Aug 10, 2021 · We determined that DCA reduced the abundance of PDK1 in breast (MDA-MB-231) and prostate (PC-3) cancer cells, while it suppressed both PDK1 and PDK2 in skeletal muscle cells (L6 myotubes).

PDK1 expression was significantly associated with metastasis, reduced chemosensitivity, and poor overall and disease-free survival. Silencing of PDK1 retarded lactate production, cell adhesion, migration, invasion, and angiogenesis, and consequently metastasis.

Sep 6, 2017 · In this sense, dichloroacetate (DCA), a pyruvate dehydrogenase kinase (PDK) inhibitor, augments usage of the glycolysis-produced pyruvate in the mitochondria increasing oxidative phosphorylation...

We show that the trifluoromethylpropanamide end of AZD7545 projects into the lipoyl-binding pocket of PDK1. This interaction results in inhibition of PDK1 and PDK3 activities by aborting kinase binding to the PDC scaffold.

Pyruvate dehydrogenase kinase 1 (PDK1) is a key factor in the connection between glycolysis and the tricarboxylic acid cycle. Restoring the mitochondrial OXPHOS function by inhibiting glycolysis through targeting PDK1 has become a hot spot for tumor therapy.

Aug 10, 2021 · We determined that DCA reduced the abundance of PDK1 in breast (MDA-MB-231) and prostate (PC-3) cancer cells, while it suppressed both PDK1 and PDK2 in skeletal muscle cells (L6 myotubes). The DCA-induced PDK1 suppression was partially dependent on hypoxia-inducible factor-1?

Aug 14, 2018 · Mitochondrial pyruvate dehydrogenase kinases (PDK 1-4) play a pivotal role in metabolic flexibility by inhibiting pyruvate dehydrogenase complex. We determined whether metabolic reprogramming, diverting metabolism from aerobic glycolysis back to OXPHOS, would inhibit platelet function.

Nov 6, 2024 · PDK1 activates glycolysis to enhance stemness in hypoxia. To further explore whether PDK1 acts as a crucial regulator of BCSC maintenance by modulating glycolysis, we evaluated PDK1-positive cancer cell characteristics using a mouse xenograft tumor model.

PDK1-catalyzed PDHA pSer 232 contributed to metabolic reprogramming in PMOP. PDHA pSer 232 level highly differs between normal and PMOP-conditioned osteoclasts. PDK1 deficiency and pharmacological PDK1 inhibition suppressed osteoclastogenesis. ICA alleviated PMOP by reversing PDK1-dependent metabolic reprogramming.

Nov 6, 2017 · Here, we show that pyruvate dehydrogenase kinase 1 (PDK1) is enriched in breast cancer stem cells (BCSCs), whereas depletion of PDK1 remarkably diminishes ALDH + subpopulations, decreases...