Ontology highlight
ABSTRACT:
SUBMITTER: Marz AM
PROVIDER: S-EPMC3624267 | biostudies-literature | 2013 Apr
REPOSITORIES: biostudies-literature
März Andreas M AM Fabian Anne-Katrin AK Kozany Christian C Bracher Andreas A Hausch Felix F
Molecular and cellular biology 20130128 7
The immunosuppressant and anticancer drug rapamycin works by inducing inhibitory protein complexes with the kinase mTOR, an important regulator of growth and proliferation. The obligatory accessory partner of rapamycin is believed to be FK506-binding protein 12 (FKBP12). Here we show that rapamycin complexes of larger FKBP family members can tightly bind to mTOR and potently inhibit its kinase activity. Cocrystal structures with FKBP51 and FKBP52 reveal the modified molecular binding mode of the ...[more]