NCT-58(NCT-58) - 药物靶点：HSP90_在研适应症：HER2阳性乳腺癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

HSP90

作用机制

HSP90 抑制剂(Heat shock 90kDa proteins inhibitors)

治疗领域

肿瘤皮肤和肌肉骨骼疾病

在研适应症

HER2阳性乳腺癌

非在研适应症-

原研机构

Korea University

在研机构

Korea 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C27H34N2O5

InChIKeyQGEKYFVMAGLOKW-UHFFFAOYSA-N

CAS号2411429-33-7

关联

100 项与 NCT-58 相关的临床结果

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100 项与 NCT-58 相关的转化医学

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100 项与 NCT-58 相关的专利（医药）

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1

项与 NCT-58 相关的文献（医药）

Cell Death Discovery2区 · 医学

The C-terminal HSP90 inhibitor NCT-58 kills trastuzumab-resistant breast cancer stem-like cells

2区 · 医学

ArticleOA

作者: Kim, Ji Young ; Park, Minsu ; Seo, Jae Hong ; Park, Jung Min ; Park, Soeun ; Farrand, Lee ; Nam, Kee Dal ; La, Minh Thanh ; Kim, Yoon-Jae ; Ann, Jihyae ; Nguyen, Cong-Truong ; Lee, Jeewoo

AbstractN-terminal HSP90 inhibitors in development have had issues arising from heat shock response (HSR) induction and off-target effects. We sought to investigate the capacity of NCT-58, a rationally-synthesized C-terminal HSP90 inhibitor, to kill trastuzumab-resistant HER2-positive breast cancer stem-like cells. NCT-58 does not induce the HSR due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills the rapidly proliferating bulk tumor cells as well as the breast cancer stem-like population, coinciding with significant reductions in stem/progenitor markers and pluripotent transcription factors. NCT-58 treatment suppressed growth and angiogenesis in a trastuzumab-resistant xenograft model, concomitant with downregulation of ICD-HER2 and HSF-1/HSP70/HSP90. These findings warrant further investigation of NCT-58 to address trastuzumab resistance in heterogeneous HER2-positive cancers.

100 项与 NCT-58 相关的药物交易

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