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https://www.readbyqxmd.com/read/29166726/-interaction-between-trpc1-and-stim1-in-calcium-sensing-receptor-mediated-calcium-influx-and-nitric-oxide-production-in-human-umbilical-vein-endothelial-cells
#1
L M Wang, H Zhong, N Tang, L J Pang, C J Zhang, F He
Objective: To investigate the interaction of Ca(2+) protein TRPC1 and STIM1 in extracellular Ca(2+) -sensing receptor (CaR)-induced extracellular Ca(2+) influx and the production of nitric oxide (NO). Methods: Human umbilical vein endothelial cells (HUVECs) were cultured and incubated with CaR agonist spermine (activating store-operates cation channels (SOC) and receptor-operated channels (ROC)), CaR negative allosteric modulator Calhex231 (blocking SOC, activating ROC) and ROC analogue TPA (activating ROC, blocking SOC), protein kinase C (PKC) inhibitor Ro31-8220, PKCs and PKCμ inhibitor Go6967(activate SOC, blocking ROC), respectively...
November 24, 2017: Zhonghua Xin Xue Guan Bing za Zhi
https://www.readbyqxmd.com/read/29166711/-effects-of-caspase-1-inhibitor-vx765-on-cold-restraint-stress-induced-acute-gastric-ulcer-in-mice
#2
S Q Zheng, X D Hong, T S Chen, P F Luo, S C Xiao
Objective: To investigate the protective effects of caspase-1 inhibitor VX765 on gastric mucosa of mice with cold-restraint stress-induced acute gastric ulcer. Methods: Twenty-four specific pathogen free male C57BL/6J mice were divided into normal control group (NC), cold restrain group (CR), VX765 pre-treatment+ cold restrain group (VCR), and rabeprazole pre-treatment+ cold restrain group (RCR) according to the random number table, with 6 mice in each group. Mice in group NC were injected intraperitoneally with solution of 10 mL/kg dimethylsulfoxide (DMSO) and phosphate buffer solution (PBS)...
November 20, 2017: Zhonghua Shao Shang za Zhi, Zhonghua Shaoshang Zazhi, Chinese Journal of Burns
https://www.readbyqxmd.com/read/29166668/interleukin-36%C3%AE-and-il-36-receptor-signaling-mediate-impaired-host-immunity-and-lung-injury-in-cytotoxic-pseudomonas-aeruginosa-pulmonary-infection-role-of-prostaglandin-e2
#3
Tetsuji Aoyagi, Michael W Newstead, Xianying Zeng, Yuta Nanjo, Marc Peters-Golden, Mitsuo Kaku, Theodore J Standiford
Pseudomonas aeruginosa is a Gram-negative pathogen that can lead to severe infection associated with lung injury and high mortality. The interleukin (IL)-36 cytokines (IL-36α, IL-36β and IL-36γ) are newly described IL-1 like family cytokines that promote inflammatory response via binding to the IL-36 receptor (IL-36R). Here we investigated the functional role of IL-36 cytokines in the modulating of innate immune response against P. aeruginosa pulmonary infection. The intratracheal administration of flagellated cytotoxic P...
November 22, 2017: PLoS Pathogens
https://www.readbyqxmd.com/read/29166609/gpr56-adgrg1-inhibits-mesenchymal-differentiation-and-radioresistance-in-glioblastoma
#4
Marta Moreno, Leire Pedrosa, Laia Paré, Estela Pineda, Leire Bejarano, Josefina Martínez, Veerakumar Balasubramaniyan, Ravesanker Ezhilarasan, Naveen Kallarackal, Sung-Hak Kim, Jia Wang, Alessandra Audia, Siobhan Conroy, Mercedes Marin, Teresa Ribalta, Teresa Pujol, Antoni Herreros, Avelina Tortosa, Helena Mira, Marta M Alonso, Candelaria Gómez-Manzano, Francesc Graus, Erik P Sulman, Xianhua Piao, Ichiro Nakano, Aleix Prat, Krishna P Bhat, Núria de la Iglesia
A mesenchymal transition occurs both during the natural evolution of glioblastoma (GBM) and in response to therapy. Here, we report that the adhesion G-protein-coupled receptor, GPR56/ADGRG1, inhibits GBM mesenchymal differentiation and radioresistance. GPR56 is enriched in proneural and classical GBMs and is lost during their transition toward a mesenchymal subtype. GPR56 loss of function promotes mesenchymal differentiation and radioresistance of glioma initiating cells both in vitro and in vivo. Accordingly, a low GPR56-associated signature is prognostic of a poor outcome in GBM patients even within non-G-CIMP GBMs...
