Thesis (Ph.D.)- University of Birmingham, Dept of Chemistry.
The substrates (10–19 μM) were incubated with the protease(s) in the concentration range of μM (as indicated for each experiment) in 50 mM Tris–HCl buffer (pH ) containing 10% glycerol. Peptide (substrate) concentration was determined based on by: 3. Recombinant 3C protease and the fluorogenic substrate were used to evaluate the IC 50 of the synthesized compounds. Compound 4 with the basic features of AG with P1-lactam ring, P1′-α,β-unsaturated ester, and P2-Boc-Phe did not inhibit the enzyme at 20 μM (the greatest concentration tested). With additional cinnamoyl groups, 6a–c showed smaller IC 50 values of , Cited by: Design, synthesis, and evaluation of azapeptides as substrates and inhibitors for human rhinovirus 3C protease. Bioorganic & Medicinal Chemistry Letters , 9 (4), DOI: /SX(99) Q. May Wang. Protease inhibitors as potential antiviral agents for the treatment of picornaviral by: A method is described here for identifying good protease substrates among approximately 10(7) possible sequences. A library of fusion proteins was constructed containing an amino-terminal domain used to bind to an affinity support, followed by a randomized protease substrate sequence and the carboxyl-terminal domain of M13 gene III. Each fusion protein was displayed as a single copy on.
Journals & Books; Help Download full text in PDF Download. Advanced. Tetrahedron. Vol Is 9 October , Pages A convenient synthesis of amino acid p-nitroanilides; synthons in the synthesis of protease substrates. Solid-to-solid peptide synthesis is an enzyme-catalyzed reaction carried out in a mixture consisting of solid substrates and up to 20% (w/w) of enzyme solution in water. Processing of the gag and pol gene precursor proteins of retroviruses is essential for infectivity and is directed by a viral protease that is itself included in one of these precursors. We demonstrate here that small synthetic peptides can be used as both model substrates and inhibitors to investigate the specificity and molecular parameters. Rich DH, Bernatowicz MS. Synthesis of analogues of the carboxyl protease inhibitor pepstatin. Effect of structure in subsite P3 on inhibition of pepsin. J Med Chem. Jul; 25 (7)– Rich DH, Sun ET. Mechanism of inhibition of pepsin by pepstatin. Effect of inhibitor structure on dissociation constant and time-dependent inhibition.
Shalini Gupta, Bhawana Pathak, in Abatement of Environmental Pollutants, Proteases. Proteases belong to group of hydrolases in which it aids in breakdown of peptide bonds in aqueous phase and synthesis in nonaqueous phase. Proteases cover wide group of industrial applications such as in food, leather, detergent, and pharmaceutical fields (Singh, ; Beena and Geevarghese, ). Synthesis of a HyCoSuL peptide substrate library to dissect protease substrate specificity. Poreba M(1)(2), Salvesen GS(1), Drag M(2). Author information: (1)Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California, USA. The substrate on which translation takes place is the ribosome. Remember that many of a cell’s ribosomes are found associated with the rough ER, and carry out the synthesis of proteins destined for the Golgi apparatus. Ribosomal RNA (rRNA) is a type of RNA that, together with proteins, composes the structure of the ribosome. Ribosomes exist. ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option.