Akt抑制剂的研究进展  

Advances in Akt inhibitors

作　　者：朱墨 郭长彬[1] ZHU Mo;GUO Chang-bin(Department of Chemistry,Beijing 100048,China)

机构地区：[1]首都师范大学化学系,北京100048

出　　处：《中国药物化学杂志》2021年第11期921-928,共8页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金项目(30873140);科技创新服务能力建设-基本科研项目(科研类)(025185305000/208)。

摘　　要：蛋白激酶B(Akt)是一种丝氨酸/苏氨酸蛋白激酶,属于AGC激酶家族成员,作为磷脂酰肌醇-3激酶(PI3K)的下游靶点,通过磷酸化其下游一系列底物来影响细胞的生长、代谢、凋亡等重要的生命活动。Akt的活性失调或过度表达现象见于多种恶性肿瘤疾病,可导致肿瘤的发生、转移以及耐药性的产生。研究表明,Akt是靶向抗肿瘤药物研发的重要靶标,Akt抑制剂可有效抑制肿瘤的生长。本文综述了Akt抑制剂的最新研究进展,并展望和讨论了临床前研究中有前景的新型Akt抑制剂。Akt is a serine/threonine kinase, belonging to the AGC kinase family.As a downstream target of phosphatidylinositol-3 kinase(PI3 K),by phosphorylating a series of downstream substrates, Akt affects cell growth, metabolism, apoptosis and other important life activities.According to the research results, the excessive activation of Akt is exhibited in prostate cancer, pancreatic cancer, bladder cancer, ovarian cancer, and breast cancer.The results of epidemiological studies indicate that Akt is an important target for the development of anti-tumor drugs, and Akt inhibitors can effectively inhibit the growth of tumors.This review summarizes and discusses the synthetic methods of dulutvir reported in the literature, in order to provide some reference for the further improvement of the new synthetic process of dulutvir.

关 键 词：Akt抑制剂 PH结构域抑制剂 ATP竞争性抑制剂 变构抑制剂 抗肿瘤靶向药物 

分 类 号：R914[医药卫生—药物化学]