Webl-Dap is also one of the most frequently found amino acids inserted in bioactive peptides, such as cyclotheonamide B, phleomycin, paenibacterin derivatives, lavendomycin, gastrin-releasing peptide receptor-specific scaffolds, capreomycin, various peptide-based antibacterials, and peptidomimetics, such as vitronectin [9,10,11,12,13,14,15,16]. WebSep 9, 1993 · The macrocyclic peptide cyclotheonamide A (CtA), isolated from the marine sponge Theonella sp., represents an unusual class of serine protease inhibitor. A complex of this inhibitor with human alpha-thrombin, a protease central to the bioregulation of thrombosis and hemostasis, was studied by x-ray crystallography.
Molecular basis for the inhibition of human alpha-thrombin by the ...
WebMay 1, 1998 · Their structures were determined by interpretation of spectral data and chemical degradation studies. They are closely related to the previously reported cyclotheonamide E, from which they differ in the N-acyl group of the alanyl side chain. Cyclotheonamides E, E2, and E3 were more active against thrombin than against trypsin. WebGraphical Abstract Structural modification at two positions is the key: Cyclotheonamide E4 unspecifically blocks trypsin-like serine proteases in a covalent fashion. We converted this compound into a reversibly binding, potent and selective β-tryptase inhibitor. Citing Literature Supporting Information Volume 5, Issue 3 March 1, 2010 Pages 367-370 chr toyota yellow
Total Synthesis of Cyclotheonamide C using a Tandem …
WebAug 1, 1995 · Three new thrombin and trypsin inhibitors, cyclotheonamides C (3), D (4), and E (8) were isolated from the marine sponge Theonella swinhoei.Their structures were determined by spectral and chemical methods. WebMolecular modeling of the thrombin inhibitor, cyclotheonamide A (CA), found two conformational families for theCA backbone, one of which resembles the bound CA structure as recently determined by X-ray crystallography. WebMar 1, 2010 · The cover picture shows the putative binding mode of cyclotheonamide A along the active-site cleft of subunit A of the β-tryptase homotetramer (top), a serine protease with trypsin-like activity that has been the focus of interest as a promising new drug target in the treatment of asthma. Based on this model, the cyclotheonamide E4 … chr toyota suv