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Rhosin

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https://www.readbyqxmd.com/read/27681226/rhoa-and-rac1-gtpases-differentially-regulate-agonist-receptor-mediated-reactive-oxygen-species-generation-in-platelets
#1
Huzoor Akbar, Xin Duan, Saima Saleem, Ashley K Davis, Yi Zheng
Agonist induced generation of reactive oxygen species (ROS) by NADPH oxidases (NOX) enhances platelet aggregation and hence the risk of thrombosis. RhoA and Rac1 GTPases are involved in ROS generation by NOX in a variety of cells, but their roles in platelet ROS production remain unclear. In this study we used platelets from RhoA and Rac1 conditional knockout mice as well as human platelets treated with Rhosin and NSC23767, rationally designed small molecule inhibitors of RhoA and Rac GTPases, respectively, to better define the contributions of RhoA and Rac1 signaling to ROS generation and platelet activation...
2016: PloS One
https://www.readbyqxmd.com/read/27187066/activation-of-rhoa-but-not-rac1-mediates-early-stages-of-s1p-induced-endothelial-barrier-enhancement
#2
Xun E Zhang, Shaquria P Adderley, Jerome W Breslin
Compromised endothelial barrier function is a hallmark of inflammation. Rho family GTPases are critical in regulating endothelial barrier function, yet their precise roles, particularly in sphingosine-1-phosphate (S1P)-induced endothelial barrier enhancement, remain elusive. Confluent cultures of human umbilical vein endothelial cells (HUVEC) or human dermal microvascular endothelial cells (HDMEC) were used to model the endothelial barrier. Barrier function was assessed by determining the transendothelial electrical resistance (TER) using an electrical cell-substrate impedance sensor (ECIS)...
2016: PloS One
https://www.readbyqxmd.com/read/26482039/chemotherapy-resistance-in-diffuse-type-gastric-adenocarcinoma-is-mediated-by-rhoa-activation-in-cancer-stem-like-cells
#3
Changhwan Yoon, Soo-Jeong Cho, B├╝lent Arman Aksoy, Do Joong Park, Nikolaus Schultz, Sandra W Ryeom, Sam S Yoon
PURPOSE: The Lauren diffuse type of gastric adenocarcinoma (DGA), as opposed to the intestinal type (IGA), often harbors mutations in RHOA, but little is known about the role of RhoA in DGA. EXPERIMENTAL DESIGN: We examined RhoA activity and RhoA pathway inhibition in DGA cell lines and in two mouse xenograft models. RhoA activity was also assessed in patient tumor samples. RESULTS: RhoA activity was higher in DGA compared with IGA cell lines and was further increased when grown as spheroids to enrich for cancer stem-like cells (CSCs) or when sorted using the gastric CSC marker CD44...
February 15, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/23382194/small-molecule-inhibitors-targeting-g-protein-coupled-rho-guanine-nucleotide-exchange-factors
#4
Xun Shang, Fillipo Marchioni, Chris R Evelyn, Nisha Sipes, Xuan Zhou, William Seibel, Matthew Wortman, Yi Zheng
The G-protein-mediated Rho guanine nucleotide exchange factor (GEF)-Rho GTPase signaling axis has been implicated in human pathophysiology and is a potential therapeutic target. By virtual screening of chemicals that fit into a surface groove of the DH-PH domain of LARG, a G-protein-regulated Rho GEF involved in RhoA activation, and subsequent validations in biochemical assays, we have identified a class of chemical inhibitors represented by Y16 that are active in specifically inhibiting LARG binding to RhoA...
February 19, 2013: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/22726684/rational-design-of-small-molecule-inhibitors-targeting-rhoa-subfamily-rho-gtpases
#5
Xun Shang, Fillipo Marchioni, Nisha Sipes, Chris R Evelyn, Moran Jerabek-Willemsen, Stefan Duhr, William Seibel, Matthew Wortman, Yi Zheng
Rho GTPases have been implicated in diverse cellular functions and are potential therapeutic targets. By virtual screening, we have identified a Rho-specific inhibitor, Rhosin. Rhosin contains two aromatic rings tethered by a linker, and it binds to the surface area sandwiching Trp58 of RhoA with a submicromolar Kd and effectively inhibits GEF-catalyzed RhoA activation. In cells, Rhosin specifically inhibited RhoA activity and RhoA-mediated cellular function without affecting Cdc42 or Rac1 signaling activities...
June 22, 2012: Chemistry & Biology
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