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https://www.readbyqxmd.com/read/28054559/the-rhoa-rock-pathway-ameliorates-adhesion-and-inflammatory-infiltration-induced-by-ages-in-glomerular-endothelial-cells
#1
Jialing Rao, Zengchun Ye, Hua Tang, Cheng Wang, Hui Peng, Weiyan Lai, Yin Li, Wanbing Huang, Tanqi Lou
A recent study demonstrated that advanced glycation end products (AGEs) play a role in monocyte infiltration in mesangial areas in diabetic nephropathy. The Ras homolog gene family, member A Rho kinase (RhoA/ROCK) pathway plays a role in regulating cell migration. We hypothesized that the RhoA/ROCK pathway affects adhesion and inflammation in endothelial cells induced by AGEs. Rat glomerular endothelial cells (rGECs) were cultured with AGEs (80 μg/ml) in vitro. The ROCK inhibitor Y27632 (10 nmol/l) and ROCK1-siRNA were used to inhibit ROCK...
January 5, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28048944/rho-kinase-inhibitors-a-patent-review-2014-2016
#2
Olivier Defert, Sandro Boland
The Rho-kinases (ROCK), ROCK1 and ROCK2, are potent, widespread biochemical modulators which have been extensively studied. Due to the involvement of ROCKs in multiple biological processes, ROCK inhibitors have pleiotropic actions and may be of relevance for a number of therapeutic applications. The drawback is however that their use might be limited by occurrence of side effects. Areas covered: Since the publication of the latest review in 2014, there have been significant advances in the field of ROCK inhibitors...
January 3, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28034288/the-non-genomic-effects-of-the-ppar%C3%AE-%C3%AE-agonist-gw0742-on-stz-treated-rat-aorta
#3
Noelia Perez-Diaz, Igor Pushkarskya, Nadia Oweisa, Lisa A Lionea, Louise S Mackenzie
BACKGROUND: The ubiquitous nuclear receptor PPARβ/δ is increasingly being studied in regards to numerous diseases including diabetes following on the finding that PPARβ/δ agonist GW0742 controls Type 1 Diabetes in rats. Studies have shown that GW0742 has off target, non- PPARβ/δ effects in the cell although there are some key questions that remain to be addressed in respect to the significance of this control on vascular tone. METHODS: Using isometric organ baths, rat aorta rings were exposed to ROCK inhibitors and the changes in contraction and dilation measured...
December 29, 2016: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/27998869/-role-of-autophagy-in-fasudil-induced-rho-kinase-inhibition-for-protection-against-myocardial-ischemia-reperfusion-injury-in-rats
#4
Hong-Wei Ye, Ting-Ting Fang, Xiao-Yu Gu, Ya Wang, Guang-Yu Zhu, Ying Yu, Qin Gao
OBJECTIVE: To investigate the changes of autophagy in ischemic myocardium of rats treated with fasudil for inhibiting Rho kinase. METHODS: The hearts isolated from male Sprague-Dawley rats were subjected to 30 min of occlusion of the left anterior descending artery followed by 120 min of reperfusion with or without treatment with fasudil or fasudil+Wort. The left ventricular hemodynamics were continuously recorded, and the coronary effluent was collected during the reperfusion to determine lactate dehydrogenase (LDH) levels...
December 20, 2016: Nan Fang Yi Ke da Xue Xue Bao, Journal of Southern Medical University
https://www.readbyqxmd.com/read/27927737/the-rock-inhibitor-fasudil-prevents-chronic-restraint-stress-induced-depressive-like-behaviors-and-dendritic-spine-loss-in-rat-hippocampus
#5
Gonzalo García-Rojo, Cristóbal Fresno, Natalia Vilches, Gabriela Díaz-Véliz, Sergio Mora, Felipe Aguayo, Aníbal Pacheco, Nicolás Parra-Fiedler, Claudio S Parra, Paulina S Rojas, Macarena Tejos, Esteban Aliaga, Jenny L Fiedler
BACKGROUND: Dendritic arbor simplification and dendritic spine loss in the hippocampus -a limbic structure implicated in mood disorders- are assumed to contribute to symptoms of depression. These morphological changes imply changes in dendritic cytoskeleton. Rho GTPases are regulators of actin dynamics through their effector Rho kinase (ROCK). We have reported that chronic stress promotes depressive-like behaviors in rats, along with dendritic spine loss in apical dendrites of hippocampal pyramidal neurons; changes associated with ROCK activation...
