Zhang Youyan, Schmidt Robert J, Foxworthy Patricia, Emkey Renee, Oler Jennifer K, Large Thomas H, Wang He, Su Eric W, Mosior Marion K, Eacho Patrick I, Cao Guoqing
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA.
Biochem Biophys Res Commun. 2005 Aug 26;334(2):729-32. doi: 10.1016/j.bbrc.2005.06.141.
A G-protein coupled receptor to niacin (nicotinic acid) was identified recently but the physiological/pharmacological role of the receptor remains poorly defined. We present our studies to demonstrate that HM74A, but not HM74, binds niacin at high affinities and effectively mediates Gi signaling events in human embryonic kidney HEK293 cells as well as in 3T3L1 adipocytes expressing HM74A. Furthermore, HM74A, but not HM74, expressed in differentiated 3T3L1 adipocytes effectively mediated inhibition of lipolysis by niacin. Our results provided direct evidence indicating that HM74A, but not HM74, was sufficient to mediate anti-lipolytic effect of niacin in adipose tissue.
最近发现了一种与烟酸（烟碱酸）结合的G蛋白偶联受体，但该受体的生理/药理作用仍不清楚。我们展示了我们的研究，以证明HM74A而非HM74能以高亲和力结合烟酸，并在人胚肾HEK293细胞以及表达HM74A的3T3L1脂肪细胞中有效介导Gi信号转导事件。此外，在分化的3T3L1脂肪细胞中表达的HM74A而非HM74能有效介导烟酸对脂解的抑制作用。我们的结果提供了直接证据，表明HM74A而非HM74足以介导烟酸在脂肪组织中的抗脂解作用。
