College of Pharmaceutical Science, Institute of Drug Development & Chemical Biology, Zhejiang University of Technology, Hangzhou 310014, China.
School of Pharmaceutical Sciences, Gannan Medical University, Ganzhou 341000, China.
Curr Med Chem. 2021;28(17):3339-3360. doi: 10.2174/0929867327666200908112847.
Overexpression of human epidermal growth factor receptor (HER)-2 is found in a variety of cancers, often portending poor clinical outcomes. Therefore, HER2 is an attractive target for treatment. This review describes the research progress of HER2 targeted inhibitors in recent years. Excellent reviews are available, so we focus on the development, mechanisms of action, and structure-activity relationships of different types of inhibitors, including monoclonal antibodies, small molecule inhibitors, and antibody-drug conjugates (ADCs). In addition, the differences among them are compared.
人表皮生长因子受体 2（HER2）的过表达存在于多种癌症中，常预示着不良的临床结局。因此，HER2 是治疗的一个有吸引力的靶点。本文描述了近年来 HER2 靶向抑制剂的研究进展。有很好的综述可供参考，因此我们重点介绍不同类型抑制剂（包括单克隆抗体、小分子抑制剂和抗体药物偶联物（ADC））的开发、作用机制和构效关系。此外，还比较了它们之间的差异。
