نتایج جستجو برای: protease inhibitor
تعداد نتایج: 245560 فیلتر نتایج به سال:
Two new double-headed protease inhibitors have been isolated from black-eyed peas. The isoinhibitors can be purified to homogeneity with greater than 90% recovery in a four-step procedure by means of sequential affinity chromatography on trypsin-Sepharose and chymotrypsin-Sepharose affinity columns. The isoinhibitors both have molecular weights near 8,000 and both have the same NH1-terminal res...
OBJECTIVE HIV protease inhibitors have been successfully used in highly active antiretroviral therapy of HIV-1 infection, but their benefits are compromised by a number of clinically important adverse side-effects. Several studies showed that protease inhibitors induce sarco/endoplasmic reticulum stress and overproduction of reactive oxygen species (ROS), but the hierarchy of these events was n...
BACKGROUND Tipranavir, a novel protease inhibitor, has demonstrated antiviral activity against protease inhibitor-resistant human immunodeficiency virus type 1 (HIV-1) isolates. The Randomized Evaluation of Strategic Intervention in multi-drug reSistant patients with Tipranavir (RESIST-2) trial is an ongoing, open-label, phase III trial comparing ritonavir-boosted tipranavir (TPV/r) plus an opt...
BACKGROUND Cross-resistance after first-line antiretroviral therapy (ART) failure is expected to impair activity of nucleoside reverse-transcriptase inhibitors (NRTIs) in second-line therapy for patients with HIV, but evidence for the effect of cross-resistance on virological outcomes is limited. We aimed to assess the association between the activity, predicted by resistance testing, of the NR...
Rhoads, M. L., Fetterer, R. H., Hill, D. E., and Urban, J. F., Jr. 2000. Trichuris suis: A secretory chymotrypsin/elastase inhibitor with potential as an immunomodulator. Experimental Parasitology 95, 36– 44. A serine protease inhibitor, termed TsCEI, was purified from adultstage Trichuris suis by acid precipitation, affinity chromatography (elastase–agarose), and reverse-phase HPLC. The molecu...
Kunitz-type serine protease inhibitors are involved in various physiological processes, such as ion channel blocking, blood coagulation, fibrinolysis, and inflammation. While spider-derived Kunitz-type proteins show activity in trypsin or chymotrypsin inhibition and K(+) channel blocking, no additional role for these proteins has been elucidated. In this study, we identified the first spider (A...
The tryptophan time-resolved fluorescence intensity and anisotropy of the HIV-1 protease dimer is shown to be a quick and efficient method for the conformational characterization of protease inhibitor complexes. Four fluorescence lifetimes were needed to adequately describe the fluorescence decay of the two tryptophan residues, W6 and W42, per protease monomer. As a result of the wavelength dep...
The effects of many protease inhibitor (PI)-selected mutations on the susceptibility to individual PIs are unknown. We analyzed in vitro susceptibility test results on 2,725 HIV-1 protease isolates. More than 2,400 isolates had been tested for susceptibility to fosamprenavir, indinavir, nelfinavir, and saquinavir; 2,130 isolates had been tested for susceptibility to lopinavir; 1,644 isolates ha...
Approximately 20 years has passed since the first human trial with HIV-1 protease inhibitors. Protease inhibitors set the stage for combination therapy in the mid-1990s but are now rarely used in first-line combination therapy and reserved for salvage therapy. Initially, resistance to protease inhibitors was deemed unlikely due to the small enzymatic target with limited genetic diversity, the e...
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