In this study, virtual screening and molecular dynamics (MD) protocols were applied to screen 2826 FDA-approved natural product drugs from the Selleckchem.com library for prospective inhibitors of SARS-CoV-2 main protease. From through HTVS, SP XP docking analysis, hyperoside, rutin hydrate, rutoside quercitrin displayed a stronger binding affinity with respective scores –11.389, –11.340, –11.0...

in april 1999, dr. schlomo staszewski had a simple message for clinicians attending his first prn lecture: that protease inhibitors were a less-than-ideal therapeutic option and that focus should be placed on prescribing protease inhibitor-sparing regimens, whenever possible. “We were seeing problems with dosing, with side effects, with dietary restrictions, with resistance and cross resistance...

Objective: Investigations were carried out to isolate bacteria from saline-alkali soils and determined optimized alkaline protease activity and stability produced by a wild strain of bacillus sp. in submerged fermentation (SMF). Methods: Optimum temperature for enzyme activity in the crude extract was 40 ◦C at a pH between 8.0 and 9.0. The studies on pH stability showed that the enzyme...

Proteases, also known as proteolytic enzymes, are enzymes that catalyze the breakdown of proteins by hydrolysis of peptide bonds. Earlier proteases were considered as only protein degrading enzymes, however now dramatically the view has changed. Proteases are extremely important signalling molecules that are involved in numerous vital processes like apoptosis, cell growth and activation, adhesi...

A series of novel HIV-1 protease inhibitors based on two pseudosymmetric dipeptide isosteres have been synthesized and evaluated. The inhibitors were designed by incorporating N-phenyloxazolidinone-5-carboxamides into the hydroxyethylene and (hydroxyethyl)hydrazine dipeptide isosteres as P2 and P2' ligands. Compounds with (S)-phenyloxazolidinones attached at a position proximal to the central h...

the aim of the present work was to purify cysteine protease inhibitors from rapeseed (brassica napus l.), with potential activity on digestive protease of colorado potato beetle (cpb), leptinotarsa decemlineata (say). ammonium sulfate precipitated proteinaceous fractions; 30, 50, 70, and 100% showed 39.07, 57.03, 51.47, and 22.44% inhibition on the fourth instar larval gut general protease acti...

The Kunitz-type protease inhibitors are the best-characterized family of serine protease inhibitors, probably due to their abundance in several organisms. These inhibitors consist of a chain of ~60 amino acid residues stabilized by three disulfide bridges, and was first observed in the bovine pancreatic trypsin inhibitor (BPTI)-like protease inhibitors, which strongly inhibit trypsin and chymot...

M1 myeloid leukemic cells overexpressing wild-type p53 undergo apoptosis. This apoptosis can be suppressed by some cytokines, protease inhibitors, and antioxidants. We now show that induction of apoptosis by overexpressing wild-type p53 is associated with activation of interleukin-1beta-converting enzyme (ICE)-like proteases, resulting in cleavage of poly(ADP- ribose) polymerase and the proenzy...

Extensive efforts have been made to develop anti-HIV drugs from potential HIV-1 protease inhibitor1'2) since the protease inhibitors have been proven to produce immature and non-infectious viruses3'4). In order to find HIV-1 protease inhibitors and study the kinetics of inhibition of the protease, many assay methods have been devised using the protease produced by genetic engineering techniques...