Moffatt James D
Veterinary Basic Sciences, The Royal Veterinary College, Royal College Street, London, NW1 0TU, UK.
Naunyn Schmiedebergs Arch Pharmacol. 2007 Mar;375(1):1-9. doi: 10.1007/s00210-007-0139-9. Epub 2007 Feb 10.
Proteinase-activated receptors (PARs) are G-protein-coupled receptors that convert specific extracellular proteolytic activity into intracellular signals, and have been suggested to play diverse roles in the body. In this review, evidence for the roles of PARs in bladder contractility and inflammation are presented. The role of PARs in prostate cancer is also reviewed. The existing literature in this area can be difficult to interpret due to the many nonspecific actions of the pharmacological tools employed. Although there are reports that PAR activators can cause contraction of bladder smooth muscle, further pharmacological and molecular studies are required to define roles for these receptors in bladder contractility. While structural studies suggest that roles for PARs in bladder inflammation are likely, few functional investigations have been performed. The significance of the expression of PARs on sensory nerves innervating the bladder and changes in receptor expression in inflammatory disease models are fascinating areas for future research. Finally, it seems probable that PARs, particularly PAR1, may play important roles in the growth and metastasis of prostate cancers.
蛋白酶激活受体（PARs）是G蛋白偶联受体，可将特定的细胞外蛋白水解活性转化为细胞内信号，并被认为在体内发挥多种作用。在本综述中，介绍了PARs在膀胱收缩性和炎症中作用的证据。还综述了PARs在前列腺癌中的作用。由于所使用的药理学工具存在许多非特异性作用，该领域的现有文献可能难以解释。尽管有报道称PAR激活剂可引起膀胱平滑肌收缩，但仍需要进一步的药理学和分子研究来确定这些受体在膀胱收缩性中的作用。虽然结构研究表明PARs在膀胱炎症中可能起作用，但很少有功能研究。PARs在支配膀胱的感觉神经上的表达意义以及炎症疾病模型中受体表达的变化是未来研究的迷人领域。最后，PARs，尤其是PAR1，似乎可能在前列腺癌的生长和转移中起重要作用。
