A review.The preparation of α-aminoalkyl-α'-(halomethyl) ketone derivatives was reviewed.The application of these compounds toward the synthesis of saquinavir (invirase), palinavir, nelfinavir (viracept), amprenavir (agenerase) was discussed.

01 Apr 2002·Journal of Molecular BiologyQ2 · BIOLOGY

In Vitro Cleavage of eIF4GI but not eIF4GII by HIV-1 Protease and its Effects on Translation in the Rabbit Reticulocyte Lysate System

Q2 · BIOLOGY

Article

Author: Théophile Ohlmann ; Jérôme Garin ; Simon J. Morley ; Florence Roux ; Didier Décimo ; Jean-Luc Darlix ; Déborah Prévôt

In eukaryotic cells, protein synthesis is regulated by a set of initiation factors (eIF) that are required for recruiting the 40 S ribosomal subunit onto the mRNA molecule. Among these proteins, eIF4GI, which is targeted by picornaviral proteases, makes a bridge between the mRNA cap structure (via eIF4E) and the 40 S ribosome (via eIF3). Recently, internal ribosome entry segment (IRES) elements have been characterized in the genomic RNA of both simian immunodeficiency virus (SIV) and human immunodeficiency virus type 1 (HIV-1), suggesting that viral expression of these two viruses can be regulated at the translational level. Thus, by analogy with members of the picornavirus family, we have investigated the action of the HIV-1 protease on initiation factors eIF4GI and eIF4GII using cell extracts and the rabbit reticulocyte lysate system. Our results show that eIF4GI, but not eIF4GII, is substrate for HIV-1 protease and this effect can be prevented by a HIV-1 protease inhibitor, palinavir. However, in contrast to picornaviral proteases, the cleavage of eIF4GI by HIV-1 protease occurs at multiple sites and impairs translation of both cap-dependent and IRES-containing RNAs, except for the HCV IRES, which does not require eIF4GI or eIF4GII for activity.

01 Jun 1998·Journal of Pharmaceutical SciencesQ3 · MEDICINE

Pharmacokinetic Aspects of Palinavir, an HIV Protease Inhibitor, in Sprague–Dawley Rats

Q3 · MEDICINE

Article

Author: Francine Liard ; Christiane Yoakim ; William L. Paris ; Jorge Jaramillo

Palinavir is a potent peptidomimetic in vitro inhibitor of the human immunodeficiency virus type 1 (HIV-1) and type 2 (HIV-2) proteases and of the replication of HIV and SIV laboratory strains in cell culture.The pharmacokinetics of palinavir after i.v., oral (po), and intraduodenal (id) administration were studied in Sprague-Dawley rats.Plasma samples were analyzed for palinavir concentration using a liquid-liquid extraction followed by HPLC anal.Noncompartmental anal. was used to calculate kinetic parameters.The area under the plasma concentration (C) vs. time (t) curve (AUC) values for palinavir showed nonlinear pharmacokinetics.The half-life of palinavir was 0.7 h.Other parameters, including C_max, mean residence time (MRT), total clearance (Cl_tot), and volume of distribution at steady state (V_SS) also changed with dosing.The bioavailability estimated after intraduodenal administration (29.8%) was not different from that obtained after oral administration (26.1%).

100 Deals associated with Palinavir

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Indication	Highest Phase	Country/Location	Organization	Date
HIV Infections	Phase 1	US	-	-
HIV Infections	Phase 1	-	C.H. Boehringer Sohn AG & Co. KG	-

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