Method for assaying histone methylation enzyme activity
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United States of America Patent
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Apr 21, 2015
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Jan 31, 2013
app pub date -
Apr 15, 2011
filing date -
Apr 19, 2010
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Abstract
Provided are a method for measuring histone methyltransferase activity, a method for screening for compounds that inhibit histone methyltransferase activity, a reagent kit for measuring histone methyltransferase activity, and a kit for screening for compounds that inhibit histone methyltransferase activity. A substrate compound represented by general formula (I): R1-X-K-R2 (I), or a salt thereof, wherein R1 represents a hydrogen atom or a protecting group for an amino terminus; X represents a peptide consisting of 0 or 1 or more amino acid residues; K represents a lysine residue; and R2 represents a dye label linked via an amide bond to the carbonyl terminus of a lysine residue, wherein the cleavage of the amide bond by peptidase changes the fluorescence property or chromogenic property of the dye label, and the methylation of the ε amino group of the lysine residue by the histone methyltransferase decreases susceptibility to peptidase, is used.
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