Getting the message across: pathophysiology and signaling via receptors for polypeptide hormones and proteinases.
Getting the message across: pathophysiology and signaling via receptors for polypeptide hormones and proteinases.
复制标题
DOI：
10.25011/cim.v33i2.12352
复制
发表时间：
2010-04
期刊：
影响因子：
--
通讯作者：
M. Hollenberg
中科院分区：
文献类型：
--
作者：
M. Hollenberg
本文对蛋白酶在产生激素样细胞信号中的作用进行了个性化概述。还概述了意想不到的发现路径，该路径引导一名研究人员花费了四年的时间，从早期对催产素和加压素与其神经素结合蛋白相互作用的研究，到当前对蛋白酶激活受体 (PAR) G 蛋白偶联家族特有的系留配体激活机制的研究。重点不仅在于有趣的 PAR 受体家族，还在于蛋白酶激活信号转导途径的替代机制。还总结了 PAR 在从关节炎到结肠炎等炎症性疾病中可能发挥的潜在生理和病理生理作用。还讨论了将 PAR 作为药物靶点的治疗意义。
This article provides a personalized overview of the role of proteinases in generating hormone-like cell signals. Also outlined is the unexpected route of discovery that led one investigator over a four-decade time span, from early studies of the interactions of oxytocin and vasopressin with their neurophysin binding proteins to current studies of the tethered ligand activation mechanism that is unique for the G-protein-coupled family of proteinase-activated receptors (PARs). The focus is not only on the intriguing PAR receptor family, but also on alternative mechanisms whereby proteinases activate signal transduction pathways. Also summarized are the potential physiological and pathophysiological roles that PARs may play in the setting of inflammatory disorders ranging from arthritis to colitis. The therapeutic implications of considering PARs as drug targets are also discussed.