CBB-3001(CBB-3001) - 药物靶点：KDM1A_专利_临床

概要

基本信息

药物类型

化学药

别名

靶点

KDM1A

作用机制

KDM1A抑制剂(赖氨酸特异性组蛋白脱甲基酶-1抑制剂)

治疗领域

肿瘤其他疾病

在研适应症-

非在研适应症

胚胎癌畸胎癌

原研机构

University of Nevada

在研机构-

非在研机构

University of Nevada

最高研发阶段无进展临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 CBB-3001 相关的临床结果

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100 项与 CBB-3001 相关的转化医学

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100 项与 CBB-3001 相关的专利（医药）

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1

项与 CBB-3001 相关的文献（医药）

2018-05-01·Bioorganic & Medicinal Chemistry3区 · 医学

New histone demethylase LSD1 inhibitor selectively targets teratocarcinoma and embryonic carcinoma cells

3区 · 医学

Article

作者: Saxena, Lovely ; Zhang, Xuan ; Hoang, Nam ; Zheng, Guangrong ; Leng, Feng ; Bhowmik, Pradip ; Zhang, Chunxiao ; Yin, Feng ; Lu, Fei ; Vo, Van ; Zhang, Hui

LSD1/KDM1 is a histone demethylase that preferentially removes methyl groups from the mono- and di-methylated lysine 4 in histone H3 (H3K4), key marks for active chromatin for transcriptional activation. LSD1 is essential for pluripotent embryonic stem cells and embryonic teratocarcinoma/carcinoma cells and its expression is often elevated in various cancers. We developed a new LSD1 inhibitor, CBB3001, which potently inhibited LSD1 activity both in vitro and in vivo. CBB3001 also selectively inhibited the growth of human ovarian teratocarcinoma PA-1 and mouse embryonic carcinoma F9 cells, caused the downregulation of pluripotent stem cell proteins SOX2 and OCT4. However, CBB3001 does not have significant inhibition on the growth of human colorectal carcinoma HCT116 cells or mouse fibroblast NIH3T3 cells that do not express these stem cell proteins. Our studies strongly indicate that CBB3001 is a specific LSD1 inhibitor that selectively inhibits teratocarcinoma and embryonic carcinoma cells that express SOX2 and OCT4.

100 项与 CBB-3001 相关的药物交易

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