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https://www.readbyqxmd.com/read/28632992/targeting-the-rhogtpase-rock-pathway-for-the-treatment-of-vhl-hif-pathway-driven-cancers
#1
Jordan M Thompson, Jaime Landman, Olga V Razorenova
The loss of the von Hippel-Lindau (VHL) tumor-suppressor is a major driver of Clear Cell Renal Cell Carcinoma (CC-RCC) resulting in the stabilization and overactivation of hypoxia inducible factors (HIFs). ROCK 1 is a well-known protein serine/threonine kinase which is recognized as having a role in cancer including alterations in cell motility, metastasis and angiogenesis. As a function of the later effect, we recently investigated and identified a synthetic lethal interaction between VHL loss and ROCK1 inhibition in CC-RCC that is dependent on HIF overactivation...
June 20, 2017: Small GTPases
https://www.readbyqxmd.com/read/28609185/discovery-and-preclinical-development-of-netarsudil-a-novel-ocular-hypotensive-agent-for-the-treatment-of-glaucoma
#2
Cheng-Wen Lin, Bryan Sherman, Lori A Moore, Carmen L Laethem, Da-Wen Lu, Padmanabhan P Pattabiraman, Ponugoti Vasantha Rao, Mitchell A deLong, Casey C Kopczynski
PURPOSE: Rho-associated protein kinase (ROCK) inhibitors lower intraocular pressure (IOP) by increasing aqueous outflow through the trabecular meshwork (TM). The preclinical characterization of netarsudil, a new ROCK/norepinephrine transporter (NET) inhibitor currently in clinical development, is presented herein. METHODS: The kinase inhibitory activity of netarsudil was compared to its esterase metabolite, netarsudil-M1, and 3 other ROCK inhibitors using a commercially available kinase assay kit...
June 13, 2017: Journal of Ocular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28608941/tgf-%C3%AE-stimulates-expression-of-chondroitin-polymerizing-factor-in-nucleus-pulposus-cells-through-the-smad3-rhoa-rock1-and-mapk-signaling-pathways
#3
Bo Hu, Chen Xu, Peng Cao, Ye Tian, Ying Zhang, Changgui Shi, Jun Xu, Wen Yuan, Huajiang Chen
The enzyme chondroitin polymerizing factor (ChPF) is primarily involved in extension of the chondroitin sulfate backbone required for the synthesis of sulfated glycosaminoglycan (sGAG). Transforming growth factor beta (TGF-β) upregulates sGAG synthesis in nucleus pulposus cells; however, the mechanisms mediating this induction are incompletely understood. Our study demonstrated that ChPF expression was negatively correlated with the grade of degenerative intervertebral disc disease. Treatment of nucleus pulposus cells with TGF-β induced ChPF expression and enhanced Smad2/3, RhoA/ ROCK activation, and the JNK, p38 and ERK1/2 MAPK signaling pathways...
June 13, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28598808/mir-199a-b-5p-inhibits-hepatocellular-carcinoma-progression-by-post-transcriptionally-suppressing-rock1
#4
Yangyang Zhan, NanXin Zheng, Fei Teng, Leilei Bao, Fang Liu, Mingjian Zhang, Meng Guo, Wenyuan Guo, Guoshan Ding, Quanxing Wang
In this study, we explored the actions of miR-199a/b-5p during hepatocellular carcinoma (HCC) progression and its potential target genes. Through heatmap miRNA expression analysis of 15 matched HCC tumor and adjacent non-tumor liver tissues from the TCGA database, we detected 19 mRNAs that were upregulated and 13 that were downregulated specifically in HCC. Among these, miR-199 family members were downregulated in HCC tumors and cell lines, as compared to controls. Low miR-199a/b-5p expression was also associated with poor overall survival of HCC patients...
May 22, 2017: Oncotarget
https://www.readbyqxmd.com/read/28576719/phenolic-derivatives-from-blaps-japanensis-and-their-biological-evaluation
#5
REVIEW
Tao Zheng, Yong-Ming Yan, Zheng-Chao Tu, Qi Luo, Fu-Rong Xu, Yong-Xian Cheng
This study was designed to characterize compounds from two thousands of insects of Blaps japanensis. With this purpose, pipajiains A-C (1-3), three novel phenolic derivatives, pipajiains D (4) and E (5), two new natural occurring compounds, and four known substances were isolated thereof. Their structures were identified by spectroscopic methods. Biological activities of all these compounds towards EV71, tuberculosis, COX-2, ROCK1/2, and JAK3 kinases were evaluated.