December 7, 2016: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27919951/rho-associated-protein-kinase-rock-inhibitors-inhibit-survivin-expression-and-sensitize-pancreatic-cancer-stem-cells-to-gemcitabine
#6
Hiroyuki Takeda, Masashi Okada, Shuhei Suzuki, Kenta Kuramoto, Hirotsugu Sakaki, Hikaru Watarai, Tomomi Sanomachi, Shizuka Seino, Takashi Yoshioka, Chifumi Kitanaka
BACKGROUND: Targeting pathways regulating survivin expression, which has been implicated in multidrug resistance of cancer cells, is a promising strategy to overcome cancer chemoresistance. To date, the role of rho-associated protein kinases (ROCKs) in survivin expression remains largely unknown. MATERIALS AND METHODS: The effects of ROCK inhibitors Y-27632 and fasudil on survivin expression and cell viability were determined by immunoblot analysis and dye exclusion, respectively, in PANC-1 CSLC, a cancer stem cell line derived from a serum-cultured, gemcitabine-sensitive pancreatic cancer cell line, PANC-1...
2016: Anticancer Research
https://www.readbyqxmd.com/read/27879448/rhoa-kinase-inhibition-with-fasudil-versus-simvastatin-in-murine-models-of-cerebral-cavernous-malformations
#7
Robert Shenkar, Changbin Shi, Cecilia Austin, Thomas Moore, Rhonda Lightle, Ying Cao, Lingjiao Zhang, Meijing Wu, Hussein A Zeineddine, Romuald Girard, David A McDonald, Autumn Rorrer, Carol Gallione, Peter Pytel, James K Liao, Douglas A Marchuk, Issam A Awad
BACKGROUND AND PURPOSE: We sought to compare the effect of chronic treatment with commonly tolerated doses of Fasudil, a specific RhoA kinase (ROCK) inhibitor, and simvastatin (with pleiotropic effects including ROCK inhibition) on cerebral cavernous malformation (CCM) genesis and maturation in 2 models that recapitulate the human disease. METHODS: Two heterozygous murine models, Ccm1(+/-)Msh2(-)(/-) and Ccm2(+/-)Trp53(-/-), were treated from weaning to 4 to 5 months of age with Fasudil (100 mg/kg per day), simvastatin (40 mg/kg per day) or with placebo...
January 2017: Stroke; a Journal of Cerebral Circulation
https://www.readbyqxmd.com/read/27856608/reversal-of-bone-marrow-mobilopathy-and-enhanced-vascular-repair-by-angiotensin-1-7-in-diabetes
#8
Goutham Vasam, Shrinidh Joshi, Sean E Thatcher, Stephen H Bartelmez, Lisa A Cassis, Yagna Pr Jarajapu
Ang-(1-7)/MasR pathway activates vascular repair-relevant functions of bone marrow progenitor cells. We tested the effects of Ang-(1-7) on mobilization and vasoreparative functions of progenitor cells that are impaired in diabetes. Study was carried out in streptozotocin-induced diabetic or db/db mice. Diabetes resulted in decreased number of Lineage(-) Sca-1(+) c-Kit(+) (LSK) cells in the circulation, which was normalized by Ang-(1-7). Diabetes-induced depletion of LSK cells in the bone marrow was reversed by Ang-(1-7)...
