[HTML][HTML] The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain

SR Edwards, TJ Wandless - Journal of Biological Chemistry, 2007 - ASBMB
Rapamycin is an immunosuppressive drug that binds simultaneously to the 12-kDa FK506-
and rapamycin-binding protein (FKBP12, or FKBP) and the FKBP-rapamycin binding (FRB)
domain of the mammalian target of rapamycin (mTOR) kinase. The resulting ternary complex
has been used to conditionally perturb protein function, and one such method involves
perturbation of a protein of interest through its mislocalization. We synthesized two
rapamycin derivatives that possess large substituents at the C-16 position within the FRB …