ART (protein product of agouti-related transcript) as an antagonist of MC-3 and MC-4 receptors

被引：195

作者：

Fong, TM

Mao, C

MacNeil, T

Kalyani, R

Smith, T

Weinberg, D

Tota, MR

VanderPloeg, LHT

机构：

[1] Merck Research Laboratories, R80M-213, Rahway, NJ 07065

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1997年 / 237卷 / 03期

关键词：

D O I：

10.1006/bbrc.1997.7200

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The mRNA encoding an agouti related protein (ART) of unknown biochemical function was previously reported to be up-regulated in the hypothalamus of two genetically obese mouse strains. We have expressed human ART as a secreted protein in COS-7 cells, and show that recombinant ART is functionally active in inhibiting the binding of a radiolabeled alpha-melanocyte stimulating hormone (alpha-MSH) analog to the human melanocortin-3 (MC-3) and melanocortin-4 (MC-4) receptors, while it is not a potent inhibitor of the human melanocortin-5 (MC-5) receptor. ART is an antagonist of the human MC-S and MC-4 receptors as determined in functional assay. ART appears to be approximately 100-fold more potent than agouti with reference to the MC-3R and MC-4R binding affinity. These data suggest that ART may be a physiological regulator of feeding behavior. (C) 1997 Academic Press.

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页码：629 / 631

页数：3

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