November 21, 2017: Cell Reports
https://www.readbyqxmd.com/read/29166595/positive-and-negative-regulation-of-the-master-metabolic-regulator-mtorc1-by-two-families-of-legionella-pneumophila-effectors
#5
Justin A De Leon, Jiazhang Qiu, Christopher J Nicolai, Jessica L Counihan, Kevin C Barry, Li Xu, Rosalie E Lawrence, Brian M Castellano, Roberto Zoncu, Daniel K Nomura, Zhao-Qing Luo, Russell E Vance
All pathogens must acquire nutrients from their hosts. The intracellular bacterial pathogen Legionella pneumophila, the etiological agent of Legionnaires' disease, requires host amino acids for growth within cells. The mechanistic target of rapamycin complex 1 (mTORC1) is an evolutionarily conserved master regulator of host amino acid metabolism. Here, we identify two families of translocated L. pneumophila effector proteins that exhibit opposing effects on mTORC1 activity. The Legionella glucosyltransferase (Lgt) effector family activates mTORC1, through inhibition of host translation, whereas the SidE/SdeABC (SidE) effector family acts as mTORC1 inhibitors...
November 21, 2017: Cell Reports
https://www.readbyqxmd.com/read/29166574/altered-tnf-%C3%AE-response-by-aconibal-%C3%A2-and-methotrexate-in-a-lipopolysaccharide-induced-setting-of-inflammatory-conditions-potential-on-a-synergistic-combination
#6
Gunhyuk Park, Seoung Hoon Lee, Ji-Ye Han, Dal-Seok Oh
ETHNOPHARMACOLOGICAL RELEVANCE: Aconitum carmichaelii (AC) is a common herbal medicine used as anti-inflammatory and analgesic agent in Eastern Asia. In Korea, a commercial processed AC (Aconibal(®)) is traditionally used to treat the symptoms of spondylosis deformans and rheumatic pain. AIM OF STUDY: Rheumatoid arthritis (RA) is systemic and auto-immune disease characterized by chronic inflammation. Methotrexate (MTX) is often the first-line therapy for RA. If MTX monotherapy is ineffective or RA is initially severe, adding a tumor necrosis factor (TNF)-α inhibitor to the treatment can be beneficial...
November 19, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29166018/discovery-of-small-molecule-inhibitors-of-ubiquitin-specific-protease-7-usp7-using-integrated-nmr-and-in-silico-techniques
#7
Paola Di Lello, Richard Pastor, Jeremy M Murray, Robert A Blake, Frederick Cohen, Terry D Crawford, Joy Drobnick, Jason Drummond, Lorna Kategaya, Tracy Kleinheinz, Till Maurer, Lionel Rouge, Xianrui Zhao, Ingrid Wertz, Chudi Ndubaku, Vickie Tsui
USP7 is a deubiquitinase implicated in destabilizing the tumor suppressor p53 and for this reason it has gained increasing attention as a potential oncology target for small molecule inhibitors. Herein we describe the biophysical, biochemical and computational approaches that led to the identification of 4-(2-aminopyridin-3-yl)-phenol compounds described by Kategaya et al.1 as specific inhibitors of USP7. Fragment based lead discovery (FBLD) by NMR combined with virtual screening and re-mining of biochemical high-throughput screening (HTS) hits led to the discovery of a series of ligands that bind in the "palm" region of the catalytic domain of USP7 and inhibit its catalytic activity...
