蛋白激酶B
PI3K/AKT/mTOR通路
变构调节
小分子
医学
计算生物学
药理学
癌症研究
生物信息学
化学
生物
生物化学
信号转导
酶
作者
Pingqing Fu,Guo Yu,Lu Yang,Yi Xu,Na Liu,Xuejun Zhu,Xiaowu Dong,Jinxin Che
标识
DOI:10.1080/13543776.2023.2273895
摘要
Protein kinase B (Akt), an essential protein in the PI3K/Akt/mTOR signaling pathway, plays a crucial role in tumor progression. Over the past two years, different types of Akt modulators have continued to emerge in the patent literature.This review focuses on the patent literature covering small molecule inhibitors, peptides, PROTACs, and antisense nucleic acids targetingAkt from 2020 to present. Also, we discuss the outcomes of several clinical trials, combination strategies for different mechanisms, and the application of Akt regulators in other non-oncology indications.Our search for relevant information was conducted using various databases, including the European Patent Office, SciFinder, andPubMed, from 01.2020 to 04.2023.In recent years, some combination therapeutic strategies involvingAkt inhibitors have shown promising clinical outcomes. Future research can be directed toward developing new applications of Akt inhibitors, which may have implications for other diseases beyond cancer. New attempts suggest that targeting allosteric sites may be a potential solution to the problem of isoform selectivity.Furthermore, directly knocking out Akt protein by using the degraderssuggests a promising direction for future development.
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