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 …

Glycolysis, The Sweet Appetite of the Tumour Microenvironment

Z Kooshan, L Cárdenas-Piedra, J Clements, J Batra - Cancer Letters, 2024 - Elsevier
Cancer cells display an altered metabolic phenotype, characterised by increased glycolysis
and lactate production, even in the presence of sufficient oxygen-a phenomenon known as …

Epigallocatechin gallate circumvents drug‐induced resistance in non‐small‐cell lung cancer by modulating glucose metabolism and AMPK/AKT/MAPK axis

Y Zhou, S Huang, Y Guo, M Ran, W Shan… - Phytotherapy …, 2023 - Wiley Online Library
Upon prolonged use of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors
(TKIs) in non‐small‐cell lung cancer (NSCLC), acquired drug resistance inevitably occurs …

Combined inhibition of pyruvate dehydrogenase kinase 1 and lactate dehydrogenase a induces metabolic and signaling reprogramming and enhances lung …

Y Zhou, Y Guo, M Ran, W Shan, C Granchi… - Cancer Letters, 2023 - Elsevier
Lung adenocarcinoma (LUAD) is one of the most prevalent and aggressive types of lung
cancer. Metabolic reprogramming plays a critical role in the development and progression of …

Aberrant upregulation of PDK1 in ovarian cancer cells impairs CD8+ T cell function and survival through elevation of PD-L1

JJ Wang, MK Siu, YX Jiang, TH Leung, DW Chan… - …, 2019 - Taylor & Francis
Blockade of the programmed cell death 1 (PD-1)/PD-1 ligand-1 (PD-L1) pathway has been
exploited therapeutically in many cancer types. Upregulation of PD-L1 in tumor cells …

Dichloroacetophenone biphenylsulfone ethers as anticancer pyruvate dehydrogenase kinase inhibitors in non-small cell lung cancer models

Y Guo, Y Zhou, P Wu, M Ran, N Xu, W Shan… - Chemico-Biological …, 2023 - Elsevier
Abstract Pyruvate dehydrogenase kinase 1 (PDK1) is an important metabolic enzyme which
is often overexpressed in many types of cancers, including non-small-cell lung cancers …

[HTML][HTML] The oncogenic and prognostic role of PDK1 in the progression and metastasis of ovarian cancer

S Yao, W Shang, L Huang, R Xu, M Wu… - Journal of Cancer, 2021 - ncbi.nlm.nih.gov
Ovarian cancer (OC) is the most lethal of gynecological tumors in women. Tumor
metabolism has become a new opportunity in the treatment of tumors. Pyruvate …

Inhibition of pyruvate dehydrogenase kinase 1 enhances the anti-cancer effect of EGFR tyrosine kinase inhibitors in non-small cell lung cancer

Z Yang, SL Zhang, X Hu, KY Tam - European Journal of Pharmacology, 2018 - Elsevier
Although epidermal growth factor receptor (EGFR) inhibitors have been used to treat non-
small cell lung cancer (NSCLC) for decades with great success in patients with EGFR …

Recent advances in pyruvate dehydrogenase kinase inhibitors: Structures, inhibitory mechanisms and biological activities

Y Li, Z Xie, X Lei, X Yang, S Huang, W Yuan, X Deng… - Bioorganic …, 2024 - Elsevier
Metabolism is reprogrammed in a variety of cancer cells to ensure their rapid proliferation.
Cancer cells prefer to utilize glycolysis to produce energy as well as to provide large …

Synthesis, biological evaluation and structure-activity relationship of novel dichloroacetophenones targeting pyruvate dehydrogenase kinases with potent anticancer …

B Xu, ZP Wang, Q Liu, X Yang, X Li, D Huang… - European Journal of …, 2021 - Elsevier
Pyruvate dehydrogenase kinases (PDKs) are promising therapeutic targets that have
received increasing attentions in cancer metabolism. In this paper, we report the synthesis …