November 17, 2016: Diabetes
https://www.readbyqxmd.com/read/27825961/repression-of-microrna-function-mediates-inflammation-associated-colon-tumorigenesis
#9
Takeshi Yoshikawa, Jianfeng Wu, Motoyuki Otsuka, Takahiro Kishikawa, Nobumi Suzuki, Akemi Takata, Motoko Ohno, Rei Ishibashi, Mari Yamagami, Ryo Nakagawa, Naoya Kato, Masaaki Miyazawa, Jiahuai Han, Kazuhiko Koike
BACKGROUND & AIMS: Little is known about the mechanisms by which chronic inflammation contributes to carcinogenesis, such as the development of colon tumors in patients with inflammatory bowel diseases. Specific microRNA (miRNAs) can function as suppressors or oncogenes, and widespread alterations in miRNA expression have been associated with tumorigenesis. We studied whether alterations in miRNA function contribute to inflammation-associated colon carcinogenesis. METHODS: We studied the effects of inflammatory cytokines, such as tumor necrosis factor, interleukin-1α (IL1A), and IL1β (IL1B), on miRNA function, measured by activity of reporter constructs containing miRNA-binding sites in their 3' untranslated regions, in human 293T embryonic kidney, Caco-2, HT29, and HCT116 colon carcinoma cells, as well as dicer(+/+) and dicer(-/-), and Apobec3(+/+) and Apobec3(-/-) mouse embryonic fibroblasts...
November 5, 2016: Gastroenterology
https://www.readbyqxmd.com/read/27795403/the-andes-virus-nucleocapsid-protein-directs-basal-endothelial-cell-permeability-by-activating-rhoa
#10
Elena E Gorbunova, Matthew J Simons, Irina N Gavrilovskaya, Erich R Mackow
: Andes virus (ANDV) predominantly infects microvascular endothelial cells (MECs) and nonlytically causes an acute pulmonary edema termed hantavirus pulmonary syndrome (HPS). In HPS patients, virtually every pulmonary MEC is infected, MECs are enlarged, and infection results in vascular leakage and highly lethal pulmonary edema. We observed that MECs infected with the ANDV hantavirus or expressing the ANDV nucleocapsid (N) protein showed increased size and permeability by activating the Rheb and RhoA GTPases...
October 25, 2016: MBio
https://www.readbyqxmd.com/read/27791202/fasudil-an-inhibitor-of-rho-associated-coiled-coil-kinase-improves-cognitive-impairments-induced-by-smoke-exposure
#11
Deng Xueyang, Ma Zhanqiang, Ma Chunhua, Hao Kun
The current study was designed to investigate the pathological changes in brain induced by smoke exposure, and explore whether fasudil could alleviate these impairments.Adult C57BL/6 mice were exposed to tobacco smoking for four months, and fasudil was treated from the third months. To investigate lung injuries, the immunohistochemistry of lung tissue, immune cell infiltrations, cytokine productions in bronchoalveolar lavage (BAL) fluid, and seurm inflammatory cytokines were evaluated. To investigate cognitive impairments, Morris water maze test, hippocampal inflammatory cytokines and Rho associated signaling pathways were evaluated...
October 24, 2016: Oncotarget
https://www.readbyqxmd.com/read/27760762/endothelin-1-rho-kinase-interactions-impair-lung-structure-and-cause-pulmonary-hypertension-after-bleomycin-exposure-in-neonatal-rat-pups
#12
Jason Gien, Nancy Tseng, Gregory Seedorf, Katherine Kuhn, Steven H Abman
Bronchopulmonary dysplasia (BPD) is the chronic lung disease associated with premature birth, characterized by impaired vascular and alveolar growth. In neonatal rats bleomycin decreases lung growth and causes pulmonary hypertension (PH), which is poorly responsive to nitric oxide. In the developing lung, through Rho kinase (ROCK) activation, ET-1 impairs endothelial cell function; however, whether ET-1-ROCK interactions contribute to impaired vascular and alveolar growth in experimental BPD is unknown. Neonatal rats were treated daily with intraperitoneal bleomycin with and without selective ETA (BQ123/BQ610) and ETB (BQ788) receptor blockers, nonselective ET receptor blocker (ETRB) (bosentan), or fasudil (ROCK inhibitor)...
