药物发现
药物开发
蛋白质降解
计算生物学
药品
生物信息学
疾病
小分子
药物重新定位
药物靶点
蛋白质组学
可药性
制药工业
医学
蛋白质组
生物
数据科学
作者
Haobin Li,Jinyun Dong,Maohua Cai,Zhiyuan Xu,Xiang-Dong Cheng,Jiang-Jiang Qin
标识
DOI:10.1186/s13045-021-01146-7
摘要
Targeting pathogenic proteins with small-molecule inhibitors (SMIs) has become a widely used strategy for treating malignant tumors. However, most intracellular proteins have been proven to be undruggable due to a lack of active sites, leading to a significant challenge in the design and development of SMIs. In recent years, the proteolysis-targeting chimeric technology and related emerging degradation technologies have provided additional approaches for targeting these undruggable proteins. These degradation technologies show a tendency of superiority over SMIs, including the rapid and continuous target consumption as well as the stronger pharmacological effects, being a hot topic in current research. This review mainly focuses on summarizing the development of protein degradation technologies in recent years. Their advantages, potential applications, and limitations are also discussed. We hope this review would shed light on the design, discovery, and clinical application of drugs associated with these degradation technologies.
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