Fong T M, Mao C, MacNeil T, Kalyani R, Smith T, Weinberg D, Tota M R, Van der Ploeg L H
Merck Research Laboratories, Rahway, New Jersey 07065, USA.
Biochem Biophys Res Commun. 1997 Aug 28;237(3):629-31. doi: 10.1006/bbrc.1997.7200.
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-3 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.
先前有报道称，编码一种生化功能未知的刺鼠相关蛋白（ART）的信使核糖核酸（mRNA）在两种遗传性肥胖小鼠品系的下丘脑内表达上调。我们已在COS-7细胞中将人ART表达为一种分泌蛋白，并表明重组ART在抑制放射性标记的α-黑素细胞刺激素（α-MSH）类似物与人黑素皮质素-3（MC-3）和黑素皮质素-4（MC-4）受体结合方面具有功能活性，而它并非人黑素皮质素-5（MC-5）受体的有效抑制剂。在功能测定中确定，ART是人类MC-3和MC-4受体的拮抗剂。就MC-3R和MC-4R结合亲和力而言，ART的效力似乎比刺鼠肽强约100倍。这些数据表明，ART可能是进食行为的生理调节因子。
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