Results 211 to 220 of about 71,029 (252)
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Resistance to HIV integrase inhibitors
Current Opinion in HIV and AIDS, 2012HIV 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. The purpose of this review is to provide new information about the most recent mutations identified and other mutations that confer ...
T. Mesplède, P. Quashie, M. Wainberg
semanticscholar +7 more sources
Tolerability of HIV integrase inhibitors
Current Opinion in HIV and AIDS, 2012This 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.Phase 2 and 3 clinical trials show that all three INSTIs are well tolerated in treatment-naive and treatment-experienced patients with ...
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, 2021Purpose 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, 2010Integrase 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
ChemInform Abstract: Potential Inhibitors of HIV Integrase
ChemInform, 1999AbstractChemInform 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
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Thiazolothiazepine Inhibitors of HIV-1 Integrase
Journal of Medicinal Chemistry, 1999A 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.+12 more
openaire +5 more sources
The Hunt for HIV-1 Integrase Inhibitors
AIDS Patient Care and STDs, 2006Currently, there are three distinct mechanistic classes of antiretrovirals: inhibitors of the HIV- 1 reverse transcriptase and protease enzymes and inhibitors of HIV entry, including receptor and coreceptor binding and cell fusion. A new drug class that inhibits the HIV-1 integrase enzyme (IN) is in development and may soon be available in the clinic ...
Michael J. Kozal, Max Lataillade
openaire +2 more sources
Integrase inhibitors to treat HIV/Aids
Nature Reviews Drug Discovery, 2005HIV 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+2 more
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Raltegravir: an integrase inhibitor for HIV-1
Expert Opinion on Investigational Drugs, 2008The 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
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Coumarin-Based Inhibitors of HIV Integrase
Journal of Medicinal Chemistry, 1997The structures of a large number of HIV-1 integrase inhibitors have in common two aryl units separated by a central linker. Frequently at least one of these aryl moieties must contain 1,2-dihydroxy substituents in order to exhibit high inhibitory potency.
Terrence R. Burke+8 more
openaire +3 more sources