泛素
癌症
癌症治疗
功能(生物学)
蛋白质水解
计算生物学
信号转导
泛素连接酶
生物
生物信息学
细胞生物学
生物化学
遗传学
基因
酶
作者
Moyang Lv,Weichao Hu,Shengwei Zhang,Lijiao He,Changjiang Hu,Shiming Yang
出处
期刊:Cancer Letters
[Elsevier BV]
日期:2022-04-30
卷期号:539: 215716-215716
被引量:10
标识
DOI:10.1016/j.canlet.2022.215716
摘要
Proteolysis-targeting chimeras (PROTACs) are small molecules that specifically link E3 ubiquitin ligases to proteins of interest to mediate targeted ubiquitination and degradation. PROTACs are advantageous since they can target undruggable proteins with multiple domains, particularly those with smooth surfaces that lack a common binding domain for small-molecule inhibitors (SMIs). This review provides an overview of PROTAC technology and third-generation PROTAC development. We focused on designing and executing the most recent clinical trials involving PROTACs in cancer therapy. Additionally, we summarized novel findings regarding the mechanisms and signaling pathways involved in cancer development, such as the scaffolding function of certain proteins ignored by traditional SMIs and several recognized oncoproteins that participate in novel signaling pathways. We also discussed strategies for enhancing PROTAC antitumor activity and specificity.
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