Jeong Jeongyun, Kang Dong Il, Lee Geun Taek, Kim Isaac Yi
Department of Urologic Oncology and Dean and Betty Gallo Prostate Cancer Center, The Cancer Institute of New Jersey, Robert Wood Johnson Medical School, New Brunswick, NJ, USA.
Korean J Urol. 2010 Aug;51(8):511-7. doi: 10.4111/kju.2010.51.8.511. Epub 2010 Aug 18.
The bone morphogenetic proteins (BMPs), as members of the transforming growth factor-beta (TGF-beta) superfamily, not only control bone formation, but also regulate multiple key steps during embryonic development and differentiation. Furthermore, BMPs play critical roles in maintaining the homeostasis of the cardiovascular, pulmonary, reproductive, urogenital, and nervous systems in adult life. Like all members of the TGF-beta superfamily, BMP signaling is mediated through a heteromeric complex of type I and type II transmembrane serine/threonine kinase receptors. The subsequent signal transduction cascade includes either the canonical Smad-dependent or non-canonical Smad-independent pathways. Reflecting the critical function of BMPs, BMP signaling is tightly regulated at multiple steps by various mechanisms including extracellular endogenous antagonists, neutralizing antibodies/extracellular soluble receptor domains, small molecule inhibitors, cytoplasmic inhibitory Smads, and transcriptional co-repressors. Recently, dorsomorphin, the first small molecule inhibitor of BMP signaling, was identified and suggested as a useful tool for dissecting the mechanisms of signaling pathways and for developing novel therapeutics for diverse human diseases that are related to the BMP signaling pathways. In this article, we discuss various mechanisms involved in regulating BMP signaling pathways and their implications for urology.
骨形态发生蛋白(BMPs)作为转化生长因子-β(TGF-β)超家族的成员,不仅控制骨形成,还在胚胎发育和分化过程中调节多个关键步骤。此外,BMPs在维持成年期心血管、肺、生殖、泌尿生殖和神经系统的稳态中发挥关键作用。与TGF-β超家族的所有成员一样,BMP信号通过I型和II型跨膜丝氨酸/苏氨酸激酶受体的异源复合物介导。随后的信号转导级联包括经典的Smad依赖性或非经典的Smad非依赖性途径。反映BMPs的关键功能,BMP信号在多个步骤中受到多种机制的严格调控,这些机制包括细胞外内源性拮抗剂、中和抗体/细胞外可溶性受体结构域、小分子抑制剂、细胞质抑制性Smads和转录共抑制因子。最近,发现了BMP信号的首个小分子抑制剂——多穗柯素,并认为它是剖析信号通路机制以及开发与BMP信号通路相关多种人类疾病新疗法的有用工具。在本文中,我们讨论了参与调节BMP信号通路的各种机制及其对泌尿外科的意义。