Rapamycin-inspired macrocycles with new target specificity.
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ABSTRACT:
SUBMITTER: Guo Z
PROVIDER: S-EPMC6435255 | biostudies-literature | 2019 Mar
REPOSITORIES: biostudies-literature
Publications
Rapamycin-inspired macrocycles with new target specificity.
Guo Zufeng Z Hong Sam Y SY Wang Jingxin J Rehan Shahid S Liu Wukun W Peng Hanjing H Das Manisha M Li Wei W Bhat Shridhar S Peiffer Brandon B Ullman Brett R BR Tse Chung-Ming CM Tarmakova Zlatina Z Schiene-Fischer Cordelia C Fischer Gunter G Coe Imogen I Paavilainen Ville O VO Sun Zhaoli Z Liu Jun O JO
Nature chemistry 20181210 3
Rapamycin and FK506 are macrocyclic natural products with an extraordinary mode of action, in which they form binary complexes with FK506-binding protein (FKBP) through a shared FKBP-binding domain before forming ternary complexes with their respective targets, mechanistic target of rapamycin (mTOR) and calcineurin, respectively. Inspired by this, we sought to build a rapamycin-like macromolecule library to target new cellular proteins by replacing the effector domain of rapamycin with a combina ...[more]
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