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HIV protease inhibitors

AIDS, 1996
The protease encoded by the human immunodeficiency virus (HIV protease) mediates the maturation of newly formed HIV particles through proteolytic processing of the gag and gag-pol gene products. Because of its essential role in the HIV replication cycle, this enzyme represents a logical target for the treatment of HIV infection.
A, Carr, D A, Cooper
  +7 more sources

Resistance to HIV protease inhibitors

Haemophilia, 1998
Summary. Resistance to the HIV‐1 protease inhibitor indinavir involves the accumulation of multiple amino acid substitutions in the viral protease. A minimum of 11 amino acid positions have been identified as potential contributors to phenotypic resistance.
C. A. Lee   +5 more
openaire   +2 more sources

Heterocyclic HIV-Protease Inhibitors

Current Medicinal Chemistry, 2013
In the panorama of HIV protease inhibitors (HIV PIs), many efforts have been devoted to the development of new compounds with reduced peptidic nature in order to improve pharmacokinetics and pharmacodynamics features. The introduction of cyclic scaffolds in the design of new chemical entities reduces flexibility and affords more rigid inhibitors ...
CALUGI, CHIARA   +2 more
openaire   +3 more sources

Hyperlipidemia and inhibitors of HIV protease

Current Opinion in Clinical Nutrition and Metabolic Care, 2001
HIV protease inhibitors have been successfully incorporated into therapy for patients with HIV. These otherwise efficacious treatments present with multiple metabolic side-effects and body habitus changes known as the lipodystrophy syndrome. Direct associations of the lipid abnormalities with protease inhibitor use have been described, and ongoing ...
O, Distler   +3 more
openaire   +2 more sources

HIV Protease Assays

Current Protocols in Pharmacology, 1998
AbstractThe fluorescence‐based assay described in this unit is used not only to screen large numbers of compounds in a 96‐well format for the ability to inhibit human immunodeficiency virus‐1 (HIV) protease, but also to determine accurately the affinity of inhibitors for the enzyme.
openaire   +2 more sources

Prodrugs of HIV Protease Inhibitors

Current Pharmaceutical Design, 2003
Despite the efficiency of the present polytherapies against AIDS, HIV replication continues indicating difficulties in drug adherence, drug-drug interactions, resistance issues, and the existence of reservoirs or sanctuaries for the virus. Moreover, most of the current FDA-approved HIV protease inhibitors (PIs) display disadvantageous physicochemical ...
Pierre, Vierling, Jacques, Greiner
openaire   +2 more sources

HIV protease structural database

Proceedings. IEEE Computer Society Bioinformatics Conference, 2003
HIV Protease Database (HIVdb) is a repository for those structures of HIV protease that have never been released or deposited to the Protein Data Bank (PDB). Together with the official PDB data, HIVdb provided a unique source of information in a statistical sense.
Veerasamy Ravichandran   +4 more
openaire   +1 more source

HIV protease and the pathogenesis of AIDS

Research in Virology, 1996
L'aspartate protease du VIH (virus de l'immunodeficience acquise humaine) est une enzyme codee par le virus et facilitant le processus viral a la surface cellulaire. Bien que cette protease fut consideree initialement comme specifique des proteines du VIH, elle interagit egalement avec de nombreux substrats de la cellule hote.
B, Goldberg, R B, Stricker
openaire   +2 more sources

HIV protease

1995
Abstract The retroviral protease, which plays an essential role in virion maturation (1), has been subjected to intensive studies and drug discovery efforts. The HIV-1 protease has a unique cleavage specificity and belongs to the family of aspartyl proteases.
C Debouck   +3 more
openaire   +1 more source

Peptidomimetic Inhibitors of HIV Protease

Current Topics in Medicinal Chemistry, 2004
There are currently (July, 2002) six protease inhibitors approved for the treatment of HIV infection, each of which can be classified as peptidomimetic in structure. These agents, when used in combination with other antiretroviral agents, produce a sustained decrease in viral load, often to levels below the limits of quantifiable detection, and a ...
John T, Randolph, David A, DeGoey
openaire   +2 more sources

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