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Modification of the enkephalin "message" with an artificial polycationic C-terminus.

Abstract：

:The C-terminal "address" sequences of prodynorphin-derived opioid peptides contain an unusually high proportion of basic residues, which are known to be crucial for conferring high activity and selectivity for kappa-opioid receptors. In an effort to investigate the possibility that the polycationic "tails" may be involved in a coulombic interaction with a complementary polyanionic receptor domain, we attached a series of achiral peptide-like cationic fragments to the C-terminus of the opioid peptide "message", Tyr-Gly-Gly-Phe. Binding of the various compounds to opioid receptor types in guinea pig brain membranes was weak, and the pharmacologic activities in the guinea pig ileum were marginal. These results indicate either that the chosen ligand design does not satisfy the structural requirements of the hypothesized coulombic interaction or that the latter is a minor criterion governing receptor recognition.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Jacobson AR,Tam SW,Sayre LM

doi

10.1021/jm00113a020

subject

Has Abstract

pub_date

1991-09-01 00:00:00

pages

2816-21

issue

9

eissn

0022-2623

issn

1520-4804

journal_volume

34

pub_type

杂志文章

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