C - Chemistry – Metallurgy – 12 – Q
Patent
C - Chemistry, Metallurgy
12
Q
C12Q 1/48 (2006.01) A61K 38/00 (2006.01) A61P 35/00 (2006.01) G01N 33/68 (2006.01)
Patent
CA 2613322
The present invention features a method for determining the methyltransferase activity of a polypeptide and screening for modulators of methyltransferase activity, more particularly for modulators of the methylation of retinoblastoma by SMYD3. The invention further provides a method or pharmaceutical composition for prevention or treating of colorectal cancer, hepatocellular carcinoma, bladder cancer and/or breast cancer using a modulator so identified. N-terminal truncated forms of SMYD3 (alias ZNFN3A1) have higher methylating activity. Lys 824 is a preferred methylation site on the RB1 protein for SMYD3.
La présente invention concerne une méthode de détermination de l'activité méthyltransférase d'un polypeptide et de criblage de modulateurs d'activité méthyltransférase, plus particulièrement de modulateurs de la méthylation du rétinoblastome par SMYD3. L'invention concerne également une méthode ou une composition pharmaceutique de prévention ou de traitement du cancer colorectal, du carcinome hépatocellulaire, du cancer de la vessie et/ou du cancer du sein à l'aide d'un modulateur ainsi identifié.
Furukawa Yoichi
Hamamoto Ryuji
Nakamura Yusuke
Nakatsuru Shuichi
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Oncotherapy Science Inc.
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