November 22, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29165873/andrographolide-inhibits-hypoxia-induced-hypoxia-inducible-factor-1%C3%AE-and-endothelin-1-expression-through-the-heme-oxygenase-1-co-cgmp-mkp-5-pathways-in-ea-hy926-cells
#8
Hung-Chih Lin, Shih-Li Su, Wan-Chun Lin, Ai-Hsuan Lin, Ya-Chen Yang, Chong-Kuei Lii, Haw-Wen Chen
Andrographolide is a potent anti-inflammatory agent found in Andrographis paniculata. Endothelin 1 (ET-1) is an endothelium-derived vasoconstrictor with pro-inflammatory properties secreted in response to hypoxia. Mitogen-activated protein kinase phosphatase 5 (MKP-5) is a dual-specificity phosphatase that dephosphorylates threonine and tyrosine residues of MAPKs. We showed previously that hypoxia-induced HIF-1α expression and ET-1 secretion are dependent on p38 MAPK in EA.hy926 cells. Here, we investigate what role MKP-5 plays in andrographolide's inhibition of hypoxia-induced expression of HIF-1α and ET-1...
November 22, 2017: Environmental Toxicology
https://www.readbyqxmd.com/read/29165795/therapeutic-potency-of-mtor-signaling-pharmacological-inhibitors-in-the-treatment-of-proinflammatory-diseases-current-status-and-perspectives
#9
REVIEW
Arash Soltani, Amirhossein Bahreyni, Nadia Boroumand, Mostafa Karimi Roshan, Majid Khazaei, Mikhail Ryzhikov, Saman Soleimanpour, Amir Avan, Seyed Mahdi Hassanian
Mammalian target of rapamycin (mTOR) signaling pathway controls cell energy metabolism. There is an interplay between mTOR and proinflammatory signaling pathways, supporting the role of the pathway in the pathogenesis of inflammatory diseases. Inhibition of mTOR signaling using specific pharmacological inhibitors could offer therapeutic promise in several inflammatory-associated diseases. In this review, we summarize recent findings on the regulatory effects of mTOR signaling on inflammation and the therapeutic potency of mTOR pharmacological inhibitors in the treatment of inflammatory diseases including cancer, neurodegenerative diseases, atherosclerosis, sepsis and rheumatoid arthritis for a better understanding and hence a better management of these diseases...
November 22, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/29165747/the-effect-of-rosmarinus-officinalis-and-chemotherapeutic-etoposide-on-glioblastoma-u87-mg-cell-culture
#10
Meryem Damla Özdemir, Dilek Göktürk
AIM: Glioblastoma (GBM) is the most invasive and common type of brain cancer with very poor prognosis. One of the drugs administered for GBM pharmacotherapy is etoposide (VP-16), which belongs to the topoisomerase inhibitor family. It can be used in combination with other drugs or chemicals to avoid high dose toxicities or augment its effect at lower doses. In this study we aimed to investigate whether high dose toxicities of etoposide can be overcome when used in combination with a natural compound named Rosmarinus Officinalis...
October 11, 2017: Turkish Neurosurgery
https://www.readbyqxmd.com/read/29165716/targeting-bcr-abl-independent-tki-resistance-in-chronic-myeloid-leukemia-by-mtor-and-autophagy-inhibition
#11
Rebecca Mitchell, Lisa E M Hopcroft, Pablo Baquero, Elaine K Allan, Kay Hewit, Daniel James, Graham Hamilton, Arunima Mukhopadhyay, Jim O'Prey, Alan Hair, Junia V Melo, Edmond Chan, Kevin M Ryan, Véronique Maguer-Satta, Brian J Druker, Richard E Clark, Subir Mitra, Pawel Herzyk, Franck E Nicolini, Paolo Salomoni, G Vignir Helgason
Background: Imatinib and second-generation tyrosine kinase inhibitors (TKIs) nilotinib and dasatinib have statistically significantly improved the life expectancy of chronic myeloid leukemia (CML) patients; however, resistance to TKIs remains a major clinical challenge. Although ponatinib, a third-generation TKI, improves outcomes for patients with BCR-ABL-dependent mechanisms of resistance, including the T315I mutation, a proportion of patients may have or develop BCR-ABL-independent resistance and fail ponatinib treatment...
