Ontology highlight
ABSTRACT:
SUBMITTER: Masini T
PROVIDER: S-EPMC5553292 | biostudies-literature | 2016
REPOSITORIES: biostudies-literature
Journal of enzyme inhibition and medicinal chemistry 20160719 sup4
The last decade has witnessed the reawakening of cancer metabolism as a therapeutic target. In particular, inhibition of pyruvate dehydrogenase kinase (PDK) holds remarkable promise. Dichloroacetic acid (DCA), currently undergoing clinical trials, is a unique PDK inhibitor in which it binds to the allosteric pyruvate site of the enzyme. However, the safety of DCA as a drug is compromised by its neurotoxicity, whereas its usefulness as an investigative tool is limited by the high concentrations r ...[more]