O) with two carbonyl groups are in general more potent against purified IN than those containing only one
NEAMATI N., TURPIN J. A, WINSLOW H. E., CHRISTENSEN J. L., WILLIAMSON K., ORR A., RICE W. G., POMMIER Y., GAROFALO A., BRIZZI A., CAMPIANI G., FIORINI I., NACCI V.   +12 more
openaire   +5 more sources

Integrase inhibitors to treat HIV/Aids

Nature Reviews Drug Discovery, 2005
HIV integrase is a rational target for treating HIV infection and preventing AIDS. It took approximately 12 years to develop clinically usable inhibitors of integrase, and Phase I clinical trials of integrase inhibitors have just begun. This review focuses on the molecular basis and rationale for developing integrase inhibitors.
Allison A. Johnson, Yves Pommier, Christophe Marchand   +2 more
openaire   +3 more sources

Raltegravir: an integrase inhibitor for HIV-1

Expert Opinion on Investigational Drugs, 2008
The need to develop antiretroviral agents with novel mechanisms of action persists for the treatment of both antiretroviral- experienced and antiretroviral-naive patients with HIV/AIDS. This is mandated, in part, by the perpetual advent of antiretroviral-resistant HIV-1 strains.
Martin Markowitz, Teresa H. Evering
openaire   +3 more sources