生化/生理作用
BCI-121 是一种底物竞争性 SMYD3 抑制剂，可降低核组蛋白 H3 lys4 二甲基化和三甲基化的级别（通过HT29 细胞中 50%/H3K4me2 和 40%H3K4me3；48小时内100μM BCI-121实现），下调已知的 SMYD3 靶基因转录，并选择性影响 SMYD3 依赖的癌症培养物增殖（46%/HT29 和 54%/HCT116 增殖减少；72小时内的100μM BCI-121），对低表达 SMYD3 的癌细胞几乎没有抗增殖作用。BCI-121 通过直接亲和作用靶向 SMYD3（kon 357.7/M/s；k off 4.23 × 10 -3 /s；K D = K off/ K on = 11.8μM），并与组蛋白结合 SMYD3（% 抑制率/[组蛋白H4 肽]:[BCI-121] 比值 = 36.5%/1：1 和 51.0%/1：2.5）有效竞争。
BCI121能够减少MDA-MB-231细胞的间充质特征。它还可以降低它们体外和体内的入侵能力。
WGK
WGK 3
Tianjiao Lyu et al.
International journal of cancer, 146(6), 1553-1567 (2019-09-11)
Detachment of cancer cells from the primary tumor and formation of spheroids in ascites is required for implantation metastasis in epithelial ovarian cancer (EOC), but the underlying mechanism of this process has not been thoroughly elucidated. To mimic this process
SMYD3 promotes the epithelial-mesenchymal transition in breast cancer
Fenizia C, et al.
Nucleic Acids Research, 47(3), 1278-1293 (2018)
Ryuji Hamamoto et al.
Cancer science, 107(4), 377-384 (2016-01-12)
Protein methylation is one of the important post-translational modifications. Although its biological and physiological functions were unknown for a long time, we and others have characterized a number of protein methyltransferases, which have unveiled the critical functions of protein methylation
Alessia Peserico et al.
Journal of cellular physiology, 230(10), 2447-2460 (2015-03-03)
SMYD3 is a histone lysine methyltransferase that plays an important role in transcriptional activation as a member of an RNA polymerase complex, and its oncogenic role has been described in different cancer types. We studied the expression and activity of
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