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G蛋白信号调节 (RGS)蛋白是新近发现的能调节G蛋白功能的蛋白家族。RGS能通过加速鸟苷三磷酸 (GTP)水解抑制G蛋白信号 ,即其GTP酶活化蛋白 (GAP)功能。此外 ,RGS还能通过其RGS区域和非RGS区域产生非GAP功能。此类蛋白的组织分布特异 ,受到信号传递物质的调节并能在活细胞产生特定功能 ,也因此而成为新的药理和治疗靶点。以RGS蛋白为靶点的药物分为 5类 :增强内源性激动剂功能的药物 ;阻断外源性G蛋白偶联受体 (GPCR)激动剂脱敏的药物 ;增强外源性激动剂功能的药物 ;RGS蛋白效应器信号抑制剂 ;RGS激动剂。
The G protein signaling (RGS) protein is a newly discovered family of proteins that regulate the function of G proteins. RGS inhibits G-protein signaling by accelerating guanosine triphosphate (GTP) hydrolysis, ie its GTPase-activating protein (GAP) function. In addition, RGS can generate non-GAP capabilities through its RGS and non-RGS regions. Tissue distribution of such proteins specific, regulated by signaling substances and can produce specific functions in living cells, and therefore has become a new pharmacological and therapeutic targets. Drugs that target RGS proteins fall into five categories: drugs that enhance the function of endogenous agonists; drugs that block the desensitization of exogenous G protein-coupled receptor (GPCR) agonists; drugs that enhance exogenous agonists Functional Drugs; RGS Protein Effector Signal Inhibitors; RGS Agonists.