Ontology highlight
ABSTRACT:
SUBMITTER: Yang R
PROVIDER: S-EPMC6253843 | biostudies-literature | 2018 Nov
REPOSITORIES: biostudies-literature
MedChemComm 20180924 11
Targeting pyruvate dehydrogenase kinases (PDKs) reverses the Warburg effect, which could be a potential therapeutic target for anti-cancer drug discovery. In this paper, we identified 12 potential PDK inhibitors by virtual ligand screening of a chemical library, and then further verified them by an enzymatic assay, in which <b>6</b>, <b>7</b>, and <b>11</b> strongly inhibited the function of PDKs, with IC<sub>50</sub> values of 1.26, 0.62, and 0.41 μM against PDK1, respectively, and showed a sim ...[more]