CCG-203971 是一种第二代 Rho/MRTF/SRF 通路抑制剂,CCG-203971 可抑制 PC-3 细胞迁移(IC50值为4.2 μM)。 产品性质 英文别名(English Synonym) CCG-203971 中文名称(Chinese Name) / 靶点(Target) others 通路(Pathway) GPCR/G Protein CAS号(CAS NO.) ...
Rho/MRTF/SRFmitochondriabioenergeticshistone-4acetylationoxidative stressRhoA-regulated gene transcription by serum response factor (SRF) and its transcriptional cofactor myocardin-related transcription factors (MRTFs) signaling pathway has emerged as a promising therapeutic target for pharmacological intervention ...
R.R.N. is a President and Founder of Fibrosix, Inc. R.R.N. and E.M.L. are part of the following patent “Inhibitors of Myocardin-Related Transcription Factor and Serum Response Factor (MRTF/SRF)-Mediated Gene Transcription and Methods for use of the same”, Serial Number 14/934,769...
Yuan等[43]研究发现巩膜成纤维细胞受到机械应力后可激活RhoA,通过RhoA/ROCK2-MRTF-A/SRF途径,使得心肌相关转录因子-A(MRTF-A)核转移,α-SMA表达增加,诱导其分化为肌成纤维细胞。另外,MDIA和ROCK在Rho引起的应力纤维形成过程中同时被激活,MDIA通过成核和聚合产生肌动蛋白细丝,而ROCK激活肌球蛋白使其交联,从而诱导...
Among them, it has been well known that RhoA activates SRF (36). The mechanism by which RhoA activates SRF has been proposed as follows; MAL/MKL1, a member of the myocardin-related transcription factor (MRTF) is a cofactor of SRF that binds to monomeric G-actin in the cytosol but ...
CCG-100602 inhibits RhoA/C-mediated, SRF-driven luciferase expression in PC-3 prostate cancer cells (IC50 :9.8 μM). 体外活性 CCG-100602 抑制 MRTF-A/SRF 激活基因的表达。在 3-30 μM 浓度下,CCG-100602 减少了黏附的 hASC 细胞的数量[1]。
[180], and repress fibrogenesis by blocking RhoA/ROCK/MYLK/SRF signaling in colonic myofibroblasts, representing a new therapy for intestinal fibrosis in IBD patients [117]. Furthermore, several substances have shown therapeutic potential by affecting RhoA/ROCK signaling. Oxymatrine, a Chinese herb ...
localization of FLAG-MRTF-A, and the effect of MRTF-A overexpression on smooth muscle alpha-actin promoter activity was inhibited by dominant negative RhoA... K Lockman,JS Hinson,MD Medlin,... - 《Journal of Biological Chemistry》 被引量: 287发表: 2004年 EphrinA1 inactivates integrin-mediated...
Disclosed herein are inhibitors of Rho/MRTF/SRF-mediated gene transcription, and methods for their use in treating or preventing diseases such as cancer and fibrosis. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereofScott D. Larsen...
Disclosed herein are inhibitors of Rho/MRTF/SRF-mediated gene transcription, and methods for their use in treating or preventing diseases such as cancer and fibrosis. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof: wherein the substituents ...