Department of Chemistry and Center for Diagnostics and Therapeutics, Georgia State University, Petit Science Center, Atlanta, Georgia, USA.
Med Res Rev. 2020 Nov;40(6):2682-2713. doi: 10.1002/med.21720. Epub 2020 Aug 16.
Smart drugs, such as antibody-drug conjugates, for targeted therapy rely on the ability to deliver a warhead to the desired location and to achieve activation at the same site. Thus, designing a smart drug often requires proper linker chemistry for tethering the warhead with a vehicle in such a way that either allows the active drug to retain its potency while being tethered or ensures release and thus activation at the desired location. Recent years have seen much progress in the design of new linker activation strategies. Herein, we review the recent development of chemical strategies used to link the warhead with a delivery vehicle for preferential cleavage at the desired sites.
智能药物，如抗体药物偶联物，用于靶向治疗依赖于将弹头递送到所需位置的能力，并在同一部位实现激活。因此，设计智能药物通常需要适当的连接子化学，以便将弹头与载体连接起来，使活性药物在连接时保持其效力，或者确保在所需位置释放和激活。近年来，新的连接子激活策略的设计取得了很大进展。本文综述了用于将弹头与递药载体连接的化学策略的最新进展，这些策略用于在所需部位优先进行裂解。
