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Synthesis of a novel potent cyclic peptide MC4-ligand by ring-closing metathesis.

Abstract：

:The synthesis of a novel potent cyclic peptide MC4-ligand by ring-closing metathesis (RCM) is described. Based on the Ac-Nle-Gly-Lys-D-Phe-Arg-Trp-Gly-NH2-MC4 ligand, Ac-Nle-Alg-Lys-D-Phe-Arg-Trp-Alg-NH2 was designed and synthesized followed by cyclization using RCM. Both compounds are high affinity and selective MC4-R-agonists. The cyclic RCM-peptide was more potent in a rat-grooming assay.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Wels B,Kruijtzer JA,Garner K,Nijenhuis WA,Gispen WH,Adan RA,Liskamp RM

doi

10.1016/j.bmc.2005.04.027

subject

Has Abstract

pub_date

2005-07-01 00:00:00

pages

4221-7

issue

13

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(05)00326-3

journal_volume

13

pub_type

杂志文章

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