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[Resistance to integrase inhibitors].

Enfermedades infecciosas y microbiologia clinica, 2009
Integrase inhibitors are the most recently approved family of antiretroviral agents for the treatment of HIV infection. As with other antiretroviral agents, under pharmacological pressure, the virus selects resistance mutations if viral suppression is incomplete.
Carolina, Garrido   +2 more
openaire   +2 more sources

The clinical pharmacology of integrase inhibitors

Expert Review of Clinical Pharmacology, 2018
Introduction: Treatment of HIV infection has consistently evolved in the last three decades. A steady improvement in efficacy tolerability, safety, and practical aspects of treatment intake has made HIV infection much easier to manage over the long term, and in optimal treatment conditions the life expectancy of persons living with HIV infection now ...
Di Perri, Giovanni   +3 more
openaire   +2 more sources

Coumarin-Based Inhibitors of HIV Integrase

Journal of Medicinal Chemistry, 1997
The 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.
H, Zhao   +8 more
openaire   +2 more sources

HIV INTEGRASE INHIBITORS

2022
HIV infection is incredibly detrimental and fatal to people. Unfortunately, despite recent advancements and medications, it has not yet been completely eradicated. Opportunistic infections are added to the list of disorders in AIDS (Acquired Immune Deficiency Syndrome), an infectious disease that develops as a result of an impaired immune system.
openaire   +1 more source

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.   +12 more
openaire   +4 more sources

Next-Generation Integrase Inhibitors

Drugs, 2013
The integrase enzyme facilitates the incorporation of HIV-1 proviral DNA into the host cell genome and catalyses a function vital to viral replication. Inhibitors of this enzyme represent the newest class of antiretroviral drugs in our armamentarium to treat HIV-1 infection.
Sharon L, Karmon, Martin, Markowitz
openaire   +2 more sources

Inhibitors of Human Immunodeficiency Virus Integrase

1999
Integration of the viral DNA into a host cell chromosome is an essential step for HIV replication and maintenance of persistent infection. Two viral factors are essential for integration: the viral DNA termini (the att sites) and IN. Accruing knowledge of the IN structure, catalytic mechanisms, and interactions with other proteins can be used to design
Y, Pommier, N, Neamati
openaire   +2 more sources

Integrase Inhibitors

2015
Jill Blumenthal, Charles Hicks
openaire   +2 more sources

Integrase inhibitor gains FDA approval

American Journal of Health-System Pharmacy, 2007
Merck on October 12 announced the approval of raltegravir, an HIV integrase inhibitor, as part of a combination regimen in treatment-experienced HIV-infected adults whose virus is active and resistant to multiple antiviral agents.
openaire   +1 more source

[Integrase inhibitor, CCR5 antagonist, fusion inhibitor].

Nihon rinsho. Japanese journal of clinical medicine, 2010
Integrase inhibitors have a novel antiretroviral mechanism which prevents proviral DNA integration into the CD4+ cell chromosome. Promising results have been seen in clinical trials in treatment-naïve and -experienced infected individuals. CCR5 antagonists bind to CCR5, one of the second receptors of HIV-1, and inhibit HIV-1 entry into CD4+ cells ...
openaire   +1 more source

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