Guduru Shiva Krishna Reddy, Arya Prabhat
Center for Drug Discovery , Department of Pharmacology and Chemical Biology , Baylor College of Medicine , One Baylor Plaza , Houston , Texas 77030 , USA . Email:
Department of Pharmacology and Chemical Biology , Baylor College of Medicine , One Baylor Plaza , Houston , Texas 77030 , USA.
Medchemcomm. 2017 Nov 22;9(1):27-43. doi: 10.1039/c7md00474e. eCollection 2018 Jan 1.
Over the years, rapamycin has attracted serious attention due to its remarkable biological properties and as a potent inhibitor of the mammalian target of rapamycin (mTOR) protein through its binding with FKBP-12. Several efficient strategies that utilize synthetic and biosynthetic approaches have been utilized to develop small molecule rapamycin analogs or for synthesizing hybrid compounds containing a partial rapamycin structure to improve pharmacokinetic properties. Herein, we report selected case studies related to the synthesis of rapamycin-derived compounds and hybrid molecules to explore their biological properties.
多年来,雷帕霉素因其卓越的生物学特性以及通过与FKBP - 12结合作为雷帕霉素哺乳动物靶标(mTOR)蛋白的有效抑制剂而备受关注。已经采用了几种利用合成和生物合成方法的有效策略来开发小分子雷帕霉素类似物或合成含有部分雷帕霉素结构的杂合化合物,以改善药代动力学性质。在此,我们报告与雷帕霉素衍生化合物和杂合分子合成相关的选定案例研究,以探索它们的生物学特性。