Strosberg A D, Pietri-Rouxel F
Institut Cochin de Génétique Moléculaire, CNRS UPR 0415, Paris, France.
Trends Pharmacol Sci. 1996 Oct;17(10):373-81. doi: 10.1016/s0165-6147(96)80011-3.
The cloning, sequencing and expression in model systems of the previously unidentified beta 3-adrenoceptor recently led to an extensive functional characterization. Ligand binding and adenylate cyclase activation studies helped define a specific profile that is quite distinct from that of the beta 1- and beta 2-adrenoceptors, but strongly reminiscent of most of the 'atypical' beta-adrenoceptor-mediated responses reported in earlier pharmacological studies. More recently, a naturally occurring variation in the human beta 3-adrenoceptor has been correlated with hereditary obesity and with increased dynamic capacity to add on weight and develop non-insulin dependent diabetes in Western obese patients. Donny Strosberg and France Pietri-Rouxel describe how results now provide a consistent picture of an important role for the human beta 3-adrenoceptor in the regulation of lipid metabolism and as an obvious target for drugs to treat some forms of obesity and diabetes.
最近,对先前未被识别的β3肾上腺素能受体进行克隆、测序并在模型系统中表达,从而对其进行了广泛的功能特性研究。配体结合和腺苷酸环化酶激活研究有助于确定一种特定的特征,该特征与β1和β2肾上腺素能受体的特征截然不同,但与早期药理学研究中报道的大多数“非典型”β肾上腺素能受体介导的反应极为相似。最近,人类β3肾上腺素能受体的一种天然变异与遗传性肥胖以及西方肥胖患者体重增加和患非胰岛素依赖型糖尿病的动态能力增强有关。唐尼·斯特罗斯伯格和弗朗斯·皮埃特里 - 鲁塞尔描述了这些结果如何为人类β3肾上腺素能受体在脂质代谢调节中的重要作用提供了一个连贯的图景,以及如何成为治疗某些形式肥胖和糖尿病药物的明显靶点。