Elevated levels of neutrophil elastase in CPOD (Chronic Obstructive Pulmonary Disease) airways are regarded as the main trigger lung destruction and inflammation. SLPI (Secretory leukocyte protease inhibitor), an inhibitor protease, represents attractive candidate for treatment chronic diseases due to proteases excess. The antiprotease active site has been located on C-terminal domain. This stu...

Dengue virus (DENV) protease is an attractive target for drug development; however, no compounds have reached clinical development to date. In this study, we utilized a potent West Nile virus protease inhibitor of the pyrazole ester derivative class as a chemical starting point for DENV protease drug development. Compound potency and selectivity for DENV protease were improved through structure...

Purpose of the study Fos-Amprenavir is one of the protease inhibitor that is recommended to treat protease inhibitor naïve of experienced patients. Amprenavir and darunavir share at least in part chemical structures and thus a possible selection of close protease gene mutations. Little is known about the frequency and the type of resistance mutations selected after virological failure to FosAmp...

protease inhibitors have played an instrumental role in decreasing mortality and morbidity among people with hiv infection. At the same time, this class of antiretrovirals has been associated with a number of disadvantages. First, protease inhibitor therapy often comes with a high pill burden, complex dosing schedules, and careful dietary considerations. Second, they are associated with a growi...

it has already been reported that muscle necrosis induced by various phenylenediamine derivatives are correlated with their autoxidation rate. now in a more detailed investigation of the cytotoxic mechanism using a model system of isolated hepatocytes and ring-methylated structural isomer durenediamine (dd) we have shown that under aerobic conditions, phenylenediamine induced cytotoxicity and r...

Inhibition of the main protease (Mpro) SARS-CoV-2 has been suggested to be vital in shutting down viral replication a host. Most efforts aimed at inhibiting MPro activity have channeled into competitive inhibition active site, but this strategy will require high inhibitor concentration and impressive inhibitor-MPro binding affinity. Allosteric can potentially serve as an effective for alleviati...

An endogenous inhibitor of the reticulocyte ATP-dependent proteolytic system has been purified partially by ammonium sulfate precipitation from rabbit reticulocyte and erythrocyte extracts. Inhibitor-free protease rapidly degrades 21-40% of the substrate [14C]methyl-alpha-casein per hour, resembling ATP-dependent activity in reticulocyte extracts. This proteolytic activity is not stimulated by ...

BACKGROUND Serine protease inhibitors act as modulators of serine proteases, playing important roles in protecting animal toxin peptides from degradation. However, all known serine protease inhibitors discovered thus far from animal venom belong to the Kunitz-type subfamily, and whether there are other novel types of protease inhibitors in animal venom remains unclear. PRINCIPAL FINDINGS Here...