December 1, 2016: American Journal of Physiology. Lung Cellular and Molecular Physiology
https://www.readbyqxmd.com/read/27756191/fasudil-inhibits-tissue-factor-and-plasminogen-activator-inhibitor-1-secretion-by-peripheral-blood-mononuclear-cells-in-capd-patients
#13
Wenning Li, Wen Chen, Maowei Xie, Haiyang Huang, Huiluan Su, Hui Han, Daofa Zhang, Ying Zhang, Xiaohong Yang, Wentan Xu, Yan Su, Wei Wu, Yun Huang, Keying Fu, Jiali Wei
Disturbances in hemostasis are common complications of kidney diseases and correlate well with cardiovascular mortality. Little is known about the effects of fasudil on tissue factor (TF) and plasminogen activator inhibitor-1 (PAI-1) expression in peripheral blood mononuclear cells (PBMCs) in CAPD patients. PBMCs were isolated from 13 individuals with CAPD and 13 healthy subjects. After 4 h of incubation with or without LPS (10 ng/mL), TF and PAI-1 mRNA of PBMCs were detected by RT-PCR. The levels of TF and PAI-1 in culture supernatants of PBMCs were determined by ELISA...
October 2016: Renal Failure
https://www.readbyqxmd.com/read/27753928/os-05-03-decreased-rho-kinase-based-calcium-sensitization-in-hypertensive-ren-2-transgenic-rats-tgr
#14
Josef Zicha, Michal Behuliak, Ivana Vaneckova
OBJECTIVE: Comparing BP response to Ca channel opener BAY K8644 prior and after Rho kinase inhibition we demonstrated lowered calcium sensitization in spontaneously hypertensive rats (SHR), although BP response of intact SHR to Rho kinase inhibitor fasudil was enhanced (Behuliak et al. J Hypertens 31:2025,2013). The aim of the present study was to evaluate calcium sensitization in hypertensive TGR and their normotensive HanSD controls using the same methods. We also tried to elucidate the interference of baroreflex-activated sympathetic activity with BP response to fasudil...
September 2016: Journal of Hypertension
https://www.readbyqxmd.com/read/27743639/protective-effect-of-inhaled-rho-kinase-inhibitor-on-lung-ischemia-reperfusion-injury
#15
Keiji Ohata, Toyofumi F Chen-Yoshikawa, Toshi Menju, Ei Miyamoto, Satona Tanaka, Mamoru Takahashi, Hideki Motoyama, Kyoko Hijiya, Akihiro Aoyama, Hiroshi Date
BACKGROUND: Rho-kinase, an intracellular serine/threonine kinase, is a key regulator of cytoskeletal dynamics. Recent studies have demonstrated that Rho-kinase is involved in the ischemia-reperfusion injury (IRI) pathogenesis of many organs; however, its involvement with lung IRI remains unclear. This study assessed the association of Rho-kinase with lung IRI and evaluated the protective effect of inhaled Rho-kinase inhibitors in lung IRI. METHODS: The study included isolated rat lung perfusion models, divided into three groups: sham, Rho-kinase inhibitor, and warm ischemia (n = 6 each)...
October 12, 2016: Annals of Thoracic Surgery
https://www.readbyqxmd.com/read/27693712/design-of-efficient-computational-workflows-for-in-silico-drug-repurposing
#16
Quentin Vanhaelen, Polina Mamoshina, Alexander M Aliper, Artem Artemov, Ksenia Lezhnina, Ivan Ozerov, Ivan Labat, Alex Zhavoronkov
Here, we provide a comprehensive overview of the current status of in silico repurposing methods by establishing links between current technological trends, data availability and characteristics of the algorithms used in these methods. Using the case of the computational repurposing of fasudil as an alternative autophagy enhancer, we suggest a generic modular organization of a repurposing workflow. We also review 3D structure-based, similarity-based, inference-based and machine learning (ML)-based methods. We summarize the advantages and disadvantages of these methods to emphasize three current technical challenges...
