Furoates and thenoates inhibit pyruvate dehydrogenase kinase 2 allosterically by binding to its pyruvate regulatory site. [PDF]
, 2016 The last decade has witnessed the reawakening of cancer metabolism as a therapeutic target. In particular, inhibition of pyruvate dehydrogenase kinase (PDK) holds remarkable promise.
Tiziana Masini (2883941) +9 more
core +2 more sources
Protein phosphorylation in yeast mitochondria [PDF]
, 1987 We describe the identification and submitochondrial localization of four protein kinases and of their target proteins in derepressed yeast mitochondria. The activity of one of the kinases depends on the presence of cyclic AMP (cAMP).
Günter Müller +3 more
core +1 more source
Long-term regulation of pyruvate dehydrogenase complex. Evidence that kinase-activator protein (KAP) is free pyruvate dehydrogenase kinase [PDF]
Biochemical Journal, 1991 The kinase-activator protein (KAP) of pyruvate dehydrogenase complex (PDC) has been purified approx. 2250-fold from high-speed supernatants of mitochondrial extracts from the liver of 48 h-starved rats. Purified KAP demonstrates kinase activity towards both the E1 component of PDC and towards a synthetic peptide corresponding to the major ...
B S, Jones, S J, Yeaman
openaire +2 more sources
Effect of diet on linoleic acid desaturation and on some enzymes of carbohydrate metabolism
Journal of Lipid Research, 1970 The effect of diet on the desaturation of linoleic acid to gamma-linolenic acid by liver microsomal preparations, on blood glucose and insulin levels, and on activities of glucokinase, hexokinase, pyruvate kinase, and alpha-glycerophosphate dehydrogenase
I.N. De Gomez Dumm +2 more
doaj +1 more source
Reversing tozasertib resistance in glioma through inhibition of pyruvate dehydrogenase kinases
Molecular Oncology, 2022 Acquired resistance to conventional chemotherapeutic agents limits their effectiveness and can cause cancer treatment to fail. Because enzymes in the aurora kinase family are vital regulators of several mitotic events, we reasoned that targeting these ...
Esther P. Jane +6 more
doaj +1 more source
Refining the Role of Pyruvate Dehydrogenase Kinases in Glioblastoma Development
Cancers, 2022 Glioblastoma (GB) are the most frequent brain cancers. Aggressive growth and limited treatment options induce a median survival of 12–15 months. In addition to highly proliferative and invasive properties, GB cells show cancer-associated metabolic characteristics such as increased aerobic glycolysis. Pyruvate dehydrogenase (PDH) is a key enzyme complex
Claire M. Larrieu +11 more
openaire +5 more sources
Hyperosmotic stress induces PARP1‐mediated HPF1‐dependent mono(ADP‐ribosyl)ation
FEBS Letters, EarlyView.Sorbitol‐induced hyperosmotic stress rapidly induces reversible mono(ADP‐ribosyl)ation (MARylation) on PARP1 without the signs of genotoxic signaling. We show that PARP1 autoMARylation is HPF1 dependent and forms hydroxylamine‐resistant O‐glycosidic linkages.
Anna Georgina Kopasz +11 more
wiley +1 more source
N 6 -methyladenosine regulates glycolysis of cancer cells through PDK4
Nature Communications, 2020 Dysregulation of N6-Methyladenosine (m6A) is associated with cancer progression. Here, authors show that m6A methylation of pyruvate dehydrogenase kinase 4 (PDK4) positively regulates its mRNA stability and translation, and consequently affects ...
Zihan Li +7 more
doaj +1 more source
Key glycolytic enzyme activities of skeletal muscle are decreased under fed and fasted states in mice with knocked down levels of Shc proteins. [PDF]
PLoS ONE, 2015 Shc proteins interact with the insulin receptor, indicating a role in regulating glycolysis. To investigate this idea, the activities of key glycolytic regulatory enzymes and metabolites levels were measured in skeletal muscle from mice with low levels ...
Kevork Hagopian +4 more
doaj +1 more source
Lactic Acid Fermentation Is Required for NLRP3 Inflammasome Activation
Frontiers in Immunology, 2021 Activation of the Nod-like receptor 3 (NLRP3) inflammasome is important for activation of innate immune responses, but improper and excessive activation can cause inflammatory disease.
Hsin-Chung Lin +13 more
doaj +1 more source