May 30, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28558357/long-non-coding-rna-hoxa11-as-functions-as-a-competing-endogenous-rna-to-regulate-rock1-expression-by-sponging-mir-124-3p-in-osteosarcoma
#6
Mingxing Cui, Jingyu Wang, Qingjiang Li, Junlei Zhang, Jinling Jia, Xinli Zhan
Long non-coding RNAs (lncRNAs) have been strongly associated with various types of cancer. this study was to explore the critical role of lncRNA HOXA11-AS in osteosarcoma (OS) progression. Briefly, we should that the expression of HOXA11-AS was upregulated in OS tissues and cell lines. The high expression of HOXA11-AS was associated with advanced clinical stage, distant metastasis and poor overall survival of OS. In addition, We found that HOXA11-AS silencing suppressed OS cells proliferation, invasion and induced cell arrest in G0/G1 phase...
May 27, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28533114/2-aminomethylthieno-3-2-d-pyrimidin-4-3h-ones-bearing-3-methylpyrazole-hinge-binding-moiety-highly-potent-selective-and-time-dependent-inhibitors-of-cdc7-kinase
#7
Osamu Kurasawa, Misaki Homma, Yuya Oguro, Tohru Miyazaki, Kouji Mori, Noriko Uchiyama, Kenichi Iwai, Akihiro Ohashi, Hideto Hara, Sei Yoshida, Nobuo Cho
In order to increase the success rate for developing new Cdc7 inhibitors for cancer therapy, we explored a new chemotype which can comply with the previously-constructed pharmacophore model. Substitution of a pyridine ring of a serendipitously-identified Cdc7 inhibitor 2b with a 3-methylpyrazole resulted in a 4-fold increase in potency and acceptable kinase selectivity, leading to the identification of thieno[3,2-d]pyrimidin-4(3H)-one as an alternative scaffold. Structure-activity relationship (SAR) study revealed that incorporation of a substituted aminomethyl group into the 2-position improved kinase selectivity...
May 2, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28521412/microrna-335-and-its-target-rock1-synergistically-influence-tumor-progression-and-prognosis-in-osteosarcoma
#8
Yong Wang, Ningning Wang, Xiandong Zeng, Jie Sun, Guangbin Wang, Huimian Xu, Wei Zhao
MicroRNA (miR)-335 and Rho-associated serine-threonine protein kinase 1 (Rock1) is ectopically expressed in multiple malignant tumors including osteosarcoma. The present study aimed to clarify whether the combined ectopically expressed miR-335 and Rock1 was correlated with clinicopathological features and prognosis in patients with osteosarcoma. The expression of miR-335 and Rock1 in 91 osteosarcoma tissue samples and 47 noncancerous bone tissues were determined respectively by in situ hybridization and immunohistochemistry...
May 2017: Oncology Letters
https://www.readbyqxmd.com/read/28487419/membrane-depolarization-activates-bk-channels-through-rock-mediated-%C3%AE-1-subunit-surface-trafficking-to-limit-vasoconstriction
#9
M Dennis Leo, Xue Zhai, Padmapriya Muralidharan, Korah P Kuruvilla, Simon Bulley, Frederick A Boop, Jonathan H Jaggar
Membrane depolarization of smooth muscle cells (myocytes) in the small arteries that regulate regional organ blood flow leads to vasoconstriction. Membrane depolarization also activates large-conductance calcium (Ca(2+))-activated potassium (BK) channels, which limits Ca(2+) channel activity that promotes vasoconstriction, thus leading to vasodilation. We showed that in human and rat arterial myocytes, membrane depolarization rapidly increased the cell surface abundance of auxiliary BK β1 subunits but not that of the pore-forming BKα channels...
May 9, 2017: Science Signaling
https://www.readbyqxmd.com/read/28484504/effect-of-qskl-on-mapk-and-rhoa-pathways-in-a-rat-model-of-heart-failure
#10
Kai Xia, Qiyan Wang, Chun Li, Zifan Zeng, Yong Wang, Wei Wang
Qishenkeli (QSKL) is one of the Chinese medicine formulae for treating heart failure and has been shown to have an antifibrotic effect. However, the mechanism of its therapeutic effects remains unclear. In this study, we aimed to explore whether QSKL could exert an antifibrotic effect by attenuating ras homolog family member A (RhoA) and mitogen activated protein kinase (MAPK) pathways. Rats were randomly divided into sham group, model group, QSKL group, and positive control group. Heart failure was induced by ligation of the left ventricle anterior descending artery...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/28454380/mir-150-is-downregulated-in-osteosarcoma-and-suppresses-cell-proliferation-migration-and-invasion-by-targeting-rock1
#11
Chang-Hui Li, Teng-Bo Yu, Hong-Wei Qiu, Xia Zhao, Chuan-Li Zhou, Chao Qi
Osteosarcoma (OS) is the most common form of bone malignancy in children and adolescents. A class of molecules known as microRNAs (miRNAs) have been routinely associated in the development and progression of OS. The present study was centered on the less well-known miRNA, miRNA (miR)-150, and its role in OS was investigated. The levels of miR-150 were examined in 40 tissue specimens from patients with OS and adjacent normal tissues using reverse transcription-quantitative polymerase chain reaction (RT-qPCR) analysis...
