Computer Aided Drug Design Laboratory, Department of Pharmaceutical Chemistry, JSS College of Pharmacy, JSS Academy of Higher Education and Research, Sri Shivarathreeshwara Nagara, Mysuru 570015 India.
Computer Aided Drug Design Laboratory, Department of Pharmaceutical Chemistry, JSS College of Pharmacy, JSS Academy of Higher Education and Research, Sri Shivarathreeshwara Nagara, Mysuru 570015 India.
Bioorg Chem. 2024 Oct;151:107695. doi: 10.1016/j.bioorg.2024.107695. Epub 2024 Aug 9.
HER2 receptors, overexpressed in certain human cancers, have drawn significant attention in cancer research due to their correlation with poor survival rates. Researchers have developed monoclonal antibodies like Trastuzumab and Pertuzumab against HER2 receptors, which have proven highly beneficial in cancer therapy. Bispecific antibodies like Zanidatamab and antibody-drug conjugates like T-DM1 have been developed to overcome the resistance associated with monotherapy. Small molecules such as Lapatinib, Neratinib, and Pyrotinib were initially developed for treating breast cancer. However, ongoing research is investigating their potential use in other types of cancer, often in combination with other medications. EGFR/HER2 dual-targeted drugs have overcome drug resistance associated with HER2-targeted monotherapy. This comprehensive review covers the structural characteristics of HER2, the HER family signaling pathway mechanism, recent findings regarding HER2 receptor involvement in various cancers, and diverse HER2-targeted therapies. This information provides a comprehensive understanding of HER2-targeted strategies in the evolving field of cancer treatment.
HER2 受体在某些人类癌症中过度表达，由于与生存率降低相关，因此在癌症研究中受到了极大关注。研究人员开发了针对 HER2 受体的单克隆抗体，如曲妥珠单抗和帕妥珠单抗，它们在癌症治疗中已被证明非常有效。双特异性抗体，如zanidatamab，和抗体药物偶联物，如 T-DM1，已被开发用于克服与单药治疗相关的耐药性。小分子药物，如拉帕替尼、奈拉替尼和吡咯替尼，最初是为治疗乳腺癌而开发的。然而，正在进行的研究正在调查它们在其他类型癌症中的潜在用途，通常与其他药物联合使用。EGFR/HER2 双重靶向药物克服了与 HER2 靶向单药治疗相关的耐药性。本综述全面介绍了 HER2 的结构特征、HER 家族信号通路机制、最近关于 HER2 受体在各种癌症中的作用的发现，以及各种 HER2 靶向治疗方法。这些信息为了解癌症治疗领域不断发展的 HER2 靶向策略提供了全面的认识。
