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促肾上腺皮质激素释放因子家族肽与促肾上腺皮质激素释放因子受体:它们在能量平衡调节中的作用。

The corticotropin-releasing factor family of peptides and CRF receptors: their roles in the regulation of energy balance.

作者信息

Richard Denis, Lin Qin, Timofeeva Elena

机构信息

D.B. Brown Chair on Obesity Research and Laval Hospital Research Center, Laval University, Quebec (Qué), Canada G1K 7P4.

出版信息

Eur J Pharmacol. 2002 Apr 12;440(2-3):189-97. doi: 10.1016/s0014-2999(02)01428-0.

Abstract

The corticotropin-releasing factor (CRF) system could play a significant role in the regulation of energy balance. This system, which includes CRF, CRF-related peptides and CRF receptors, is part of a huge network of cells connected to central and peripheral pathways modulating energy metabolism. CRF and CRF-related peptides, which elicit their effects through G-protein-coupled receptors known in mammals as CRF(1) receptor and CRF(2) receptor, are capable of strong anorectic and thermogenic effects. Also supporting a role for the CRF system in the regulation of energy balance are findings demonstrating alterations in this system in obese and food-deprived animals that concur to facilitate energy deposition. In recent years, great progress has been made in understanding the specific physiological roles of the CRF system. In that respect, the discovery of urocortins II and III, two endogenous ligands of the CRF(2) receptor, and the development of selective and long-acting antagonists for the CRF receptors, have led to a better comprehension of the role of the CRF system in the regulation of energy balance. Although there are still important unresolved issues in the field of CRF research, the progress made recently warrants investigations aimed at evaluating the CRF system as a potential target for anti-obesity drugs.

摘要

促肾上腺皮质激素释放因子(CRF)系统可能在能量平衡调节中发挥重要作用。该系统包括CRF、CRF相关肽和CRF受体,是与调节能量代谢的中枢和外周途径相连的庞大细胞网络的一部分。CRF和CRF相关肽通过哺乳动物中称为CRF(1)受体和CRF(2)受体的G蛋白偶联受体发挥作用,具有强大的厌食和产热作用。肥胖和食物缺乏动物中该系统的改变有助于能量沉积,这一发现也支持CRF系统在能量平衡调节中的作用。近年来,在理解CRF系统的特定生理作用方面取得了很大进展。在这方面,CRF(2)受体的两种内源性配体urocortins II和III的发现,以及CRF受体选择性长效拮抗剂的开发,使人们对CRF系统在能量平衡调节中的作用有了更好的理解。尽管CRF研究领域仍有重要的未解决问题,但最近取得的进展值得开展研究,以评估CRF系统作为抗肥胖药物潜在靶点的可能性。

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