April 2017: Oncology Letters
https://www.readbyqxmd.com/read/28450943/clinicopathological-significance-of-rock1-and-pik3ca-expression-in-nasopharyngeal-carcinoma
#12
Xuanyi Wang, Yuxiang Huang, Renhua Guo, Yongbiao Liu, Yayun Qian, Dan Liu, Xiaojun Dai, Zheng Wei, Feng Jin, Yanqing Liu
The aim of the present study was to determine the expression of rho-associated coiled-coil-containing protein kinase 1 (ROCK1) and phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit α (PIK3CA) in nasopharyngeal carcinoma (NPC), and to assess the association between the expression of these proteins and the clinicopathological features of NPC. ROCK1 and PIK3CA expressions were assessed in a tissue microarray of sections prepared from the tumors of 81 patients with NPC using immunohistochemistry...
March 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28438902/crucial-role-of-rock2-mediated-phosphorylation-and-upregulation-of-fhod3-in-the-pathogenesis-of-angiotensin-ii-induced-cardiac-hypertrophy
#13
Qing Zhou, Si-Si Wei, Hong Wang, Qian Wang, Wei Li, Gang Li, Jian-Wen Hou, Xiao-Meng Chen, Jie Chen, Wei-Ping Xu, Yi-Gang Li, Yue-Peng Wang
Cardiac hypertrophy is characterized by increased myofibrillogenesis. Angiotensin II (Ang-II) is an essential mediator of the pressure overload-induced cardiac hypertrophy in part through RhoA/ROCK (small GTPase/Rho-associated coiled-coil containing protein kinase) pathway. FHOD3 (formin homology 2 domain containing 3), a cardiac-restricted member of diaphanous-related formins, is crucial in regulating myofibrillogenesis in cardiomyocytes. FHOD3 maintains inactive through autoinhibition by an intramolecular interaction between its C- and N-terminal domains...
June 2017: Hypertension
https://www.readbyqxmd.com/read/28435089/cobalt-chloride-induces-rhoa-rock-activation-and-remodeling-effect-in-h9c2-cardiomyoblasts-involvement-of-pi3k-akt-and-mapk-pathways
#14
Cheng-I Cheng, Yueh-Hong Lee, Po-Han Chen, Yu-Chun Lin, Ming-Huei Chou, Ying-Hsien Kao
Chronic heart failure is a serious complication of myocardial infarction, one of the major causes of death worldwide that often leads to adverse cardiac hypertrophy and poor prognosis. Hypoxia-induced cardiac tissue remodeling is considered an important underlying etiology. This study aimed to delineate the signaling profiles of RhoA/ROCK, PI3K/Akt, and MAPK and their involvement in regulation of remodeling events in cultured H9c2 cardiomyoblast cells. In addition to its growth-suppressive effect, the hypoxia-mimetic chemical, cobalt chloride (CoCl2) significantly induced RhoA kinase activation as revealed by increased MBS phosphorylation and ROCK1/2 expression in H9c2 cells...
August 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28434818/expression-of-a-kinase-anchor-protein-13-and-rho-associated-coiled-coil-containing-protein-kinase-in-restituted-and-regenerated-mucosal-epithelial-cells-following-mucosal-injury-and-colorectal-cancer-cells-in-mouse-models
#15
Yumi Kangawa, Toshinori Yoshida, Takeshi Tanaka, Akira Kataoka, Naomi Koyama, Tomoka Ohsumi, Shim-Mo Hayashi, Makoto Shibutani
We demonstrate the expression patterns of A-kinase anchor protein 13 (AKAP13), a scaffold protein that acts upstream of Rho signaling, and Rho-associated coiled-coil containing protein kinase (ROCK) 1/2 in mouse colorectal cancer and during the healing stage of mouse colitis. BALB/c mice received an intraperitoneal injection of azoxymethane at 10mg/kg, followed by two 7-day cycles of 3% dextran sulfate sodium (DSS) administered through their drinking water to induce colon cancer, or a 7-day administration of 4% DSS to induce colitis...
