癌症治疗中靶向蛋白激酶A：最新进展
Targeting protein kinase A in cancer therapy: an update.
作者信息
Sapio Luigi, Di Maiolo Francesca, Illiano Michela, Esposito Antonietta, Chiosi Emilio, Spina Annamaria, Naviglio Silvio
机构信息
Department of Biochemistry, Biophysics and General Pathology. Second University of Naples, Medical School, Italy.
出版信息
EXCLI J. 2014 Aug 18;13:843-55. eCollection 2014.
Protein Kinase A (PKA) is a well known member of the serine-threonin protein kinase superfamily. PKA, also known as cAMP-dependent protein kinase, is a multi-unit protein kinase that mediates signal transduction of G-protein coupled receptors through its activation upon cAMP binding. The widespread expression of PKA subunit genes, and the myriad of mechanisms by which cAMP is regulated within a cell suggest that PKA signaling is one of extreme importance to cellular function. It is involved in the control of a wide variety of cellular processes from metabolism to ion channel activation, cell growth and differentiation, gene expression and apoptosis. Importantly, since it has been implicated in the initiation and progression of many tumors, PKA has been proposed as a novel biomarker for cancer detection, and as a potential molecular target for cancer therapy. Here, we highlight some features of cAMP/PKA signaling that are relevant to cancer biology and present an update on targeting PKA in cancer therapy.
蛋白激酶A（PKA）是丝氨酸 - 苏氨酸蛋白激酶超家族中一个广为人知的成员。PKA，也被称为环磷酸腺苷（cAMP）依赖性蛋白激酶，是一种多亚基蛋白激酶，它通过在结合cAMP后被激活来介导G蛋白偶联受体的信号转导。PKA亚基基因的广泛表达以及细胞内调节cAMP的众多机制表明，PKA信号传导对细胞功能极为重要。它参与控制从代谢到离子通道激活、细胞生长和分化、基因表达及细胞凋亡等各种各样的细胞过程。重要的是，由于PKA与许多肿瘤的发生和发展有关，它已被提议作为癌症检测的新型生物标志物以及癌症治疗的潜在分子靶点。在此，我们着重介绍一些与癌症生物学相关的cAMP/PKA信号传导特征，并呈现癌症治疗中靶向PKA的最新进展。
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