As a powerful tool to advance drug discovery, molecular imaging may provide new insights into the process of drug effect and therapy at cellular and molecular levels. When compared with other detection methods, fluorescence-based strategies are highly attractive and can be used to illuminate pathways of drugs’ transport, with multi-color capacity, high specificity and good sensitivity. The conjugates of fluorescent molecules and therapeutic agents create exciting avenues for real-time monitoring of drug delivery and distribution, both in vitro and in vivo. In this short review, we discuss recent developments of small molecule-based fluorophore-drug conjugates, including non-cleavable and cleavable ones, that are capable of visualizing drug delivery.

作为促进药物发现的有力工具，分子成像可以在细胞和分子水平上为药物作用和治疗过程提供新见解。与其他检测方法相比，基于荧光的策略具有很高的吸引力，可用于阐明药物的运输途径，具有多色能力，高特异性和良好的灵敏度。荧光分子和治疗剂的结合物为体外和体内实时监测药物的输送和分配创造了令人兴奋的途径。在这篇简短的综述中，我们讨论了能够可视化药物传递的基于小分子的荧光团-药物偶联物的最新进展，包括不可裂解和可裂解的偶联物。