信号通路图
AKT
Akt又称PKB，即蛋白激酶B，是一种丝氨酸/苏氨酸蛋白激酶，参与了多个细胞过程，包括糖代谢，细胞增殖，凋亡转录以及细胞迁移。该家族主要有三个成 员：AKT1，AKT2和AKT3。其中，Akt1通过抑制细胞凋亡过程参与了细胞生存途径，Akt1酶也能诱导蛋白质的合成途径，因此是一个重要的信号 蛋白介导组织的生长。因为它可以阻止细胞凋亡，从而促进细胞的存活，AKT1参与了在许多类型的癌症发生。AKT2是胰岛素信号转导通路中的一个重要信号 分子，而AKT3则是主要表达在脑部。它的激活机制是：PI3K可以被G蛋白偶联受体或者受体酪氨酸激酶激活，随后激活的PI3K可以把PIP2磷酸化从 而形成PIP3。PIP3可以募集AKT将其正确定位在膜上，然后AKT可以被PDPK1和 mTORC2 磷酸化而被激活，并经一步参与接下来的各种功能~
下面是主要地抑制剂
A-674563
A-674563 is a potent selective protein kinase B/Akt inhibitor with an IC50 of 14 nM.
AT7867
AT7867 is a potent and oral AKT and p70 S6 kinase inhibitor with an IC50 of 17 nM.
CCT128930
CCT128930 is a novel potent ATP-competitive, AKT inhibitor with an IC50 of 6 nM.
GSK690693
GSK690693 is a pan-Akt kinase inhibitor, IC50 of Akt 1, 2, and 3 at 2, 13, and 9 nM respectively.
MK-2206
MK-2206 is a highly selective, potent non-ATP competitive allosteric Akt inhibitor with IC50 of 5.3 nM,12 nM, 65 nM for Akt1, Akt2 and Akt3 respectively.
Palomid 529 (P529)
Palomid 529 (P529) is a novel potent antitumour PI3K/Akt/mTOR inhibitor with a GI50 of <35 μM in the NCI-60 cell lines panel.
Perifosine
Perifosine is a novel Akt and PI3K inhibitor with IC50 of median 4.7 ?M.
PHT-427
PHT-427 is a Novel Akt/phosphatidylinositide-dependent protein kinase 1 pleckstrin homology domain inhibitor with an IC50 of 6.3 μM for AKT inhibition in Panc-1 cells.
Triciribine
Triciribine is a synthetic tricyclic nucleoside which acts as a specific inhibitor of the Akt signaling pathway.
Triciribine phosphate (NSC-280594)
Triciribine phosphate (NSC-280594) is a novel potent, small-molecule Akt inhibitor.
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