Pyruvate dehydrogenase kinases (PDKs) have recently emerged as an attractive target for
cancer therapy. Herein, we prepared a series of compounds derived from dichloroacetate …

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

In many types of cancers, pyruvate dehydrogenase kinase (PDK) is abnormally
overexpressed and has become a promising target for cancer therapy. However, few highly …

Pyruvate dehydrogenase kinases (PDKs) are promising therapeutic targets that have
received increasing attentions in cancer metabolism. In this paper, we report the synthesis …

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 …

Highlights•An overview of the structural information of PDKs.•The development of PDK
inhibitors as anticancer agents is described.•New thoughts in the quest for the designs of …

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

Pyruvate is irreversibly decarboxylated to acetyl coenzyme A by mitochondrial pyruvate
dehydrogenase complex (PDC). Decarboxylation of pyruvate is considered a crucial step in …

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