Vetter Irina, Kym Philip R, Szallasi Arpad
Institute for Molecular Bioscience & School of Pharmacy; The University of Queensland ; Brisbane, Australia.
Centralized Lead Optimization; AbbVie ; Chicago, IL, USA.
Temperature (Austin). 2015 May 26;2(2):150-1. doi: 10.1080/23328940.2015.1047721. eCollection 2015 Apr-Jun.
This editorial is about the roles that TRP channels play in heat and cold sensation and body temperature regulation. These roles may be exploited for therapeutic purposes (indeed, drugs targeting TRPV1, TRPA1 and TRPM8 channels are currently undergoing clinical trials for indications that range from pain through chronic cough and overactive bladder to cancer) or, conversely, may limit drug development (for example, several TRPV1 antagonists were withdrawn from clinical trials due to the hyperthermic reaction that they caused). In the future, modulation of thermosensitive TRP channels may ultimately find application in the treatment not only of pain, but also itch, stroke, asthma, and metabolic disorders. Of the multitude of targets involved in temperature sensation and body temperature regulation, why TRP channels? And why now?
这篇社论探讨了瞬时受体电位（TRP）通道在热觉、冷觉及体温调节中所起的作用。这些作用可被用于治疗目的（事实上，靶向瞬时受体电位香草酸亚型1（TRPV1）、瞬时受体电位锚蛋白1（TRPA1）和瞬时受体电位M型8（TRPM8）通道的药物目前正在进行临床试验，其适应症范围从疼痛到慢性咳嗽、膀胱过度活动症乃至癌症），或者相反，可能会限制药物研发（例如，几种TRPV1拮抗剂因引发高热反应而被撤出临床试验）。未来，对热敏性TRP通道的调控最终可能不仅在疼痛治疗中得到应用，还会应用于瘙痒、中风、哮喘及代谢紊乱的治疗。在涉及温度感觉和体温调节的众多靶点中，为什么是TRP通道？又为什么是现在？
