NS1643(NS1643) - 药物靶点：hERG_在研适应症：心律失常_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

hERG

作用机制

hERG激动剂(电压门控性钾通道蛋白亚型Kv11.1激动剂)

治疗领域

心血管疾病

在研适应症

心律失常

非在研适应症-

原研机构

Neurosearch

在研机构

Neurosearch

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-

关联

100 项与 NS1643 相关的临床结果

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100 项与 NS1643 相关的转化医学

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100 项与 NS1643 相关的专利（医药）

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1

项与 NS1643 相关的文献（医药）

PLOS ONE

hERG channel agonist NS1643 strongly inhibits invasive astrocytoma cell line SMA-560

Article

作者: Stylii, Stanley S ; Luwor, Rodney B. ; Stylii, Stanley S. ; Luwor, Rodney B ; Chong, Harvey K. ; Yuan, Patrick H. ; Chong, Harvey K ; Benn, Kieran W ; French, Christopher R ; Benn, Kieran W. ; Yuan, Patrick H ; French, Christopher R.

Gliomas are highly malignant brain tumours that remain refractory to treatment. Treatment is typically surgical intervention followed by concomitant temozolomide and radiotherapy; however patient prognosis remains poor. Voltage gated ion channels have emerged as novel targets in cancer therapy and inhibition of a potassium selective subtype (hERG, Kv11.1) has demonstrated antitumour activity. Unfortunately blockade of hERG has been limited by cardiotoxicity, however hERG channel agonists have produced similar chemotherapeutic benefit without significant side effects. In this study, electrophysiological recordings suggest the presence of hERG channels in the anaplastic astrocytoma cell line SMA-560, and treatment with the hERG channel agonist NS1643, resulted in a significant reduction in the proliferation of SMA-560 cells. In addition, NS1643 treatment also resulted in a reduction of the secretion of matrix metalloproteinase-9 and SMA-560 cell migration. When combined with temozolomide, an additive impact was observed, suggesting that NS1643 may be a suitable adjuvant to temozolomide and limit the invasiveness of glioma.

100 项与 NS1643 相关的药物交易

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