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Cannabidiol Analogue CIAC001 for the Treatment of Morphine-Induced Addiction by Targeting PKM2.

Journal of Medicinal Chemistry, 2023
Opioid addiction is a chronically relapsing disorder that causes critical public health problems. Currently, there is a lack of effective drug treatment.
Sha Jin   +10 more
semanticscholar   +1 more source

Activators of PKM2 in Cancer Metabolism

Future Medicinal Chemistry, 2014
Pyruvate kinase converts phosphoenolpyruvate to pyruvate, catalyzing the rate-limiting step of glycolysis. The M1 isoenzyme of pyruvate kinase (PKM1) is found in adult tissues; whereas, PKM2 is a splicesome variant found in embryonic and cancer cells.
Kent J. Carpenter   +2 more
openaire   +2 more sources

Nuclear translocation of PKM2 mediates keratinocyte metabolic reprogramming in psoriasis

Experimental Dermatology, 2023
PKM2 mediates the Warburg effects and is crucial for tumorigenesis, but its role in hyperplastic skin disorders remains elusive. In this study, we investigated the function of PKM2 in psoriatic keratinocytes. We found that PKM2 expression and its nuclear
Luting Yang   +7 more
semanticscholar   +1 more source

Glycolytic enzyme PKM2 regulates cell senescence but not inflammation in the process of osteoarthritis

Acta Biochimica et Biophysica Sinica, 2023
Chondrocyte senescence is an important mechanism underlying osteoarthritis in the senile population and is characterized by reduced expressions of the extracellular matrix proteins.
Bohan Liu   +8 more
semanticscholar   +1 more source

Recent Advances on PKM2 Inhibitors and Activators in Cancer Applications.

Current Medicinal Chemistry, 2023
Metabolic reprogramming of cells, from the normal mode of glucose metabolism named glycolysis, is a pivotal characteristic of impending cancerous cells.
Peng Chen   +8 more
semanticscholar   +1 more source

PKM2 contributes to cancer metabolism

Cancer Letters, 2015
Reprogramming of cell metabolism is essential for tumorigenesis, and is regulated by a complex network, in which PKM2 plays a critical role. PKM2 exists as an inactive monomer, less active dimer and active tetramer. While dimeric PKM2 diverts glucose metabolism towards anabolism through aerobic glycolysis, tetrameric PKM2 promotes the flux of glucose ...
Damu Tang   +3 more
openaire   +3 more sources

PKM2, a potential target for regulating cancer

Gene, 2018
Aberrated glucose metabolism is a key future of cancer cells. Unlike normal cells, tumor cells favor glycolysis even in the presence of sufficient oxygen. Pyruvate kinase (PK), a key glucose metabolic enzyme, converts phosphoenolpyruvate (PEP) to pyruvate by transferring the high-energy phosphate group to adenosine diphosphate (ADP) to produce ...
Yu-huan Li   +6 more
openaire   +3 more sources

PKM2 functions as a histidine kinase to phosphorylate PGAM1 and increase glycolysis shunts in cancer

EMBO Journal
Phosphoglycerate mutase 1 (PGAM1) is a key node enzyme that diverts the metabolic reactions from glycolysis into its shunts to support macromolecule biosynthesis for rapid and sustainable cell proliferation.
Yang Wang   +18 more
semanticscholar   +1 more source

PKM2 Is Essential for Bladder Cancer Growth and Maintenance

Cancer Research, 2021
Abstract Pyruvate kinase M2 (PKM2) has been shown to promote tumorigenesis by facilitating the Warburg effect and enhancing the activities of oncoproteins. However, this paradigm has recently been challenged by studies in which the absence of PKM2 failed to inhibit and instead accelerated ...
Yong Xia   +7 more
openaire   +2 more sources

PKM2 as a protein kinase

Nature Reviews Molecular Cell Biology, 2012
Pyruvate kinase isoform M2 (PKM2) is a glycolytic enzyme that mediates the conversion of phosphoenolpyruvate (PEP) to pyruvate. It has been suggested that PKM2 may have additional enzymatic activities and localizes to the nucleus to regulate transcription. Here, the authors show that PKM2 can act as a kinase in the nucleus. They found that nuclear PKM2
openaire   +2 more sources

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