title: Tangeretin inhibits extracellular-signal-regulated kinase (ERK) phosphorylation.
abstract: Tangeretin is a methoxyflavone from citrus fruits, which inhibits growth of human mammary cancer cells and cytolysis by natural killer cells. Attempting to unravel the flavonoid's action mechanism, we found that it inhibited extracellular-signal-regulated kinases 1/2 (ERK1/2) phosphorylation in a dose- and time-dependent way. In human T47D mammary cancer cells this inhibition was optimally observed after priming with estradiol. The spectrum of the intracellular signalling kinase inhibition was narrow and comparison of structural congeners showed that inhibition of ERK phosphorylation was not unique for tangeretin. Our data add tangeretin to the list of small kinase inhibitors with a restricted intracellular inhibition profile.
authors.affiliation: Laboratory of Experimental Cancerology, Department of Radiotherapy and Nuclear Medicine, Ghent University Hospital, B-9000 Ghent, Belgium.
authors.forename: Séverine
authors.initials: S
authors.lastname: Van Slambrouck
authors.forename: Virinder S
authors.initials: VS
authors.lastname: Parmar
authors.forename: Sunil K
authors.initials: SK
authors.lastname: Sharma
authors.forename: Bart
authors.initials: B
authors.lastname: De Bondt
authors.forename: Fleur
authors.initials: F
authors.lastname: Foré
authors.forename: Peter
authors.initials: P
authors.lastname: Coopman
authors.forename: Barbara W
authors.initials: BW
authors.lastname: Vanhoecke
authors.forename: Tom
authors.initials: T
authors.lastname: Boterberg
authors.forename: Herman T
authors.initials: HT
authors.lastname: Depypere
authors.forename: Guy
authors.initials: G
authors.lastname: Leclercq
authors.forename: Marc E
authors.initials: ME
authors.lastname: Bracke
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000201:enzymology*; D045744:Cell Line, Tumor; D004958:Estradiol / Q000494:pharmacology; D048049:Extracellular Signal-Regulated MAP Kinases / Q000037:antagonists & inhibitors*; D005260:Female; D047309:Flavones / Q000494:pharmacology*; D006801:Humans; D019950:Mitogen-Activated Protein Kinase 1 / Q000037:antagonists & inhibitors; D048052:Mitogen-Activated Protein Kinase 3 / Q000037:antagonists & inhibitors; D015394:Molecular Structure; D010766:Phosphorylation / Q000187:drug effects; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D015398:Signal Transduction / Q000187:drug effects
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D047309:Flavones; D047428:Protein Kinase Inhibitors; D004958:Estradiol; D048049:Extracellular Signal-Regulated MAP Kinases; D019950:Mitogen-Activated Protein Kinase 1; D048052:Mitogen-Activated Protein Kinase 3; C059006:tangeretin