| abstract |
FIELD: biotechnology.SUBSTANCE: present invention relates to inhibition of wild-type forms and certain mutant forms of human histone EZH2 methyltransferase — a catalytic subunit of the PRC2 complex, catalysing from mono- to trimethylation of lysine 27 on histone H3 (H3-K27), to methods for treating various types of cancer, including follicular lymphoma and diffuse large-B-cell lymphoma (DLBCL), and to methods for determining the capability of responding to an EZH2 inhibitor in an individual. The method for identifying an individual as responsive to a selective inhibitor of Y641 EZH2 mutant on includes a) obtaining a tissue sample from the individual; b) identifying the level of dimethylation (me2) of H3-K27 if present in said tissue sample, and comparing the level of dimethylation (me2) with the reference level of dimethylation (me2); wherein said individual is responsive to a selective inhibitor of Y641 EZH2 mutant when said level of dimethylation (me2) is absent or lower than said reference level of dimethylation (me2), and wherein the reference level constitutes a level of dimethylation (me2) of H3-K27 in the tissue sample from the individual wherein the Y641 EZH2 mutant is not expressed.EFFECT: inhibition of certain forms of human histone EZH2 methyltransferase.10 cl, 4 tbl, 14 dwg, 11 ex |