BIM-46228(BIM-46228) - 药物靶点：Ftase x SYNGAP1 x 转移酶_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

Ftase x SYNGAP1 x 转移酶

作用机制

Ftase抑制剂(蛋白法尼基转移酶复合体抑制剂)、SYNGAP1 inhibitors(Ras GTPase inhibitors)、转移酶抑制剂

治疗领域

肿瘤

在研适应症-

非在研适应症

肿瘤

原研机构

Institut Henri Beaufour

在研机构-

非在研机构

Institut Henri Beaufour

最高研发阶段无进展药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C31H26N6O2

InChIKeyQVDKEDZDNKOUGI-UHFFFAOYSA-N

CAS号280775-15-7

关联

100 项与 BIM-46228 相关的临床结果

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100 项与 BIM-46228 相关的转化医学

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100 项与 BIM-46228 相关的专利（医药）

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1

项与 BIM-46228 相关的文献（医药）

2001-03-01·International Journal of Cancer1区 · 医学

Inhibition of human tumor cell growthin vivo by an orally bioavailable inhibitor of human farnesyltransferase, BIM-46228

1区 · 医学

Article

作者: Thomas Gordon ; Gilles Favre ; Marie-Christine Brezak ; Marie-Odile Lonchampt ; Isabelle Viossat ; Barry Morgan ; Philip Kasprzyk ; Isabelle Ader ; Anne Pradines ; Christine Toulas ; Grégoire P. Prevost

Oncogenic mutations of the ras gene leading to constitutive activation of downstream effectors have been detected in a wide spectrum of human cancers (pancreas, thyroid, colon, non-small-cell lung cancer). Membrane anchorage of Ras, required for functional activity in signal transduction, is facilitated by post-translational modifications resulting in covalent attachment of a farnesyl group to the cysteine in the C-terminal CAAX motif. This attachment is mediated by farnesyltransferase (FTase). Here, we report a novel FTase inhibitor, BIM-46228, which showed (i) specific inhibition of purified human FTase enzyme, (ii) inhibition of proliferation in vitro in a large spectrum of human tumor cell lines, (iii) inhibition of growth of human tumor xenografts in athymic nude mice treated by per os administration and (iv) the benefits of in vitro combination of its activity with chemotherapy or radiotherapy.

100 项与 BIM-46228 相关的药物交易

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