PDK1 (pyruvate dehydrogenase kinase isoform 1) is involved in the regulation of enzymatic activity of mammalian pyruvate dehydrogenase (PDH) that is a part of a mitochondrial multienzyme complex to catalyze the oxidative decarboxylation of pyruvate and is one of the major enzymes responsible for the regulation of homeostasis of carbohydrate fuels in mammals. PDK1 has been found to serve as an effective therapeutic target for inhibition of glioblastoma growth.