Tyrosine phosphorylation of mitochondrial pyruvate dehydrogenase kinase 1 is important for cancer metabolism

T Hitosugi, J Fan, TW Chung, K Lythgoe, X Wang, J Xie… - Molecular cell, 2011 - cell.com
Many tumor cells rely on aerobic glycolysis instead of oxidative phosphorylation for their
continued proliferation and survival. Myc and HIF-1 are believed to promote such a …

Pyruvate dehydrogenase kinase as a novel therapeutic target in oncology

G Sutendra, ED Michelakis - Frontiers in oncology, 2013 - frontiersin.org
Current drug development in oncology is non-selective as it typically focuses on pathways
essential for the survival of all dividing cells. The unique metabolic profile of cancer, which is …

Pyruvate dehydrogenase complex activity controls metabolic and malignant phenotype in cancer cells

T McFate, A Mohyeldin, H Lu, J Thakar… - Journal of Biological …, 2008 - ASBMB
High lactate generation and low glucose oxidation, despite normal oxygen conditions, are
commonly seen in cancer cells and tumors. Historically known as the Warburg effect, this …

Targeting pyruvate dehydrogenase kinase signaling in the development of effective cancer therapy

S Anwar, A Shamsi, T Mohammad, A Islam… - … et Biophysica Acta (BBA …, 2021 - Elsevier
Pyruvate is irreversibly decarboxylated to acetyl coenzyme A by mitochondrial pyruvate
dehydrogenase complex (PDC). Decarboxylation of pyruvate is considered a crucial step in …

JX06 selectively inhibits pyruvate dehydrogenase kinase PDK1 by a covalent cysteine modification

W Sun, Z Xie, Y Liu, D Zhao, Z Wu, D Zhang, H Lv… - Cancer research, 2015 - AACR
Pyruvate dehydrogenase kinase PDK1 is a metabolic enzyme responsible for switching
glucose metabolism from mitochondrial oxidation to aerobic glycolysis in cancer cells, a …

Metabolic flexibility in cancer: targeting the pyruvate dehydrogenase kinase: pyruvate dehydrogenase axis

BL Woolbright, G Rajendran, RA Harris… - Molecular cancer …, 2019 - AACR
Cancer cells use alterations of normal metabolic processes to sustain proliferation
indefinitely. Transcriptional and posttranscriptional control of the pyruvate dehydrogenase …

Induction of pyruvate dehydrogenase kinase-3 by hypoxia-inducible factor-1 promotes metabolic switch and drug resistance

CW Lu, SC Lin, KF Chen, YY Lai, SJ Tsai - Journal of Biological Chemistry, 2008 - ASBMB
The switch of cellular metabolism from mitochondrial respiration to glycolysis is the hallmark
of cancer cells and associated with tumor malignancy. However, the mechanism of this …

Mitochondrial activation by inhibition of PDKII suppresses HIF1a signaling and angiogenesis in cancer

G Sutendra, P Dromparis, A Kinnaird, TH Stenson… - Oncogene, 2013 - nature.com
Most solid tumors are characterized by a metabolic shift from glucose oxidation to glycolysis,
in part due to actively suppressed mitochondrial function, a state that favors resistance to …

Microenvironmental control of glucose metabolism in tumors by regulation of pyruvate dehydrogenase

T Golias, M Kery, S Radenkovic… - International journal of …, 2019 - Wiley Online Library
During malignant progression cancer cells undergo a series of changes, which promote
their survival, invasiveness and metastatic process. One of them is a change in glucose …

Tyr phosphorylation of PDP1 toggles recruitment between ACAT1 and SIRT3 to regulate the pyruvate dehydrogenase complex

J Fan, C Shan, HB Kang, S Elf, J Xie, M Tucker, TL Gu… - Molecular cell, 2014 - cell.com
Mitochondrial pyruvate dehydrogenase complex (PDC) is crucial for glucose homeostasis in
mammalian cells. The current understanding of PDC regulation involves inhibitory serine …