November 20, 2017: Journal of the National Cancer Institute
https://www.readbyqxmd.com/read/29165700/epigenetic-therapy-novel-translational-implications-for-arrest-of-environmental-dioxin-induced-disease-in-females
#12
Zaraq Khan, Ye Zheng, Tiffanny L Jones, Abigail A Delaney, Luiz F Correa, Chandra C Shenoy, Khashayarsha Khazaie, Gaurang S Daftary
Increased toxicant exposure and resultant environmentally-induced diseases are a tradeoff of industrial productivity. Dioxin (TCDD: 2,3,7,8 tetrachlorodibenzo-p-dioxin), a ubiquitous by-product is associated with a spectrum of diseases including endometriosis, a common, chronic disease in women. TCDD activates cytochrome p450 (CYP) metabolic enzymes, which alters organ function to cause disease. In contrast, the transcription factor, Krüppel-Like Factor (KLF) 11 represses these enzymes via epigenetic mechanisms...
November 17, 2017: Endocrinology
https://www.readbyqxmd.com/read/29165597/gsta1-expression-is-correlated-with-aldosterone-level-in-kcnj5-mutated-adrenal-aldosterone-producing-adenoma
#13
Xintao Li, Baojun Wang, Lu Tang, Yu Zhang, Luyao Chen, Liangyou Gu, Fan Zhang, Jinzhi Ouyang, Xu Zhang
Context: KCNJ5 mutation is a major cause of aldosterone-producing adenoma (APA). The development of APA apart from KCNJ5 mutation is less investigated. Objective: To investigate other mechanisms affecting aldosterone secretion apart from KCNJ5. Patients and Methods: Six pairs of KCNJ5-mutated, high and low aldosterone-secreting APAs, five non-KCNJ5-mutated APAs and four normal adrenal glands were assayed by Affymetrix Genechip Human Transcriptome Array 2...
November 20, 2017: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/29165430/subcutaneous-administration-of-infliximab-attenuated-silica-induced-lung-fibrosis
#14
Hua Zhang, Jun-Na Sui, Lei Gao, Jian Guo
OBJECTIVES: To investigate the influence of the anti-tumor necrosis factor-α infliximab (IFX) in the case of rats with silicosis. MATERIAL AND METHODS: Forty-eight Wistar rats were randomly divided into 3 groups. The study group (N = 16) - silicosis was induced by intratracheal instillation of 50 mg silica on day 1, and IFX was subcutaneously administered at a dose of 15 mg/kg of body weight from day 2 to day 6, the vehicle group (N = 16) - silica used as the study group but without IFX, the sham group (N = 16) - 1 ml of saline was intratracheal-used...
November 21, 2017: International Journal of Occupational Medicine and Environmental Health
https://www.readbyqxmd.com/read/29165315/an-expression-screen-for-aged-dependent-micrornas-identifies-mir-30a-as-a-key-regulator-of-aging-features-in-human-epidermis
#15
Charlotte Muther, Lara Jobeili, Maëlle Garion, Sandrine Heraud, Amélie Thepot, Odile Damour, Jérôme Lamartine
The mechanisms affecting epidermal homeostasis during aging remain poorly understood. To identify age-related microRNAs, a class of non-coding RNAs known to play a key role in the regulation of epidermal homeostasis, an exhaustive miRNA expression screen was performed in human keratinocytes from young or elderly subjects. Many microRNAs modulated by aging were identified, including miR-30a, in which both strands were overexpressed in aged cells and epidermal tissue. Stable MiR-30a over-expression strongly impaired epidermal differentiation, inducing severe barrier function defects in an organotypic culture model...
