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人源化抗体曲妥珠单抗对抗癌药物的非共价携带

Non-covalent carriage of anticancer agents by humanized antibody trastuzumab.

作者信息

Yadav Arpita, Sharma Sweta, Yadav Veejendra Kumar

机构信息

Department of Chemistry, University Institute of Engineering and Technology, Chhatrapati Shahuji Maharaj University, Kanpur, 208024, India.

Department of Chemistry, Indian Institute of Technology, Kanpur, 208016, India.

出版信息

J Mol Model. 2016 May;22(5):112. doi: 10.1007/s00894-016-2986-0. Epub 2016 Apr 25.

Abstract

This article explores the internalization and non-covalent carriage of small molecule anticancer agents like vinca alkaloids by humanized monoclonal antibody trastuzumab. Such carriage is marked by significant reduction in side effects and increased therapeutic value of these anticancer agents. This study is coherent with few clinical observations of enhanced efficiency of these anticancer agents when co-administered with therapeutic antibodies. This study will also serve as the foundation for screening a database of anticancer agents for possible compounds that may be co-delivered alongwith the antibody. Based on this study vincristine conformation inside antibody and its charge environment may be used as descriptors for screening purposes.

摘要

本文探讨了人源化单克隆抗体曲妥珠单抗对长春花生物碱等小分子抗癌药物的内化和非共价携带。这种携带的特点是这些抗癌药物的副作用显著降低,治疗价值增加。这项研究与这些抗癌药物与治疗性抗体联合使用时效率提高的一些临床观察结果相一致。该研究还将作为筛选抗癌药物数据库中可能与抗体共同递送的化合物的基础。基于这项研究,抗体内部长春新碱的构象及其电荷环境可作为筛选的描述符。

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