Mahabeer R, Bhoola K D
Department of Experimental and Clinical Pharmacology, Medical School, University of Natal, Congella, Durban, South Africa.
Pharmacol Ther. 2000 Oct;88(1):77-89. doi: 10.1016/s0163-7258(00)00080-2.
Recent evidence increasingly supports the view that kinins exercise an important regulatory control in inflammation and in the growth and proliferation of cancer cells. The induction of tissue kallikrein (TK) gene results in either increased or new expression of this protease, resulting in an increased capacity to form kinins. The cellular actions of kinins are initiated and controlled by kinin B1 and B2 receptors. This review collates in detail current knowledge on the molecular profile and status of TK (hKLK1, hKLK2, and hKLK3) and the kinin B1 and B2 receptor genes. The development of TK inhibitors, as well as kinin receptor antagonists, for use in immune-modulated disorders and in tumours may provide a new generation of drugs of therapeutic value.
最近的证据越来越支持这样一种观点，即激肽在炎症以及癌细胞的生长和增殖过程中发挥着重要的调节控制作用。组织激肽释放酶（TK）基因的诱导会导致这种蛋白酶的表达增加或出现新的表达，从而增强形成激肽的能力。激肽的细胞作用由激肽B1和B2受体启动和控制。本综述详细整理了关于TK（hKLK1、hKLK2和hKLK3）以及激肽B1和B2受体基因的分子特征和状态的当前知识。开发用于免疫调节疾病和肿瘤的TK抑制剂以及激肽受体拮抗剂可能会提供具有治疗价值的新一代药物。
