Src激酶抑制剂研究进展  

The progress of Src inhibitors

作　　者：王琴 刘力[1] 乐意[1,2] 鄢龙家 WANG Qin;LIU Li;LE Yi;YAN Long-jia(School of Pharmaceutical Sciences,Guizhou University,Guiyang 550025,China;Guizhou Engineering Laboratory for Synthetic Drugs,Guiyang 550025,China)

机构地区：[1]贵州大学药学院,贵州贵阳550025 [2]贵州省合成药物工程实验室,贵州贵阳550025

出　　处：《中国药物化学杂志》2021年第4期312-319,共8页Chinese Journal of Medicinal Chemistry

摘　　要：Src是一种非受体型酪氨酸蛋白激酶,它对维持机体正常生理功能具有重要作用。Src基因作为第一个被发现的原癌基因,其编码的癌蛋白——Src激酶在多种肿瘤的发生、发展、迁移和侵袭起着重要作用。在正常细胞和组织中Src激酶被精确调控,然而在多种肿瘤细胞中均有高表达。因此,以Src激酶作为抗肿瘤药物靶点的研究受到广泛关注。本文作者基于小分子抑制剂与Src激酶结合方式的不同(分为ATP竞争抑制剂、变构抑制剂和共价抑制剂),对近十年里小分子Src激酶抑制剂的研究进行综述。Coronaviruses(CoVs) are single-stranded positive-sense enveloped RNA viruses.Severe acute respiratory syndrome-coronavirus-2(SARS-CoV-2),which is the seventh coronavirus known to infect humans, causes a new coronavirus disease(COVID-19) outbreak since December 2019.The Main protease(Mpro) is a key enzyme for SARS-CoV-2 replication, which is encoded by the polypeptide and responsible for processing the polypeptide into functional proteins.This review focused on the status of various effective anti-SARS-CoV-2 chemotherapies targeting Mpro discovered since the outbreak of SARS-CoV-2 in the end of 2019.The peptidomimetic, non-peptidomimetic small molecule inhibitors, metal coupling(complexation) inhibitors of SARS-CoV-2 were summarised, and the structural features and binding modes of these inhibitors were described in details.

关 键 词：抗肿瘤 酪氨酸激酶 SRC激酶 小分子抑制剂 

分 类 号：R914[医药卫生—药物化学]