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
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Probing chelation motifs in HIV integrase inhibitors [PDF]
Proceedings of the National Academy of Sciences, 2012 A series of HIV integrase (HIV-1 IN) inhibitors were synthesized to evaluate the role of the metal-binding group (MBG) in this class of metalloenzyme inhibitors. A total of 21 different raltegravir-chelator derivative (RCD) compounds were prepared that differed only in the nature of the MBG.
Arpita, Agrawal +7 more
openaire +2 more sources
Integrase Inhibitor Prodrugs: Approaches to Enhancing the Anti-HIV Activity of β-Diketo Acids
Molecules, 2015 HIV integrase, encoded at the 3′-end of the HIV pol gene, is essential for HIV replication. This enzyme catalyzes the incorporation of HIV DNA into human DNA, which represents the point of “no-return” in HIV infection.
Vasu Nair, Maurice Okello
doaj +1 more source
Pyrone-based inhibitors of metalloproteinase types 2 and 3 may work as conformation-selective inhibitors. [PDF]
, 2011 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
HIV-1 integrase polymorphisms are associated with prior antiretroviral drug exposure
Retrovirology, 2009 In a recent summary of integrase sequences, primary integrase inhibitor mutations were rare. In a review of integrase inhibitor-naïve Australian HIV-1 sequences, primary mutations were not identified, although the accessory mutation G140S was detected. A
Wang Bin +5 more
doaj +1 more source
Dynein Regulators Are Important for Ecotropic Murine Leukemia Virus Infection [PDF]
, 2016 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
Resistance to inhibitors of the human immunodeficiency virus type 1 integration
Brazilian Journal of Infectious DiseasesThis review will summarize the role of integrase in HIV-1 infection, the mechanism of integrase inhibitors and resistance with an emphasis on raltegravir (RAL), the first integrase inhibitor licensed to treat HIV-1 ...
Daria J Hazuda
doaj +1 more source
Combinations of isoform-targeted histone deacetylase inhibitors and bryostatin analogues display remarkable potency to activate latent HIV without global T-cell activation [PDF]
, 2017 Current antiretroviral therapy (ART) for HIV/AIDS slows disease progression by reducing viral loads and increasing CD4 counts. Yet ART is not curative due to the persistence of CD4+ T-cell proviral reservoirs that chronically resupply active virus ...
Albert, Brice J +8 more
core +2 more sources
Integrase Strand Transfer Inhibitors in HIV Therapy [PDF]
Infectious Diseases and Therapy, 2013 HIV drug resistance has been one of the major obstacles to HIV eradication and has contributed to the need for the constant development of new antiretroviral drugs over the past 25 years. With the recent approval of dolutegravir for human therapy by the U.S.
Mesplède, Thibault, Wainberg, Mark A.
openaire +2 more sources
Screening of the NIH Clinical Collection for inhibitors of HIV-1 integrase activity
South African Journal of Science, 2018 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