Almahariq Muayad, Mei Fang C, Cheng Xiaodong
Department of Pharmacology and Toxicology, The University of Texas Medical Branch, Galveston, TX 77555, USA.
Department of Integrative Biology and Pharmacology, Texas Therapeutics Institute, Brown Foundation Institute of Molecular Medicine, The University of Texas Health Science Center at Houston, Houston, TX 77030, USA.
Acta Biochim Biophys Sin (Shanghai). 2016 Jan;48(1):75-81. doi: 10.1093/abbs/gmv115. Epub 2015 Nov 2.
The pleiotropic second messenger adenosine 3',5'-cyclic monophosphate (cAMP) regulates a myriad of biological processes under both physiological and pathophysiological conditions. Exchange protein directly activated by cAMP 1 (EPAC1) mediates the intracellular functions of cAMP by acting as a guanine nucleotide exchange factor for the Ras-like Rap small GTPases. Recent studies suggest that EPAC1 plays important roles in immunomodulation, cancer cell migration/metastasis, and metabolism. These results, coupled with the successful development of EPAC-specific small molecule inhibitors, identify EPAC1 as a promising therapeutic target for cancer treatments.
多效性第二信使3',5'-环磷酸腺苷（cAMP）在生理和病理生理条件下调节无数生物过程。cAMP直接激活的交换蛋白1（EPAC1）通过充当Ras样Rap小GTP酶的鸟嘌呤核苷酸交换因子来介导cAMP的细胞内功能。最近的研究表明，EPAC1在免疫调节、癌细胞迁移/转移和代谢中发挥重要作用。这些结果，再加上EPAC特异性小分子抑制剂的成功开发，将EPAC1确定为癌症治疗的一个有前景的治疗靶点。
