KY1022(KY1022) - 药物靶点：CTNNB x RAS_在研适应症：结直肠癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

CTNNB x RAS

作用机制

CTNNB 抑制剂(β-连环蛋白抑制剂)、RAS 抑制剂(RAS type GTPase family inhibitors)

治疗领域

肿瘤消化系统疾病

在研适应症

结直肠癌

非在研适应症-

原研机构

Yonsei University

在研机构

Yonsei University

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C17H19N3OS

InChIKeyINRQXFWQQLFWNZ-UHFFFAOYSA-N

CAS号1029721-36-5

关联

100 项与 KY1022 相关的临床结果

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100 项与 KY1022 相关的转化医学

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100 项与 KY1022 相关的专利（医药）

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1

项与 KY1022 相关的文献（医药）

2016-12-06·Oncotarget

KY1022, a small molecule destabilizing Ras via targeting the Wnt/β-catenin pathway, inhibits development of metastatic colorectal cancer

Article

作者: Choi, Kang-Yell ; Koo, Kyung-Hwa ; Han, Gyoonhee ; Yoon, Jeong-Soo ; Cho, Yong-Hee ; Park, Ki-Sook ; Cha, Pu-Hyeon ; Kaduwal, Saluja ; Shin, Wookjin ; Ro, Eun Ji ; Kim, Hyuntae ; Lee, Sang-Kyu ; Park, Jong-Chan

APC (80-90%) and K-Ras (40-50%) mutations frequently occur in human colorectal cancer (CRC) and these mutations cooperatively accelerate tumorigenesis including metastasis. In addition, both β-catenin and Ras levels are highly increased in CRC, especially in metastatic CRC (mCRC). Therefore, targeting both the Wnt/β-catenin and Ras pathways could be an ideal therapeutic approach for treating mCRC patients. In this study, we characterized the roles of KY1022, a small molecule that destabilizes both β-catenin and Ras via targeting the Wnt/β-catenin pathway, in inhibiting the cellular events, including EMT, an initial process of metastasis, and apoptosis. As shown by in vitro and in vivo studies using APCMin/+/K-RasG12DLA2 mice, KY1022 effectively suppressed the development of mCRC at an early stage of tumorigenesis. A small molecular approach degrading both β-catenin and Ras via inhibition of the Wnt/β-catenin signaling would be an ideal strategy for treatment of mCRC.

100 项与 KY1022 相关的药物交易

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