Results 201 to 210 of about 118,257 (252)
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HIV Protease Inhibitor Resistance
2014HIV protease is pivotal in the viral replication cycle and directs the formation of mature infectious virus particles. The development of highly specific HIV protease inhibitors (PIs), based on thorough understanding of the structure of HIV protease and its substrate, serves as a prime example of structure-based drug design.
Wensing, Annemarie M.J. +2 more
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Enamino-oxindole HIV protease inhibitors
Bioorganic & Medicinal Chemistry Letters, 2012We have designed and synthesized a series of HIV protease inhibitors (PIs) with enamino-oxindole substituents optimized to interact with the S2' subsite of the HIV protease binding pocket. Several of these inhibitors have sub-nanomolar K(i) and antiviral IC(50) in the low nM range against WT HIV and against a panel of multi-drug resistant (MDR) strains.
Michael, Eissenstat +8 more
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Prodrugs of HIV Protease Inhibitors
Current Pharmaceutical Design, 2003Despite 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
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Peptidomimetic Inhibitors of HIV Protease
Current Topics in Medicinal Chemistry, 2004There 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
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Resistance to HIV protease inhibitors
Haemophilia, 1998Summary. 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
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Non-Peptidic HIV Protease Inhibitors
Current Topics in Medicinal Chemistry, 2004The past decade has seen many exciting achievements and advances in the treatment of HIV infection. One of the key components in this ever-evolving remedial strategy has been medicinally efficacious enzymatic inhibitors targeting the essential viral aspartyl protease.
R Alan, Chrusciel, Joseph W, Strohbach
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AIDS clinical review, 1997
Objective. —The clinical care of people infected with human immunodeficiency virus (HIV) has been substantially affected by the introduction of HIV-specific protease inhibitors (Pis). The 4 Pls available are saquinavir mesylate, ritonavir, indinavir sulfate, and nelfinavir mesylate.
S G, Deeks, P A, Volberding
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Objective. —The clinical care of people infected with human immunodeficiency virus (HIV) has been substantially affected by the introduction of HIV-specific protease inhibitors (Pis). The 4 Pls available are saquinavir mesylate, ritonavir, indinavir sulfate, and nelfinavir mesylate.
S G, Deeks, P A, Volberding
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Journal of Enzyme Inhibition, 1992
The human immunodeficiency virus (HIV), the etiological agent for the acquired immune deficiency syndrome (AIDS), is a retrovirus which makes use of a virally-encoded aspartic protease to perform specific proteolytic processing of two of its gene products in order to form active enzymes and structural proteins within the mature virion.
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The human immunodeficiency virus (HIV), the etiological agent for the acquired immune deficiency syndrome (AIDS), is a retrovirus which makes use of a virally-encoded aspartic protease to perform specific proteolytic processing of two of its gene products in order to form active enzymes and structural proteins within the mature virion.
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Hyperlipidemia and inhibitors of HIV protease
Current Opinion in Clinical Nutrition and Metabolic Care, 2001HIV 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
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Brain Delivery of HIV Protease Inhibitors
Archiv der Pharmazie, 2003AbstractTo overcome the problems of peptidomimetic drug delivery to the specific organs, the use of dihydropyridine ↔ pyridinium chemical delivery systems to deliver peptides to the brain is considered in this work. An HIV protease inhibitor lead compound; KNI 279 was selected for the study.
Mahmoud M, Sheha +2 more
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