Pyruvate dehydrogenase kinase 4 (PDK4) activation is associated with metabolic diseases
including hyperglycemia, insulin resistance, allergies, and cancer. Structural modifications of …

Proliferating cancer cells are characterized by the Warburg effect, a metabolic alteration in
which ATP is generated from cytoplasmic glycolysis instead of oxidative phosphorylation …

Pyruvate dehydrogenase kinases (PDKs) are overexpressed in most cancer cells and are
responsible for aberrant glucose metabolism. We previously described bis (4-morpholinyl …

Warburg effect, a preference of aerobic glycolysis for energy production even in the
presence of adequate oxygen, is one of the most prominent distinctions of cancer cells from …

Herein, triphenylphosphonium cation moieties were incorporated into a
dichloroacetophenone derivative, leading to the discovery of novel mitochondria-targeted …

Dichloroacetophenone is a pyruvate dehydrogenase kinase 1 (PDK1) inhibitor with
suboptimal kinase selectivity. Herein, we report the synthesis and biological evaluation of a …

Among the different hallmarks of cancer, deregulation of cellular metabolism turned out to be
an essential mechanism in promoting cancer resistance and progression. The pyruvate …

Abstract Pyruvate dehydrogenase kinase 3 (PDK3) is a multifunctional enzyme that plays a
central role in the cancer metabolic switch by blocking pyruvate catabolism in the TCA cycle …

Most cancer cells exhibit a high rate of glycolysis and reduced capacity in mitochondrial
oxidative phosphorylation. The expression of pyruvate dehydrogenase kinases (PDKs) was …

Phosphorylation of pyruvate dehydrogenase by pyruvate dehydrogenase kinase 4 (PDK4) 4
inhibits its ability to induce a glycolytic shift. PDK4 expression is frequently upregulated in …