Recent advances in the design of choline kinase α inhibitors and the molecular basis of their inhibition
Sign Up to like & getrecommendations! Published in 2020 at "Medicinal Research Reviews"
DOI: 10.1002/med.21746
Abstract: Upregulated choline metabolism, characterized by an increase in phosphocholine (PCho), is a hallmark of oncogenesis and tumor progression. Choline kinase (ChoK), the enzyme responsible for PCho synthesis, has consequently become a promising drug target for… read more here.
Keywords: chok inhibitors; molecular basis; recent advances; choline kinase ... See more keywords
Metabolic changes in glioblastomas in response to choline kinase inhibition: In vivo MRS in rodent models
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DOI: 10.1002/nbm.4855
Abstract: Changes in glioblastoma (GBM) metabolism was investigated in response to JAS239, a choline kinase inhibitor, using MRS. In addition to the inhibition of phosphocholine synthesis, we investigated changes in other key metabolic pathways associated with… read more here.
Keywords: reduction; inhibition; response; choline kinase ... See more keywords
Choline kinase alpha 2 acts as a protein kinase to promote lipolysis of lipid droplets.
Sign Up to like & getrecommendations! Published in 2021 at "Molecular cell"
DOI: 10.1016/j.molcel.2021.05.005
Abstract: Lipid droplets are important for cancer cell growth and survival. However, the mechanism underlying the initiation of lipid droplet lipolysis is not well understood. We demonstrate here that glucose deprivation induces the binding of choline… read more here.
Keywords: choline kinase; chk; lipid droplets; lipolysis ... See more keywords
Choline kinase inhibitors EB-3D and EB-3P interferes with lipid homeostasis in HepG2 cells
Sign Up to like & getrecommendations! Published in 2019 at "Scientific Reports"
DOI: 10.1038/s41598-019-40885-z
Abstract: A full understanding of the molecular mechanism of action of choline kinase α (ChoKα) inhibitors at the cell level is essential for developing therapeutic and preventive approaches for cancer. The aim of the present study… read more here.
Keywords: homeostasis; choline; kinase; choline kinase ... See more keywords
MALAT1 as a Regulator of the Androgen-Dependent Choline Kinase A Gene in the Metabolic Rewiring of Prostate Cancer
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DOI: 10.3390/cancers14122902
Abstract: Simple Summary Despite the rapid advance in cancer therapies, treatment-resistant relapse remains a significant challenge in cancer treatment. Acquired resistance arises during or after treatment administration, and is usually the main contributor to relapse. For… read more here.
Keywords: choline kinase; prostate cancer; androgen; malat1 ... See more keywords
Choline Kinase: An Unexpected Journey for a Precision Medicine Strategy in Human Diseases
Sign Up to like & getrecommendations! Published in 2021 at "Pharmaceutics"
DOI: 10.3390/pharmaceutics13060788
Abstract: Choline kinase (ChoK) is a cytosolic enzyme that catalyzes the phosphorylation of choline to form phosphorylcholine (PCho) in the presence of ATP and magnesium. ChoK is required for the synthesis of key membrane phospholipids and… read more here.
Keywords: strategy; medicine; precision medicine; choline kinase ... See more keywords
Biological Evaluation of New Thienopyridinium and Thienopyrimidinium Derivatives as Human Choline Kinase Inhibitors
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DOI: 10.3390/pharmaceutics14040715
Abstract: Due to its role in lipid biosynthesis, choline kinase α1 (CKα1) is an interesting target for the development of new antitumor agents. In this work, we present a series of 41 compounds designed based on… read more here.
Keywords: choline kinase; evaluation new; biological evaluation; kinase ... See more keywords
Choline Kinase α Inhibitors MN58b and RSM932A Enhances the Antitumor Response to Cisplatin in Lung Tumor Cells
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DOI: 10.3390/pharmaceutics14061143
Abstract: Lung cancer is one of the main causes of death in developed countries, and non-small cell lung cancer (NSCLC) is the most frequent type (80% of patients). In advanced NSCLC, platinum-based chemotherapy is the frontline… read more here.
Keywords: choline kinase; kinase inhibitors; combination; lung ... See more keywords
Downregulation of human choline kinase α gene expression by miR-876-5p.
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DOI: 10.3892/mmr.2018.8762
Abstract: Choline kinase (CK) is the first enzyme in the CDP-choline pathway for the synthesis of phosphatidylcholine, the most abundant phospholipid in the mammalian cell membrane. This enzyme exists as three isozymes (α1, α2 and β)… read more here.
Keywords: choline; gene expression; mir 876; choline kinase ... See more keywords