Division of Anti-aging Medicine, Center for Molecular Medicine, Jichi Medical University, Shimotsuke, Tochigi, Japan.
Department of Internal Medicine, University of Texas Southwestern Medical Center, Dallas, TX, USA.
Nat Rev Nephrol. 2019 Jan;15(1):27-44. doi: 10.1038/s41581-018-0078-3.
The Klotho proteins, αKlotho and βKlotho, are essential components of endocrine fibroblast growth factor (FGF) receptor complexes, as they are required for the high-affinity binding of FGF19, FGF21 and FGF23 to their cognate FGF receptors (FGFRs). Collectively, these proteins form a unique endocrine system that governs multiple metabolic processes in mammals. FGF19 is a satiety hormone that is secreted from the intestine on ingestion of food and binds the βKlotho-FGFR4 complex in hepatocytes to promote metabolic responses to feeding. By contrast, under fasting conditions, the liver secretes the starvation hormone FGF21, which induces metabolic responses to fasting and stress responses through the activation of the hypothalamus-pituitary-adrenal axis and the sympathetic nervous system following binding to the βKlotho-FGFR1c complex in adipocytes and the suprachiasmatic nucleus, respectively. Finally, FGF23 is secreted by osteocytes in response to phosphate intake and binds to αKlotho-FGFR complexes, which are expressed most abundantly in renal tubules, to regulate mineral metabolism. Growing evidence suggests that the FGF-Klotho endocrine system also has a crucial role in the pathophysiology of ageing-related disorders, including diabetes, cancer, arteriosclerosis and chronic kidney disease. Therefore, targeting the FGF-Klotho endocrine axes might have therapeutic benefit in multiple systems; investigation of the crystal structures of FGF-Klotho-FGFR complexes is paving the way for the development of drugs that can regulate these axes.
Klotho 蛋白,包括 αKlotho 和 βKlotho,是内分泌成纤维细胞生长因子 (FGF) 受体复合物的必需组成部分,因为它们是 FGF19、FGF21 和 FGF23 与其同源 FGF 受体 (FGFR) 高亲和力结合所必需的。这些蛋白共同构成了一个独特的内分泌系统,调节哺乳动物的多种代谢过程。FGF19 是一种饱腹感激素,在进食时从肠道分泌,与肝细胞中的 βKlotho-FGFR4 复合物结合,促进对进食的代谢反应。相比之下,在禁食状态下,肝脏分泌饥饿激素 FGF21,它通过与脂肪细胞中的 βKlotho-FGFR1c 复合物和视交叉上核结合,激活下丘脑-垂体-肾上腺轴和交感神经系统,从而诱导对禁食和应激的代谢反应。最后,成骨细胞响应磷酸盐摄入分泌 FGF23,并与 FGFR 复合物结合,该复合物在肾脏小管中表达最丰富,从而调节矿物质代谢。越来越多的证据表明,FGF-Klotho 内分泌系统在与衰老相关的疾病的病理生理学中也起着至关重要的作用,包括糖尿病、癌症、动脉硬化和慢性肾病。因此,针对 FGF-Klotho 内分泌轴可能对多个系统具有治疗益处;对 FGF-Klotho-FGFR 复合物的晶体结构的研究为开发可调节这些轴的药物铺平了道路。