A series of linear and monocyclic (with a disulfide bridge only) analogues of trypsin inhibitor SFTI-1 modified in the P-1 and/or P-1' positions were synthesized by the solid-phase method. In the substrate specificity P-1 position, Phe or N-benzylglycine (Nphe) were introduced, whereas the conserved Ser6 in Bownam-Birk (BBI) inhibitors was replaced by Hse (L-homoserine), Nhse [N-(2-hydroxyethyl)glycine], Sar, and Ala. Kinetic studies of interaction of the analogues with bovine alpha-chymotrypsin have shown that in monocyclic (but not linear) analogues, Hse and Nhse are tolerated to afford potent inhibitors. This is the first evidence that the absolutely conserved Ser present in the inhibitor's P-1' position can be successfully replaced by a synthetic derivative. Copyright (C) 2011 European Peptide Society and John Wiley & Sons, Ltd.
Authors
- Łukajtis Rafał,
- Łȩgowska Anna,
- Wysocka Magdalena,
- Dȩbowski Dawid,
- Lesner Adam,
- Rolka Krzysztof,
- Adam Lesner link open in new tab ,
- Rafał Łukajtis link open in new tab
Additional information
- DOI
- Digital Object Identifier link open in new tab 10.1002/psc.1330
- Category
- Publikacja w czasopiśmie
- Type
- artykuł w czasopiśmie wyróżnionym w JCR
- Language
- angielski
- Publication year
- 2011
