MK-0518 and GS-9137: two promising integrase inhibitors in the pipeline.
نویسنده
چکیده
Possibly the most exciting news to come out of the 13th Conference on Retroviruses and Opportunistic Infections, held in Denver last February, concerned clinical trials of two experimental drugs in a new class: integrase inhibitors. If successful in further trials, integrase inhibitors could revitalize the treatment regimens of people living with multidrug-resistant HIV.
منابع مشابه
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
To gain further insight into the understanding of the antiviral resistance patterns and mechanisms of the integrase strand transfer inhibitor L-870,810, the prototypical naphthyridine analogue, we passaged the human immunodeficiency virus type 1 strain HIV-1(III(B)) in cell culture in the presence of increasing concentrations of L-870,810 (III(B)/L-870,810). The mutations L74M, E92Q, and S230N ...
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Human HIV integrase inhibitors are a novel class of antiretroviral drugs that act by blocking incorporation of the proviral DNA into the host cell genome, a crucial step in the life cycle of HIV. In the present work, quantitative methods for prediction of human pharmacokinetics were used to guide the selection of development candidates from a series of dihydroxypyrimidine and N-methylpyrimidino...
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Integrase is actively studied as an antiviral target, but many inhibitors selected from biochemical screens fail to inhibit human immunodeficiency virus (HIV) replication or primarily affect off-site targets. Here we develop and validate a replication-competent, simian virus 40-HIV integrase mutant chimera as a novel tool to classify the mechanism of action of potential integrase inhibitors. Wh...
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عنوان ژورنال:
- BETA : bulletin of experimental treatments for AIDS : a publication of the San Francisco AIDS Foundation
دوره 18 4 شماره
صفحات -
تاریخ انتشار 2006