Yoshida T, Umekawa T
First Department of Internal Medicine, Kyoto Prefectural University of Medicine.
Nihon Rinsho. 1998 Jul;56(7):1871-5.
The beta 3-adrenoceptor plays a significant role in the control of lipolysis and thermogenesis in the brown adipose tissue of rodents and humans. In human beta 3-adrenoceptor, a Trp to Arg replacement has recently been discovered. This change which occurs at position 64, in the first coding exon, has been correlated with increased weight gain, difficulty in losing weight, insulin resistance syndrome, and worsened diabetic situation. Higher percentages of this mutation are observed in Pima Indians (over 30%) and Japanese (20%). The possible functional mechanism of Trp54Arg is reported using human HEK293 cell line stably expressing the wild type and the [Arg64] beta 3-adrenoceptor type. Beta 3-adrenoceptor agonists available for humans are been also developing. In this paper we describe these points up-to-date.
β3肾上腺素能受体在啮齿动物和人类棕色脂肪组织的脂肪分解和产热控制中发挥着重要作用。在人类β3肾上腺素能受体中，最近发现了色氨酸到精氨酸的替换。这种发生在第一个编码外显子第64位的变化与体重增加、减肥困难、胰岛素抵抗综合征以及糖尿病病情恶化有关。在皮马印第安人（超过30%）和日本人（20%）中观察到这种突变的比例更高。使用稳定表达野生型和[Arg64]β3肾上腺素能受体类型的人HEK293细胞系报道了Trp54Arg的可能功能机制。可供人类使用的β3肾上腺素能受体激动剂也在研发中。在本文中，我们将对这些要点进行最新描述。
