HER2 靶向治疗的进展：从单克隆抗体到癌症治疗中的双抑制剂发展。
Advances in HER2-Targeted Therapies: From monoclonal antibodies to dual inhibitors developments in cancer treatment.
发表日期：2024 Aug 09
作者：
Meduri Bhagyalalitha, Akshatha Handattu Shankaranarayana, Sethu Arun Kumar, Manisha Singh, Karthik G Pujar, Durgesh Bidye, Gurubasavaraj Veeranna Pujar
来源：
BIOORGANIC CHEMISTRY
摘要：
HER2 受体在某些人类癌症中过度表达，由于其与较低的生存率相关，在癌症研究中引起了极大的关注。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，这些抗体已被证明在癌症治疗中非常有益。像 Zanidatamab 这样的双特异性抗体和像 T-DM1 这样的抗体药物偶联物已经被开发出来，以克服与单一疗法相关的耐药性。拉帕替尼、来那替尼和吡咯替尼等小分子最初是为了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双靶向药物克服了与HER2靶向单一疗法相关的耐药性。这篇全面的综述涵盖了 HER2 的结构特征、HER 家族信号通路机制、有关 HER2 受体参与各种癌症的最新发现以及各种 HER2 靶向疗法。此信息提供了对不断发展的癌症治疗领域中 HER2 靶向策略的全面了解。版权所有 © 2024 Elsevier Inc. 保留所有权利。
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.Copyright © 2024 Elsevier Inc. All rights reserved.