Walther-Straub-Institute of Pharmacology and Toxicology, Ludwig-Maximilians University of Munich, Goethestr. 33, 80336 Munich, Germany.
Curr Opin Pharmacol. 2011 Apr;11(2):112-6. doi: 10.1016/j.coph.2010.11.003. Epub 2010 Dec 10.
G-protein-coupled receptors are appreciated as central components of neurohormonal signaling. Recently, it turned out that they may also play a role in mechanotransduction. The angiotensin II AT(1) receptor was the first G-protein-coupled receptor claimed to be a mechanosensor. In the meantime, several other G(q/11)-coupled receptors were found to be sensitive to mechanical stimuli. Furthermore, there is first evidence to support the concept that G(i/o)-coupled receptors are susceptible to mechanical stimulation as well. Mechanical receptor activation appears to be agonist-independent and is initiated by a conformational change of the receptor protein discernible from agonist-bound conformations. Mechanically induced receptor activation plays a physiological role for myogenic vasoconstriction and is involved in the pathogenesis of cardiac hypertrophy.
G 蛋白偶联受体被认为是神经激素信号的核心组成部分。最近，事实证明它们也可能在机械转导中发挥作用。血管紧张素 II AT(1)受体是第一个被认为是机械感受器的 G 蛋白偶联受体。与此同时，还发现了其他几种 G(q/11)-偶联受体对机械刺激敏感。此外，有初步证据支持 G(i/o)-偶联受体也易受机械刺激的概念。机械受体激活似乎与激动剂无关，并且由受体蛋白的构象变化引发，这种构象变化与与激动剂结合的构象不同。机械诱导的受体激活对于肌原性血管收缩具有生理作用，并参与心肌肥厚的发病机制。
