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Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity.

Abstract：

:The tetrapeptide sequence His-Phe-Arg-Trp, derived from melanocyte-stimulating hormone (alphaMSH) and its analogs, causes a decrease in food intake and elevates energy utilization upon binding to the melanocortin-4 receptor (MC4R). To utilize this sequence as an effective agent for treating obesity, we improved its metabolic stability and intestinal permeability by synthesizing a library of backbone cyclic peptidomimetic derivatives. One analog, peptide 1 (BL3020-1), was selected according to its selectivity in activating the MC4R, its favorable transcellular penetration through enterocytes and its enhanced intestinal metabolic stability. This peptide was detected in the brain following oral administration to rats. A single oral dose of 0.5 mg/kg in mice led to reduced food consumption (up to 48% vs the control group) that lasted for 5 h. Repetitive once daily oral dosing (0.5 mg/kg/day) for 12 days reduced weight gain. Backbone cyclization was shown to produce a potential drug lead for treating obesity.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Hess S,Linde Y,Ovadia O,Safrai E,Shalev DE,Swed A,Halbfinger E,Lapidot T,Winkler I,Gabinet Y,Faier A,Yarden D,Xiang Z,Portillo FP,Haskell-Luevano C,Gilon C,Hoffman A

doi

10.1021/jm701093y

subject

Has Abstract

pub_date

2008-02-28 00:00:00

pages

1026-34

issue

4

eissn

0022-2623

issn

1520-4804

journal_volume

51

pub_type

杂志文章

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