TCD Pharma - Choline Kinase Alpha

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ChoKα is a naturally occurring intracellular enzyme that is involved in the regulation of cell proliferation and in the control of phosphorylcholine (PC) synthesis, which is a lipid that serves as a critical structural component of the cell membrane.

Regulation of phosphatidylcholine biosynthesis. Biochim Biophys Acta 1984, 779(2):217-5. Pelech SL and Vance DE.

Choline phospholipid metabolism: a target in cancer cells. J Cell Biochem 2003, 90(3):525-3. Ackerstaff E et al.

Overexpression of ChoKα but not ChoKα is oncogenic in human cells.

Differential role of human choline kinase alpha and beta enzymes in lipid metabolism: implications in cancer onset and treatment. PLoS One 2009, 12;4(11):e7819. Gallego-Ortega D et al.

ChoKα is a novel oncogene that promotes carcinogenesis in vivo.

Choline kinase activation is a critical requirement for the proliferation of primary human mammary epithelial cells and breast tumor progression. Cancer Res 2004, 64(18):6732-9. Ramírez de Molina A et al.

ChoKα is constitutively activated in most human tumour-derived cell lines.

Overexpression of choline kinase is a frequent feature in human tumour-derived cell lines and in lung, prostate and colorectal human cancers. Biochem Biophys Res Commun 2002, 296:580-583. Ramírez de Molina A et al.

ChoKα overexpression enhances cell motility and invasion in vitro.

Choline kinase overexpression increases invasiveness and drug resistance of human breast cancer cells. NMR Biomed 2010, 23: 633–642. Shah T et al.

Choline kinase is a novel oncogene that potentiates RhoA-induced carcinogenesis. Cancer Res 2005, 65:5647-53. Ramírez de Molina A et al.

ChoKα levels and activity are increased in human tumour-derived cell lines and tumours and correlate with worse prognosis in breast, lung and bladder tumours.

Increased choline kinase activity in human breast carcinomas: clinical evidence for a potential novel antitumour strategy. Oncogene 2002, 21:4317-4322. Ramírez de Molina A et al.

Choline kinase α expression to predict patient outcome in early stage Non-Small Cell Lung Cancer. Lancet Oncol 2007, 8:889-97. Ramírez de Molina A et al.

Regulation of Akt (ser473) phosphorylation by choline kinase in breast carcinoma cells. Mol Cancer 2009, 8:131. Chua BT et al.

A critical role for choline kinase-alpha in the aggressiveness of bladder carcinomas. Oncogene 2009, 28(26): 2425-35. Hernando E et al.

Activation of phosphatidylcholine cycle enzymes in human epithelial ovarian cancer cells. Cancer Res 2010, 70(5); 2126–35. Iorio E et al.

ChoKα expression is an independent factor associated with worse clinical outcome in patients with NSCLC.

Choline kinase α expression to predict patient outcome in early stage Non-Small Cell Lung Cancer. Lancet Oncol 2007, 8:889-97. Ramírez de Molina A et al.

The levels of ChoKα may be useful as diagnostic and prognostic tools in human cancer allowing a Targeted Therapy approach.

Choline kinase α expression to predict patient outcome in early stage Non-Small Cell Lung Cancer. Lancet Oncol 2007, 8:889-97. Ramírez de Molina A et al.

Choline kinase alpha in cancer prognosis and treatment. Lancet Oncol 2007, 8(10): 855-7. Glunde K and Bhujwala ZM.

siRNA technology validates ChoKα as a novel drug target.

RNA interference-mediated choline kinase suppression in breast cancer cells induces differentiation and reduces proliferation. Cancer Res 2005, 65(23):11034-43. Glunde K et al.

Choline kinase down-regulation increases the effect of 5-fluorouracil in breast cancer cells. Cancer Res 2007, 67(23):11284-90. Mori N et al.

Choline kinase alpha depletion selectively kills tumoural cells. Curr Cancer Drug Targets 2008, 8(8):709-19. Bañez-Coronel M et al.

Potent and selective inhibitors of ChoKα have been identified and demonstrate antiproliferative and antitumoural effects in vitro and in vivo on a range of human tumour derived cells.

Choline kinase inhibitory effect and antiproliferative activity of new 1,1',1"-(benzene-1,3,5-triylmethylene)tris{4-[(disubstituted)amino]pyridinium} tribromides. Eur J Med Chem 2003, 38:109-116. Conejo-García A et al.

Symmetrical bis-quinolinium compounds: new human choline kinase inhibitors with antiproliferative activity against the HT-29 cell line. J Med Chem 2005;48: 3354-63. Sánchez-Martín R et al.

Noninvasive magnetic resonance spectroscopic pharmacodynamic markers of the choline kinase inhibitor MN58b in human carcinoma models. Cancer Res 2006, 66 (1):427-34. Al-Saffar NM et al.

LUMO Energy of model compounds as an index for the inhibition of choline kinase: chemical meaning. Eur J Med Chem 2001, 36:215-225. Campos J et al.

ChoKα inhibitors exhibit a favourable safety profile including differential effects on normal and tumour cells.

Choline kinase inhibition induces the increase in ceramides resulting in a highly specific and selective cytotoxic antitumoural strategy as a potential mechanism of action. Oncogene 2004, 23: 8247-8259. Rodríguez-González A et al.

Inhibition of choline kinase renders a highly selective cytotoxic effect in tumour cells through a mitochondrial independent mechanism. Int J Oncol 2005, 26: 999-1008. Rodríguez-González A et al.

Choline kinase alpha depletion selectively kills tumoural cells. Curr Cancer Drug Targets 2008, 8(8):709-19. Bañez-Coronel M et al.

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