November 19, 2017: Aging
https://www.readbyqxmd.com/read/29165090/inhibition-of-adipogenesis-by-thiourea-derivatives
#16
Hina Siddiqui, Sarah Shafi, Farah Mukhtar, Asma Ejaz, Atta-Ur-Rahman, M Iqbal Choudhary
BACKGROUND: Obesity is one of the major health problem with inherent risk of type 2 diabetes, hypertension, CVDs etc. Adipogenesis is a major contributor in the process of obesity. Inhibition of adipocytes is one of the key approach to treat obesity. OBJECTIVE: To discover the new inhibitors of adipogenesis as the treatment for the obesity. METHOD: We describe here the synthesis and anti-adipogenic activity of thiourea derivatives 1-14. These derivatives were synthesized by the reactions of phenyl and pentafluorophenyl isothiocyanate with different aromatic amines...
November 20, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/29165070/bortezomib-in-kidney-transplant-current-use-and-perspectives
#17
Erika B Rangel, Lucio R Requião-Moura, Taina V de Sandes-Freitas, Gessika Marcelo-Gomes
BACKGROUND: Despite major advances in transplant medicine, antibody-mediated rejection (AMR) continues to have severe clinical implications and adversely affect graft survival. Therefore, the search for alternative drugs to treat AMR is widely pursued. The first-in-class proteasome inhibitor bortezomib (BZ) is a selective inhibitor of the 26S proteasome, which was initially approved for the treatment of malignant plasma cell disorders. METHODS: This review encompasses how our understanding of inhibiting proteasome pathway created the basis of BZ research and important milestones accomplished in AMR treatment in the transplant setting...
November 20, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/29164984/salvianolic-acid-a-a-novel-pi3k-akt-inhibitor-induces-cell-apoptosis-and-suppresses-tumor-growth-in-acute-myeloid-leukemia
#18
Renzhi Pei, Ting Si, Ying Lu, Jeff Xiwu Zhou, Lei Jiang
Salvianolic acid A (SAA), one of the main derivatives of Salvia miltiorrhiza, has been shown to possess anti-inflammatory and anti-thrombotic activities. Its role in inhibiting tumor growth, however, remains elusive. The aim of this study was to investigate the effect of SAA on acute myeloid leukemia (AML). Here, SAA showed a dose-dependent cell viability inhibition and apoptosis induction in AML cells. At the molecular level, SAA increased the expression of Bak and decreased the expression of Bcl-xL, following by PARP cleavage and caspase-3 activation...
November 22, 2017: Leukemia & Lymphoma
https://www.readbyqxmd.com/read/29164965/the-importance-of-flt3-mutational-analysis-in-acute-myeloid-leukemia
#19
Mrinal M Patnaik
Activating mutations in FMS-like tyrosine kinase 3 (FLT3), including internal tandem duplications (ITDs) and tyrosine kinase domain (TKD) mutations, are common in patients with acute myeloid leukemia (AML). FLT3-ITD is a negative prognostic factor that remains prognostically relevant even after intensive chemotherapy and/or stem cell transplant. FLT3 testing was historically viewed as being purely prognostic; however, with the advent of FLT3 inhibitors, it will likely be seen as both prognostic and predictive...
November 22, 2017: Leukemia & Lymphoma
https://www.readbyqxmd.com/read/29164831/udenafil-a-phosphodiesterase-5-inhibitor-reduces-body-weight-in-high-fat-fed-mice
#20
Seong Yul Ryu, Yoon Jung Choi, So Young Park, Jong Yeon Kim, Yong Dae Kim, Yong Woon Kim
PURPOSE: High-fat (HF) feeding induces hypothalamic leptin resistance via the activation of toll-like receptor 4 (TLR4). TLR4 deficiency confers resistance to diet-induced obesity. Udenafil, an anti-impotence drug, inhibits TLR4 in airway epithelial cells in vitro. In this study, we evaluated whether udenafil suppressed the hypothalamic expression of TLR4 and reduced body weight. MATERIALS AND METHODS: The hypothalamic expression of TLR4, phosphodiesterase 5 (PDE5), nuclear factor-κB (NF-κB), and myeloid differentiation primary response gene 88 (Myd88) was analyzed by real-time polymerase chain reaction after treating mice for 2 days with udenafil (0, 12, 120, or 600 μg/d)...
November 16, 2017: World Journal of Men's Health
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