September 28, 2016: Drug Discovery Today
https://www.readbyqxmd.com/read/27677924/selective-activation-of-vascular-kv-7-4-kv-7-5-k-channels-by-fasudil-contributes-to-its-vasorelaxant-effect
#17
Xuan Zhang, Hailong An, Junwei Li, Yuanyuan Zhang, Yang Liu, Zhanfeng Jia, Wei Zhang, Li Chu, Hailin Zhang
BACKGROUND AND PURPOSE: Kv 7 (Kv 7.1-7.5) channels play an important role in the regulation of neuronal excitability and the cardiac action potential. Growing evidence suggests Kv 7.4/Kv 7.5 channels play a crucial role in regulating vascular smooth muscle contractility. Most of the reported Kv 7 openers have shown poor selectivity across these five subtypes. In this study, fasudil - a drug used for cerebral vasospasm - has been found to be a selective opener of Kv 7.4/Kv 7.5 channels...
December 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27672026/central-angiotensin-ii-increases-blood-pressure-and-sympathetic-outflow-via-rho-kinase-activation-in-conscious-rabbits
#18
Peter R Pellegrino, Alicia M Schiller, Karla K V Haack, Irving H Zucker
Elevated sympathetic tone and activation of the renin-angiotensin system are pathophysiologic hallmarks of hypertension, and the interactions between these systems are particularly deleterious. The importance of Rho kinase as a mediator of the effects of angiotensin-II (AngII) in the periphery is clear, but the role of Rho kinase in sympathoexcitation caused by central AngII is not well established. We hypothesized that AngII mediates its effects in the brain by the activation of the RhoA/Rho kinase pathway...
November 2016: Hypertension
https://www.readbyqxmd.com/read/27671802/endothelial-repair-in-stented-arteries-is-accelerated-by-inhibition-of-rho-associated-protein-kinase
#19
Sarah T Hsiao, Tim Spencer, Luke Boldock, Svenja Dannewitz Prosseda, Ioannis Xanthis, Francesco J Tovar-Lopez, Heleen M M Van Beusekom, Ramzi Y Khamis, Nicolas Foin, Neil Bowden, Adil Hussain, Alex Rothman, Victoria Ridger, Ian Halliday, Cecile Perrault, Julian Gunn, Paul C Evans
AIMS: Stent deployment causes endothelial cells (EC) denudation, which promotes in-stent restenosis and thrombosis. Thus endothelial regrowth in stented arteries is an important therapeutic goal. Stent struts modify local hemodynamics, however the effects of flow perturbation on EC injury and repair are incompletely understood. By studying the effects of stent struts on flow and EC migration, we identified an intervention that promotes endothelial repair in stented arteries. METHODS AND RESULTS: In vitro and in vivo models were developed to monitor endothelialization under flow and the influence of stent struts...
December 2016: Cardiovascular Research
https://www.readbyqxmd.com/read/27643321/os-05-03-decreased-rho-kinase-based-calcium-sensitization-in-hypertensive-ren-2-transgenic-rats-tgr
#20
Josef Zicha, Michal Behuliak, Ivana Vaneckova
OBJECTIVE: Comparing BP response to Ca channel opener BAY K8644 prior and after Rho kinase inhibition we demonstrated lowered calcium sensitization in spontaneously hypertensive rats (SHR), although BP response of intact SHR to Rho kinase inhibitor fasudil was enhanced (Behuliak et al. J Hypertens 31:2025,2013). The aim of the present study was to evaluate calcium sensitization in hypertensive TGR and their normotensive HanSD controls using the same methods. We also tried to elucidate the interference of baroreflex-activated sympathetic activity with BP response to fasudil...
September 2016: Journal of Hypertension
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