LIJTF-500025(LIJTF-500025) - 药物靶点：LIMK1 x LIMK2_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

LIMK1 x LIMK2

作用机制

LIMK1抑制剂(LIM domain kinase 1 inhibitors)、LIMK2抑制剂(LIM结构域激酶-2抑制剂)

治疗领域

肿瘤

在研适应症

肿瘤

非在研适应症-

原研机构

University of Cardiff

在研机构

University of Cardiff

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-

关联

100 项与 LIJTF-500025 相关的临床结果

登录后查看更多信息

100 项与 LIJTF-500025 相关的转化医学

登录后查看更多信息

100 项与 LIJTF-500025 相关的专利（医药）

登录后查看更多信息

1

项与 LIJTF-500025 相关的文献（医药）

2022-10-27·Journal of Medicinal Chemistry1区 · 医学

Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity

1区 · 医学

Article

作者: Elkins, Jonathan M. ; Collins, Ross ; Thomas, Carys ; Ward, Simon E. ; Waters, Loren ; Foley, David W. ; Jones, Kimberley ; Gillespie, Jason A. ; Jones, D. Heulyn ; Paine, Marie ; Atack, John R. ; Lee, Hyunah ; Grubisha, Olivera ; Baldwin, Alex G.

LIM domain kinases 1 and 2 (LIMK1 and LIMK2) regulate actin dynamics and subsequently key cellular functions such as proliferation and migration. LIMK1 and LIMK2 phosphorylate and inactivate cofilin leading to increased actin polymerization. As a result, LIMK inhibitors are emerging as a promising treatment strategy for certain cancers and neurological disorders. High-quality chemical probes are required if the role of these kinases in health and disease is to be understood. To that end, we report the results of a comparative assessment of 17 reported LIMK1/2 inhibitors in a variety of in vitro enzymatic and cellular assays. Our evaluation has identified three compounds (TH-257, LIJTF500025, and LIMKi3) as potent and selective inhibitors suitable for use as in vitro and in vivo pharmacological tools for the study of LIMK function in cell biology.

100 项与 LIJTF-500025 相关的药物交易

登录后查看更多信息