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Pyruvate kinase activators for treatment of pyruvate kinase deficiency. [PDF]
Hematology Am Soc Hematol Educ Program, 2023 Pyruvate kinase (PK) deficiency is a congenital hemolytic anemia with wide-ranging clinical symptoms and complications associated with significant morbidity and reduced health-related quality of life in both children and adults.
Grace RF.
europepmc +4 more sources
Pyruvate Kinase M2 and Cancer: The Role of PKM2 in Promoting Tumorigenesis
Frontiers in Oncology, 2020 Pyruvate kinase plays a pivotal role in regulating cell metabolism. The final and rate-limiting step of glycolysis is the conversion of Phosphoenolpyruvate (PEP) to Pyruvate, which is catalyzed by Pyruvate Kinase. There are four isomeric, tissue-specific
Kulsoom Zahra +4 more
doaj +2 more sources
Protein kinase function of pyruvate kinase M2 and cancer
Cancer Cell International, 2020 Pyruvate kinase is a terminal enzyme in the glycolytic pathway, where it catalyzes the conversion of phosphoenolpyruvate to pyruvate and production of ATP via substrate level phosphorylation.
Xun Chen, Shangwu Chen, Dongsheng Yu
doaj +2 more sources
Mitapivat, a novel pyruvate kinase activator, for the treatment of hereditary hemolytic anemias
Therapeutic Advances in Hematology, 2021 Mitapivat (AG-348) is a novel, first-in-class oral small molecule allosteric activator of the pyruvate kinase enzyme. Mitapivat has been shown to significantly upregulate both wild-type and numerous mutant forms of erythrocyte pyruvate kinase (PKR ...
Hanny Al-Samkari, Eduard J van Beers
exaly +2 more sources
Pyruvate Kinase Controls Signal Strength in the Insulin Secretory Pathway
Cell Metabolism, 2020 Pancreatic β-cells couple nutrient metabolism with appropriate insulin secretion. Here, we show that pyruvate kinase (PK), which converts ADP and phosphoenolpyruvate (PEP) into ATP and pyruvate, underlies β-cell sensing of both glycolytic and ...
Arnaldo H de Souza +2 more
exaly +2 more sources
Journal of Experimental Medicine, 2019 This study identifies a novel pathway through which PCa selectively metastasizes to bone. PCa cells produce exosomes that transfer pyruvate kinase M2 to BMSCs, which in turn produce CXCL12 that promotes PCa invasion and growth.
Kenneth J. Pienta +2 more
exaly +2 more sources
Cancer & Metabolism, 2019 Background Pancreatic ductal adenocarcinoma (PDAC) is an aggressive cancer with limited treatment options. Pyruvate kinase, especially the M2 isoform (PKM2), is highly expressed in PDAC cells, but its role in pancreatic cancer remains controversial.
Lei Yu +6 more
doaj +2 more sources
HBV-Induced Pyruvate Increases Lactylation of Pyruvate Kinase M2 (PKM2) at K206 to Promote Liver Fibrosis [PDF]
PathogensWe previously demonstrated that HBV promotes liver fibrosis through the enhanced production of pyruvate. Pyruvate kinase M2 (PKM2), a key enzyme in pyruvate metabolism, plays an important role in liver fibrogenesis. Recently, lactylation of PKM2 has been
Wenxian Wen +11 more
doaj +2 more sources
Mitapivat versus Placebo for Pyruvate Kinase Deficiency.
New England Journal of Medicine, 2022 BACKGROUND Pyruvate kinase deficiency is a rare, hereditary, chronic condition that is associated with hemolytic anemia. In a phase 2 study, mitapivat, an oral, first-in-class activator of erythrocyte pyruvate kinase, increased the hemoglobin level in ...
Hanny T. Al-Samkari +18 more
semanticscholar +1 more source