鸟嘌呤核苷酸交换因子（GEFs）和GTP酶激活蛋白（GAPs）：小G蛋白调控中的关键要素。

GEFs and GAPs: critical elements in the control of small G proteins.

作者信息

Bos Johannes L, Rehmann Holger, Wittinghofer Alfred

机构信息

Department of Physiological Chemistry and Centre of Biomedical Genetics, UMC Utrecht Universiteitsweg 100, 3584 CG Utrecht, The Netherlands.

出版信息

Cell. 2007 Jun 1;129(5):865-77. doi: 10.1016/j.cell.2007.05.018.

DOI:10.1016/j.cell.2007.05.018

PMID:17540168

Abstract

Guanine nucleotide exchange factors (GEFs) and GTPase-activating proteins (GAPs) regulate the activity of small guanine nucleotide-binding (G) proteins to control cellular functions. In general, GEFs turn on signaling by catalyzing the exchange from G-protein-bound GDP to GTP, whereas GAPs terminate signaling by inducing GTP hydrolysis. GEFs and GAPs are multidomain proteins that are regulated by extracellular signals and localized cues that control cellular events in time and space. Recent evidence suggests that these proteins may be potential therapeutic targets for developing drugs to treat various diseases, including cancer.

摘要

鸟嘌呤核苷酸交换因子（GEFs）和GTP酶激活蛋白（GAPs）调节小的鸟嘌呤核苷酸结合（G）蛋白的活性，以控制细胞功能。一般来说，GEFs通过催化G蛋白结合的GDP与GTP的交换来开启信号传导，而GAPs则通过诱导GTP水解来终止信号传导。GEFs和GAPs是多结构域蛋白，受细胞外信号和局部线索的调节，这些信号和线索在时间和空间上控制细胞事件。最近的证据表明，这些蛋白可能是开发治疗包括癌症在内的各种疾病药物的潜在治疗靶点。