• Papain family cysteine proteases are key factors in the pathogenesis of cancer invasion, arthritis, osteoporosis, and microbial infections. (pnas.org)
  • An attractive target for new chemotherapy is a family of cathepsin L-like (cpL) and cathepsin B-like (cpB) cysteine proteases found in all species of Leishmania examined, and required for parasite growth or virulence ( 3 - 5 ). (pnas.org)
  • Inhibitors that would effectively target both types of cysteine proteases in Leishmania , while maintaining some selectivity versus homologous host enzymes, would be ideal drug leads. (pnas.org)
  • The irreversible inhibitors are pseudopeptide substrate analogues that take advantage of the unique reactivity of the active site sulfhydryl of cysteine proteases to confer specificity for this enzyme family but maintain activity against both cpL and cpB proteases ( 7 , 8 ). (pnas.org)
  • Saquinavir which has the trade name Invirase was the first protease inhibitor to be approved by the FDA (December 1995) for the treatment of HIV infection. (middlebury.edu)
  • Protease inhibitors (PIs) are potent with a high genetic barrier to resistance and have the potential for use as monotherapy after viral load (VL) suppression achieved on combination therapy. (openaire.eu)
  • In the present study, we report that a typical, natural protease inhibitor, the Bowman-Birk inhibitor isolated from soybeans, survives inactivation by stomach digestion in rodents and appears to be fully active as a protease inhibitor in the small intestine, where it complexes with the proteases occurring there, i.e., trypsin and chymotrypsin. (nih.gov)
  • Several of the synthetic derivatives of that lead, produced by combinatorial synthetic chemistry, proved to be potent inhibitors of homologous cpLs of malaria ( 10 ) and the Leishmania cpB ( 2 ). (pnas.org)
  • This study will be a retrospective observational study assessing identifiable tolerability problems in terms of their comparative incidence among Human Immunodeficiency Virus (HIV) patients treated with cART regimens including one of four different protease inhibitors [Atazanavir sulfate (ATV), Darunavir (DRV), Fosamprenavir (FPV), or Lopinavir (LPV)] and the impact of these identifiable tolerability problems on PI persistence, healthcare utilization, and healthcare costs. (clinicaltrials.gov)
  • Protease inhibitors not only greatly reduce the number of new HIV copies that are made, they also make those that do manage to get produced defective in some way, so that they cannot go on and infect new cells. (encyclopedia.com)
  • Once the protease is blocked, HIV makes copies of itself that cannot infect other cells. (middlebury.edu)
  • Thus, taking a combination of both nucleoside analogs and protease inhibiters, will lessen the chance for resistance. (middlebury.edu)
  • All subjects also take a background regimen of two nucleoside/nucleotide reverse transcriptase inhibitors. (clinicaltrials.gov)
  • Protease inhibitor cocktails with EDTA include separate 0.5M EDTA solution. (fishersci.ca)
  • Halt Protease Inhibitor Cocktails are 100X solutions containing optimized concentrations of six broad-spectrum protease inhibitors stabilized in high-quality dimethylsulfoxide (DMSO). (fishersci.ca)
  • The stable, concentrated liquid cocktails are easy to use, and the several different package sizes make Halt Protease Inhibitor Cocktails exceptionally convenient for either small-scale or large-scale uses. (fishersci.ca)
  • The protease cleaves the serpin at the reactive site within the RCL, establishing a covalent linkage between the serpin reactive site and the protease. (rcsb.org)
  • The resulting inactive serpin-protease complex is highly stable (By similarity). (rcsb.org)
  • Abstract C1 inhibitor (C1INH) is a serpin that regulates both complement and contact (kallikrein-kinin) system activation. (omicsonline.org)
  • Reversible inhibitors were discovered through a structure-based drug design screen and subsequent combinatorial synthetic optimization using models of both Leishmania major cpB and cpL ( 2 ). (pnas.org)
  • In studies with Leishmania mexicana , elimination of selected cysteine protease genes by homologous recombination showed that null mutants of the cpL gene array designated "cpb" had reduced virulence in highly susceptible BALB/c mice, and they produced no lesions at all in C57BL/6 or CBA/Ca mice ( 3 , 4 ). (pnas.org)
  • The Protease Inhibitor Monotherapy Versus Ongoing Triple Therapy (PIVOT) trial: a randomised controlled trial of a protease inhibitor monotherapy strategy for long-term management of human immunodeficiency virus infection. (openaire.eu)
  • However, the high fat diet does not overcome the inhibitor going through extensive metabolism in the liver by the hepatatic cytochrome P450 3A system. (middlebury.edu)