Department of Chemistry, 720 Clinic Drive, Purdue University, West Lafayette, Indiana 47907, USA.
Nat Rev Drug Discov. 2015 Mar;14(3):203-19. doi: 10.1038/nrd4519. Epub 2015 Feb 20.
Most cancer drugs are designed to interfere with one or more events in cell proliferation or survival. As healthy cells may also need to proliferate and avoid apoptosis, anticancer agents can be toxic to such cells. To minimize these toxicities, strategies have been developed wherein the therapeutic agent is targeted to tumour cells through conjugation to a tumour-cell-specific small-molecule ligand, thereby reducing delivery to normal cells and the associated collateral toxicity. This Review describes the major principles in the design of ligand-targeted drugs and provides an overview of ligand-drug conjugates and ligand-imaging-agent conjugates that are currently in development.
大多数癌症药物旨在干扰细胞增殖或存活的一个或多个事件。由于健康细胞也可能需要增殖并避免凋亡，因此抗癌药物可能对这些细胞有毒。为了最大程度地减少这些毒性，已经开发出了一些策略，其中治疗剂通过与肿瘤细胞特异性小分子配体缀合而靶向肿瘤细胞，从而减少向正常细胞的递送和相关的附带毒性。本综述描述了配体靶向药物设计的主要原则，并概述了目前正在开发的配体-药物偶联物和配体-成像剂偶联物。
