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Tangeretin inhibits extracellular‐signal‐regulated kinase (ERK) phosphorylation
Author(s) -
Van Slambrouck Séverine,
Parmar Virinder S.,
Sharma Sunil K.,
Bondt Bart De,
Foré Fleur,
Coopman Peter,
Vanhoecke Barbara W.,
Boterberg Tom,
Depypere Herman T.,
Leclercq Guy,
Bracke Marc E.
Publication year - 2005
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/j.febslet.2004.10.114
Subject(s) - phosphorylation , kinase , extracellular , mapk/erk pathway , intracellular , microbiology and biotechnology , biology , chemistry , biochemistry
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.