IN-VITRO STABILITY OF SOME REDUCED PEPTIDE-BOND PSEUDOPEPTIDE ANALOGSOF DYNORPHIN-A

Citation
Jp. Meyer et al., IN-VITRO STABILITY OF SOME REDUCED PEPTIDE-BOND PSEUDOPEPTIDE ANALOGSOF DYNORPHIN-A, Peptides, 16(7), 1995, pp. 1215-1219
Citations number
43
Categorie Soggetti
Biology
Journal title
ISSN journal
01969781
Volume
16
Issue
7
Year of publication
1995
Pages
1215 - 1219
Database
ISI
SICI code
0196-9781(1995)16:7<1215:ISOSRP>2.0.ZU;2-N
Abstract
Eight analogues of DYN A(1-11)-NH2 incorporating the nonhydrolyzable p si[CH2-NH] peptide bond surrogate were tested for their in vitro enzym atic stability in mouse brain homogenates. Results show that the Leu(5 )-Arg(6) and to a lesser extent the Arg(7)-Ile(8) and Ile(8)-Arg(9) pe ptide bonds are the more susceptible to enzymatic cleavage in the nati ve peptide. (Leu5 psi[CH2-NH]Arg(6))DYN A(1-11)-NH2 exhibits an almost complete resistance to enzymatic cleavage with a half-life greater th an 500 min in brain, compared to 42 min for the standard peptide, DYN A(1-11)-NH2.