Advances of AKT pathway in human oncogenesis and as a target for anti-cancer drug discovery.
Advances of AKT pathway in human oncogenesis and as a target for anti-cancer drug discovery.
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DOI：
10.2174/156800908783497159
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发表时间：
2008-01
影响因子：
3
通讯作者：
G. Z. Cheng;Sungman Park;Shaokun Shu;Lili He;W. Kong;Weizhou Zhang;Z. Yuan;Lu‐Hai Wang;J. Cheng
中科院分区：
文献类型：
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作者：
G. Z. Cheng;Sungman Park;Shaokun Shu;Lili He;W. Kong;Weizhou Zhang;Z. Yuan;Lu‐Hai Wang;J. Cheng
AKT(也称为PKB)在正常细胞和肿瘤细胞的生长、运动和存活等多种细胞过程中发挥着核心作用。在肿瘤发生过程中，AKT通路在上皮间充质转化(EMT)和血管生成中也起着重要作用。AKT是细胞外(包括胰岛素、IGF-1和EGF等生长因子)和细胞内(如突变/激活的受体酪氨酸激酶、PTEN、RAS和Src)信号的重要转导节点。它受磷脂酰肌醇3-激酶正向调节，受磷酸酶PTEN抑制。PI3K/PTEN/AKT通路的失控是人类恶性肿瘤中最常见的改变通路之一。近年来，对AKT信号在人类肿瘤发生中的作用以及AKT通路小分子抑制物的研究取得了显著进展。在这里，我们将讨论AKT的调节和功能，以及针对AKT的抗癌药物开发。
AKT (also known as PKB) plays a central role in a variety of cellular processes including cell growth, motility and survival in both normal and tumor cells. The AKT pathway is also instrumental in epithelial mesenchymal transitions (EMT) and angiogenesis during tumorigenesis. AKT functions as a cardinal nodal point for transducing extracellular (growth factors including insulin, IGF-1 and EGF ) and intracellular (such as mutated/activated receptor tyrosine kinases, PTEN, Ras and Src) signals. It is positively regulated by phosphatidylinositol 3-kinase and inhibited by phosphatase PTEN. Deregulation of the PI3K/PTEN/AKT pathway is one of the most common altered pathways in human malignancy. In the past few years, significant advances have been made in the understanding of AKT signaling in human oncogenesis and the development of small molecule inhibitor of AKT pathway. Here, we will discuss the regulation and function of AKT as well as targeting AKT for anti-cancer drug discovery.