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Therapie

Solas C, Muret P.
PMID: 27393201
Therapie. 2011 May-Jun;66(3):213-9. doi: 10.2515/therapie/2011032.

The HIV protease inhibitor atazanavir presents a wide inter-individual variability related to an intense hepatic metabolism. Dose-dependant elevations of bilirubin have been frequently reported with atazanavir. Relative to literature, the atazanavir therapeutic drug monitoring can it be proposed? In...

The Low-Barrier Double-Well Potential of the O(δ)(1)-H-O(δ)(1) Hydrogen Bond in Unbound HIV Protease:  A QM/MM Characterization.

Journal of chemical theory and computation

Porter MA, Molina PA.
PMID: 26627038
J Chem Theory Comput. 2006 Nov;2(6):1675-84. doi: 10.1021/ct600200s.

The presence of a low-barrier hydrogen bond (LBHB) in aspartyl proteases and its implications in drug design have been the subject of intense study. Here, we present a combined quantum mechanical/molecular mechanical (QM/MM)-Numerov procedure and use it to characterize...

P-glycoprotein, secretory transport, and other barriers to the oral delivery of anti-HIV drugs.

Advanced drug delivery reviews

Aungst BJ.
PMID: 10837770
Adv Drug Deliv Rev. 1999 Oct 18;39(1):105-116. doi: 10.1016/s0169-409x(99)00022-8.

Orally administered anti-HIV drugs must be adequately and consistently absorbed for therapy to be successful. This review discusses the barriers to achieving oral bioavailability for the currently available anti-HIV drugs. Most reverse transcriptase inhibitors have good oral bioavailabilities. Didanosine...

Oral absorption of the HIV protease inhibitors: a current update.

Advanced drug delivery reviews

Williams GC, Sinko PJ.
PMID: 10837775
Adv Drug Deliv Rev. 1999 Oct 18;39(1):211-238. doi: 10.1016/s0169-409x(99)00027-7.

Although the human immunodeficiency virus (HIV) protease inhibitors are highly effective, they are characterized by low and/or variable bioavailability with limited penetration into the central nervous system (CNS). Their clinical use is limited by patient compliance and by drug-drug...

Synthesis of heterocyclic thiosulfonates.

Organic letters

Vara Prasad JV.
PMID: 10804556
Org Lett. 2000 Apr 20;2(8):1069-72. doi: 10.1021/ol0056170.

[formula: see text] A simple synthesis of heterocyclic thiosulfonates containing indole, indoline, benzoimidazole, and quinoxaline rings is described. The synthesis of these thiosulfonates involves the preparation of the appropriately substituted thiols followed by sulfonylation to give thiosulfonates. The corresponding...

Human immunodeficiency virus protease inhibitors. From drug design to clinical studies.

Advanced drug delivery reviews

Lin JH.
PMID: 10837559
Adv Drug Deliv Rev. 1997 Sep 15;27(2):215-233. doi: 10.1016/s0169-409x(97)00044-6.

The discovery of human immunodeficiency virus (HIV) protease inhibitors is an example in which pharmacokinetic evaluation was implemented early in the discovery phase to obtain optimal pharmacological and pharmacokinetic properties. Currently, three HIV protease inhibitors, saquinavir, indinavir and ritonavir...

Transition-State Mimetics for HIV Protease Inhibitors: Stereocontrolled Synthesis of Hydroxyethylene and Hydroxyethylamine Isosteres by Ester-Derived Titanium Enolate Syn and Anti-Aldol Reactions.

The Journal of organic chemistry

Ghosh AK, Fidanze S.
PMID: 11672244
J Org Chem. 1998 Sep 04;63(18):6146-6152. doi: 10.1021/jo980159i.

Stereocontrolled syntheses of hydroxyethylene dipeptide isostere and aminoalkyl epoxides for hydroxyethylamine isosteres are described. The stereochemistry of both stereogenic centers of the aminoalkyl epoxides 10 and 15 as well as the gamma-lactone 17 was assembled by our recently developed...

Analysis of HIV Protease Killing Through Caspase 8 Reveals a Novel Interaction Between Caspase 8 and Mitochondria.

The open virology journal

Algeciras-Schimnich A, Belzacq-Casagrande AS, Bren GD, Nie Z, Taylor JA, Rizza SA, Brenner C, Badley AD.
PMID: 18818773
Open Virol J. 2007 Dec 27;1:39-46. doi: 10.2174/1874357900701010039.

Human Immunodeficiency Virus (HIV) protease initiates apoptosis of HIV-infected cells by proteolytic cleavage of procaspase 8, creating a novel peptide termed casp8p41. Expression of casp8p41 alone is sufficient to initiate caspase-dependent cell death associated with mitochondrial depolarization. Since casp8p41...

Targeting HIV protease: from peptidomimetics to non-peptide inhibitors.

IDrugs : the investigational drugs journal

Gago F.
PMID: 16158350
IDrugs. 1999 Apr;2(4):309-20.

The identification of HIV-1 protease as a target for therapeutic intervention against AIDS, soon followed by the resolution of its three-dimensional structure, has had a major impact on drug-design methodologies. The possible HIV-1 protease inhibitors that have been synthesized...

Amprenavir (Vertex Pharmaceuticals Inc).

IDrugs : the investigational drugs journal

Billich A.
PMID: 16155850
IDrugs. 1999 May;2(5):466-82.

Amprenavir is an oral, non-peptidic HIV-protease inhibitor undergoing phase III trials for the treatment of HIV and AIDS. In October 1998, Glaxo Wellcome submitted a new drug application (NDA) for amprenavir (Agenerase) in the US and Canada for which...

Distinguishing HIV-1 drug resistance, accessory, and viral fitness mutations using conditional selection pressure analysis of treated versus untreated patient samples.

Biology direct

Chen L, Lee C.
PMID: 16737543
Biol Direct. 2006 May 31;1:14. doi: 10.1186/1745-6150-1-14.

BACKGROUND: HIV can evolve drug resistance rapidly in response to new drug treatments, often through a combination of multiple mutations 123. It would be useful to develop automated analyses of HIV sequence polymorphism that are able to predict drug...

HIV Protease Inhibitors: Effect on the Opportunistic Protozoan Parasites.

The open medicinal chemistry journal

Alfonso Y, Monzote L.
PMID: 21629510
Open Med Chem J. 2011;5:40-50. doi: 10.2174/1874104501105010040. Epub 2011 Mar 09.

The impact of highly active antiretroviral therapy (HAART) in the natural history of AIDS disease has been allowed to prolong the survival of people with HIV infection, particularly whose with increased HIV viral load. Additionally, the antiretroviral therapy could...

Showing 1 to 12 of 165 entries