| Autor: |
Michael J. Lew, Patrick Perlmutter, Marie-Isabel Aguilar, K. M. Stewart, M. F. Harte, E. Boulos, S. B. Reeve, Silas Bond, M. U. Norman, R. A. Lew, A. I. Smith |
| Rok vydání: |
2001 |
| Předmět: |
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| Zdroj: |
Peptides: The Wave of the Future ISBN: 9789401039055 |
| DOI: |
10.1007/978-94-010-0464-0_257 |
| Popis: |
s-Amino acids contain an extra carbon between the amino and carboxy-termini; this modification renders the adjacent peptide bond resistant to hydrolysis [1,2]. We hypothesize that substitution of the residues at the scissile bond with s-amino acids can confer resistance to cleavage without necessarily abolishing binding to the enzyme. In the present study, we have synthesized a series of s-amino acid-substituted analogues of bradykinin (BK), and examined both their susceptibility to cleavage by and their ability to inhibit the soluble metalloendopeptidases EC 3.4.24.15 (EP24.15) and EC 3.4.24.16 (EP24.16) [3]. Our findings suggest that s-amino acid incorporation at the scissile bond completely prevents peptide hydrolysis with only minimal reduction in affinity for the enzyme. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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