ProteasenReaktionsmechanismenGeneral-base catalysis in serine proteases still poses mechanistic challenges despite decades of research. Whether proton transfer from the catalytic Ser to His and nucleophilic attacko nt he substrate are concerted or stepwise is still under debate,e ven for the classical ...
A model that describes the steps of the serine protease mechanism. (a) TM decreases dynamics in the substrate binding pocket to promote protein C binding. (b) TM-induces μs-ms dynamics that may promote the optimal activity of the catalytic triad. The backbone of residues 77-84CT (108-116...
How Might an Enzyme Mechanism Like This Arise? As a protein like a serine protease evolves, how might the earliest versions have worked, before the current elegant enzyme structures had evolved? Scientists used targeted mutations in the protease subtilisin to explore some possibilities (Carter & Wel...
Previous studies had alluded to a gradual narrowing of primary specificity, from the initial ancient serine protease with a broad primary specificity, as the mechanism by which diversity was achieved in this protease superfamily (Perona and Craik, 1997). Our findings support this view but suggest ...
It is known that trypsin could be involved in various steps of spermatogenesis in the testis [15]. Similarly to the proteasome-ubiquitin complex [16], serine protease could be responsible for cell apoptosis and tissue turnover. However, there are no data proving the potential to degrade sperm ...
Thus, the Sep1 protease of B. firmus is a novel biocontrol factor with activity against a root-knot nematode. We then used C. elegans as a model to elucidate the nematicidal mechanism of Sep1, and the results showed that Sep1 could degrade multiple intestinal and cuticle-associated proteins...
However, its regulatory mechanism remains largely unknown, partly because the structure of FAM111A protein has not been determined. Furthermore, there currently is no quantitative, in vitro assay to directly measure FAM111A protease activity, hampering the ability to examine the enzyme’s activity....
The kinin-induced release of tPA from endothelial cells is in turn suppressed by the inhibited kinin release, it being possible thereby for fibrinolysis to be downregulated by this mechanism. A further advantage of these compounds is, despite selectivity, a certain inhibitory effect of these ...
We have now found that certain aromatic compounds carrying lipophilic side chains are particularly effective as inhibitors of the serine protease, tryptase. It is envisaged that the compounds of the invention will be useful not only in the treatment and prophylaxis of asthma but also of other aller...
Hedstrom L: Serine protease mechanism and specificity. Chem Rev. 2002, 102 (12): 4501-4524. 10.1021/cr000033x. Article PubMed CAS Google Scholar Stroud RM, Kay LM, Dickerson RE: The structure of bovine trypsin: electron density maps of the inhibited enzyme at 5 Angstrom and at 2-7 An...