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Monoclonal Antibodies, Small Molecule Inhibitors and Antibody-drug Conjugates as HER2 Inhibitors
Current Medicinal Chemistry ( IF 3.5 ) Pub Date : 2021-05-01 , DOI: 10.2174/0929867327666200908112847
Xiu-Fang Li 1 , Chen-Fu Liu 2 , Guo-Wu Rao 1
Affiliation  

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.



中文翻译:

作为 HER2 抑制剂的单克隆抗体、小分子抑制剂和抗体药物偶联物

在多种癌症中发现了人类表皮生长因子受体 (HER)-2 的过度表达,这通常预示着不良的临床结果。因此,HER2 是一个有吸引力的治疗靶点。本文综述了近年来HER2靶向抑制剂的研究进展。优秀的评论是可用的,因此我们专注于不同类型抑制剂的开发、作用机制和构效关系,包括单克隆抗体、小分子抑制剂和抗体药物偶联物 (ADC)。此外,还比较了它们之间的差异。

更新日期:2021-06-08
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