蛋白激酶B
PI3K/AKT/mTOR通路
AKT2型
原癌基因蛋白质c-akt
医学
AKT3
AKT1型
癌症研究
磷酸化
信号转导
生物
细胞生物学
作者
Yu Guo,Yizhen Jin,Bingxue Qu,Yu Zhang,Jinxin Che,Xiaowu Dong
标识
DOI:10.1080/13543776.2021.1915291
摘要
Introduction: Akt is a widely known serine threonine kinase involved in a series of critical cellular pathways like cell survival and proliferation. With the development of small-molecule Akt inhibitors, new strategies such as covalent, peptide-based, and PROTAC (Proteolysis Targeting Chimera) strategies have also been used the design of Akt inhibitors. On the other hand, due to the specificity of the Akt pathway, the use of Akt modulators in combination therapy and immunotherapy has been disclosed in the past 5 years.Areas covered: This review focuses on the patent literature covering small-molecule inhibitors of Akt kinase and their applications from 2016-present.Expert opinion: Although Akt inhibitors' progress has been somewhat slow over the past five years, new strategies still provide new opportunities for the development of Akt inhibitors. Combination with Akt pathway inhibitors for tumor therapy has also been widely disclosed in patents in the last 5 years. Notably, combination strategies of Akt inhibitors and immunotherapy have started to emerge in recent years. While the clinical indications of Akt modulators should not be limited to anti-cancer, it is still worth trying the treatment of other diseases. Within the next years, current drug development around Akt inhibitors should be fascinating.
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