Ontology highlight
ABSTRACT:
SUBMITTER: Dite TA
PROVIDER: S-EPMC5995511 | biostudies-literature | 2018 Jun
REPOSITORIES: biostudies-literature
Dite Toby A TA Langendorf Christopher G CG Hoque Ashfaqul A Galic Sandra S Rebello Richard J RJ Ovens Ashley J AJ Lindqvist Lisa M LM Ngoei Kevin R W KRW Ling Naomi X Y NXY Furic Luc L Kemp Bruce E BE Scott John W JW Oakhill Jonathan S JS
The Journal of biological chemistry 20180425 23
Inhibition of the metabolic regulator AMP-activated protein kinase (AMPK) is increasingly being investigated for its therapeutic potential in diseases where AMPK hyperactivity results in poor prognoses, as in established cancers and neurodegeneration. However, AMPK-inhibitory tool compounds are largely limited to compound C, which has a poor selectivity profile. Here we identify the pyrimidine derivative SBI-0206965 as a direct AMPK inhibitor. SBI-0206965 inhibits AMPK with 40-fold greater poten ...[more]