BAY-524(BAY-524) - 药物靶点：BUB1_在研适应症：肿瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

BUB1

作用机制

BUB1 inhibitors(BUB-1 protein kinase inhibitors)

治疗领域

肿瘤

在研适应症

肿瘤

非在研适应症-

原研机构

Bayer Pharma AG

在研机构

Bayer Pharma AG

非在研机构-

最高研发阶段药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C24H24F2N6O3

InChIKeyLMRCQVHTZUUHFN-UHFFFAOYSA-N

CAS号1445830-39-6

关联

100 项与 BAY-524 相关的临床结果

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100 项与 BAY-524 相关的转化医学

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100 项与 BAY-524 相关的专利（医药）

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1

项与 BAY-524 相关的文献（医药）

eLife1区 · 生物学

Probing the catalytic functions of Bub1 kinase using the small molecule inhibitors BAY-320 and BAY-524

1区 · 生物学

ArticleOA

作者: von Schubert, Conrad ; Siemeister, Gerhard ; Baron, Anna P ; Mumberg, Dominik ; Schröder, Jens ; Hitchcock, Marion ; Fernández-Montalván, Amaury ; Nigg, Erich A ; Cubizolles, Fabien ; von Nussbaum, Franz ; Mengel, Anne

The kinase Bub1 functions in the spindle assembly checkpoint (SAC) and in chromosome congression, but the role of its catalytic activity remains controversial. Here, we use two novel Bub1 inhibitors, BAY-320 and BAY-524, to demonstrate potent Bub1 kinase inhibition both in vitro and in intact cells. Then, we compared the cellular phenotypes of Bub1 kinase inhibition in HeLa and RPE1 cells with those of protein depletion, indicative of catalytic or scaffolding functions, respectively. Bub1 inhibition affected chromosome association of Shugoshin and the chromosomal passenger complex (CPC), without abolishing global Aurora B function. Consequently, inhibition of Bub1 kinase impaired chromosome arm resolution but exerted only minor effects on mitotic progression or SAC function. Importantly, BAY-320 and BAY-524 treatment sensitized cells to low doses of Paclitaxel, impairing both chromosome segregation and cell proliferation. These findings are relevant to our understanding of Bub1 kinase function and the prospects of targeting Bub1 for therapeutic applications.

100 项与 BAY-524 相关的药物交易

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