April 20, 2017: Experimental and Toxicologic Pathology: Official Journal of the Gesellschaft Für Toxikologische Pathologie
https://www.readbyqxmd.com/read/28415789/hmga2-translocation-induced-in-skin-tumorigenesis
#16
Yong Li, Xiang-Ying Pi, Kelsey Boland, Sonali Lad, Kelly Johnson, Catherine Verfaillie, Rebecca J Morris
Hmga2 protein, a transcription factor involved in chromatin architecture, is expressed chiefly during development, where it has many key biological functions. When expressed in adult tissues from in various organs, Hmga2 is always related to cancer development. The role of Hmga2 in skin tumorigenesis is, however, not yet understood. We demonstrated that Hmga2 can be found in non-transformed epidermis, specifically located to the membrane of keratinocytes (KCs) in epidermis. Ex vivo culture of KCs and development of skin carcinomas in DMBA and TPA mouse models was associated with translocation of the Hmga2 protein from the membrane into the nucleus, where Hmga2 induced its own expression by binding to the Hmga2 promoter...
May 2, 2017: Oncotarget
https://www.readbyqxmd.com/read/28395329/vitamin-d-suppresses-oxidative-stress-induced-microparticle-release-by-human-umbilical-vein-endothelial-cells
#17
Xiuyue Jia, Jie Xu, Yang Gu, Xin Gu, Weimin Li, Yuping Wang
Endothelial microparticle (MP) release was increased in numerous cardiovascular diseases including preeclampsia. Oxidative stress is a potent inducer of endothelial dysfunction. In this study, we aimed to investigate if vitamin D could protect endothelial cells (ECs) from MP release induced by oxidative stress. Endothelial cell (from human umbilical vein) oxidative stress was induced by cultivation of cells under lowered oxygen condition (2%O2) for 48 h and cells cultured under standard condition (21%O2) served as control...
January 1, 2017: Biology of Reproduction
https://www.readbyqxmd.com/read/28373445/pi3k-catalytic-isoform-alteration-promotes-the-limk1-related-metastasis-through-the-pak1-or-rock1-2-activation-in-cigarette-smoke-exposed-ovarian-cancer-cells
#18
Ga Bin Park, Daejin Kim
AIM: To investigate the molecular mechanisms by which long-term exposure to cigarette smoke extract (CSE) contributes to ovarian cancer metastasis. MATERIALS AND METHODS: Western blot analysis for diverse p110 isoforms of phosphoinositide 3-kinase (PI3K)-related signaling pathway and epithelial-mesenchymal transition (EMT) markers was performed to analyze the underlying mechanisms. Migratory activity of CSE-exposed ovarian cancer cells was determined by transendothelial migration and invasion assay...
April 2017: Anticancer Research
https://www.readbyqxmd.com/read/28368445/vitamin-d-reduces-oxidative-stress-induced-procaspase-3-rock1-activation-and-mp-release-by-placental-trophoblasts
#19
Jie Xu, Xiuyue Jia, Yang Gu, David F Lewis, Xin Gu, Yuping Wang
Context: Increased microparticle (MP) shedding by placental trophoblasts contributes to maternal vascular inflammatory response and endothelial dysfunction in preeclampsia. Vitamin D has beneficial effects in pregnancy; however, its effect on trophoblast MP release has not been investigated. Objective: To investigate if vitamin D could protect trophoblasts from oxidative stress-induced MP release. Design: Placental trophoblasts were isolated from uncomplicated and preeclamptic placentas...
June 1, 2017: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28362714/iloprost-prostaglandin-e1-and-papaverine-relax-human-mesenteric-arteries-with-similar-potency
#20
Christoph Mahlke, Jens-Peter Kühn, Birger Mensel, André Schreiber, Annett Juretzko, Antje Steinbach, Olaf Grisk
OBJECTIVE: Non-occlusive mesenteric ischemia (NOMI) is accompanied by mesenteric artery spasms that are at least in part due to endothelin system activation. Acute treatment includes intra-arterial infusion of vasodilators such as iloprost, prostaglandin E1 (PGE1) and papaverine. Their effectiveness is not well characterized in human mesenteric arteries. We directly compared their potency to relax isolated human mesenteric arteries. To explore the potential of Rock inhibition to treat mesenteric artery spasms, we tested if endothelin-1 (ET-1)-induced mesenteric artery constrictions depend rho kinase (Rock)...
March 30, 2017: Shock
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