Five protease inhibitors with different modes of action were found to reduce the growth of transformed mouse (Py3T3, SV3T3, and 3T12) and hamster (PyBHK) cells. Some of these inhibitors caused the transformed cells to cease growth at saturation densities characteristic for nontransformed cells. The protease inhibitors were strikingly selective with regard to the transformed cells; they had esse...

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The effects of fluconazole on the pharmacokinetics of the HIV protease inhibitor ritonavir were investigated after multiple dosing in an open-label study. In this randomized, two-period crossover study, eight healthy subjects received ritonavir alone (200 mg every 6 hr for 4 days) and ritonavir with fluconazole (400 mg on day 1, 200 mg every day on days 2-5) with a 2-week washout period. Ritona...

The novel hydroquinone, (E)-2-(4-hydroxy-3-methyl-2-butenyl)-hydroquinone, and known compound, polyporenic acid C, were isolated as matrix metallo-proteinase inhibitors from the mushroom, Piptoporus betulinus.

Cruzain, the major cysteine protease of the protozoan parasite Trypanosoma cruzi, is a target of rational drug design for chemotherapy of Chagas' disease. The precise biological role of cruzain in the parasite life cycle and the mechanism involved in the trypanocidal effect of cysteine protease inhibitors are still unclear. Here we report biological and ultrastructural alterations caused by cys...

Recently we reported') the isolation and structural elucidation of a SAKAGUCHI-positive metabolite of Streptomyces, found in the course of chemical screening of microbial metabolites. The compound proved to be identical to antipain=' discovered as a protease inhibitor. In the present paper, we wish to report the isolation of another SAKAGUCHI-positive metabolite, KF77-AG6, which corresponds to ...

Human immunodeficiency virus (HIV) protease inhibitors have been successfully used in highly active antiretroviral therapy for HIV-1 infection. Treatment of patients infected with HIV with HIV protease inhibitors is unfortunately associated with a number of clinically significant metabolic abnormalities and an increased risk of premature atherosclerosis and myocardial infarction. However, the c...