PMID: 6988046Jan 1, 1980Paper

Resistance of FK 33-824 and other enkephalin analogues to peptidase degradation

Brain Research Bulletin
R Huguenin, R Maurer

Abstract

The stability of analogues of Met-enkephalin containing different chemical substitutions in the amino acid sequence to enzymatic degradation by a mouse brain extract and by rat striatal membranes have been compared. On incubation with the mouse brain extract, the naturally occurring Met-enkephalin was completely destroyed within 5 min and 50% of (D-Ala2)Met-enkephalinamide was degraded within 2 1/2 hr, with the release of Tyr, Phe, Met, D-Ala-Gly and partially (D-)Ala and Gly. (D-Ala2, MePhe4, Met(O)ol5) enkephalin (FK 33-824) was degraded to 50% within 5 hr, giving merely Tyr and the tetrapeptide D-Ala-Gly-MePhe-Met(O)ol as degradation products. No metabolism was observed after incubation for 24 hr of (MeTyr1, D-Ala2, MePhe4, Met(O)ol5) enkephalin (FW 34-569) with the mouse brain extract. On incubation with rat striatal membranes in the presence of puromycin, Met-enkephalin was rapidly inactivated, principally by cleavage of the Gly3-Phe4 bond, whereas FK 33-824 was not split.

References

Nov 1, 1977·Brain Research Bulletin·A GrynbaumN Marks
Feb 21, 1977·Biochemical and Biophysical Research Communications·N MarksA Neidle

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Citations

Sep 28, 2000·The Journal of Peptide Research : Official Journal of the American Peptide Society·Y C ChenM Chorev
Jan 1, 1981·Peptides·G A OlsonD H Coy
May 31, 1982·Biochemical and Biophysical Research Communications·B Malfroy, J C Schwartz
Mar 1, 1986·The Journal of Pharmacy and Pharmacology·S SakuradaK Suzuki

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