Amadesi Silvia, Bunnett Nigel
University of California San Francisco, 521 Parnassus Avenue, Room C317, San Francisco, California 94143-0660, USA.
Curr Opin Pharmacol. 2004 Dec;4(6):551-6. doi: 10.1016/j.coph.2004.08.004.
Serine proteases from the circulation, inflammatory cells, digestive glands and microorganisms can signal to cells by cleaving protease-activated receptors (PARs), a family of four G-protein-coupled receptors. Proteases cleave PARs at specific sites to expose tethered ligand domains that bind to and activate the cleaved receptors. Despite this irreversible mechanism of activation, PAR signaling is tightly regulated to prevent the uncontrolled stimulation of cells. Although PARs are found in all organ systems, protease signaling is of particular interest in the gastrointestinal tract, where proteases regulate neurotransmission, secretion, motility, epithelial permeability and intestinal inflammation, and can thus contribute to disease.
来自循环系统、炎症细胞、消化腺和微生物的丝氨酸蛋白酶可通过切割蛋白酶激活受体（PARs）向细胞发出信号，PARs是一个由四个G蛋白偶联受体组成的家族。蛋白酶在特定位点切割PARs，以暴露与切割后的受体结合并激活它的拴系配体结构域。尽管存在这种不可逆的激活机制，但PAR信号传导受到严格调控，以防止细胞受到不受控制的刺激。虽然PARs存在于所有器官系统中，但蛋白酶信号传导在胃肠道中特别受关注，在胃肠道中，蛋白酶调节神经传递、分泌、运动、上皮通透性和肠道炎症，因此可能导致疾病。
