The duocarmycins belong to a class of agent that has fascinated scientists for over four decades. Their exquisite potency, unique mechanism of action, and efficacy in multidrug-resistant tumour models makes them attractive to medicinal chemists and drug hunters. However, despite great advances in fine-tuning biological activity through structure–activity relationship studies (SARS), no duocarmycin-based therapeutic has reached clinical approval. In this review, we provide an overview of the most promising strategies currently used and include both tumour-targeted prodrug approaches and antibody-directed technologies.

中文翻译：

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如何释放双癌霉素的潜力用于癌症治疗？

Duocarmycins 属于一类让科学家着迷已超过四十年的药剂。它们精湛的效力、独特的作用机制以及在耐多药肿瘤模型中的功效使它们对药物化学家和药物猎人具有吸引力。然而，尽管通过结构-活性关系研究 (SARS) 在微调生物活性方面取得了很大进展，但没有一种基于双癌霉素的疗法获得临床批准。在这篇综述中，我们概述了目前使用的最有希望的策略，包括肿瘤靶向前药方法和抗体导向技术。