点击并释放：前药“按需”激活的生物正交方法。
Click and release: bioorthogonal approaches to "on-demand" activation of prodrugs.
机构信息
Laboratory of Anesthesia and Critical Care Medicine, Department of Anesthesiology, Translational Neuroscience Center, West China Hospital and State Key Laboratory of Biotherapy, Sichuan University, Chengdu, Sichuan 610041, China.
Department of Chemistry and Center for Diagnostics and Therapeutics, Georgia State University, Atlanta, Georgia 30303, USA.
出版信息
Chem Soc Rev. 2019 Feb 18;48(4):1077-1094. doi: 10.1039/c8cs00395e.
Prodrug approaches represent an excellent solution to certain pharmaceutical issues commonly encountered in the drug discovery and development process. Along this line, the chemistry needed for the bio-reversible derivatization of drug functional groups for on-demand release is critical. In recent years, "click and release" approaches have shown great promise in the design of prodrugs because of their bioorthogonality and controlled bond-cleavage, which help ensure prodrug stability during circulation and ready cleavage at the desired site of action. This review highlights recent developments of this research field and discusses issues yet to be addressed.
前药方法是解决药物发现和开发过程中某些常见药物问题的绝佳解决方案。沿着这条路线，对于按需释放的药物功能基团的生物可逆衍生化所需的化学是至关重要的。近年来，由于其生物正交性和可控的键断裂，“点击和释放”方法在前药设计中显示出巨大的潜力，这有助于确保前药在循环过程中的稳定性，并在所需的作用部位进行快速断裂。本文综述了该研究领域的最新进展，并讨论了仍待解决的问题。
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