keyword
MENU ▼
Read by QxMD icon Read
search

Antagonist

keyword
https://www.readbyqxmd.com/read/28645196/antagonistic-regulation-of-cyclin-expression-by-the-bzip-transcription-factors-pcr1-and-atf1-during-g2-m-transition
#1
Sushobhana Bandyopadhyay, Protiti Maiti Ghosh, Sohini Basu, Madhurima Paul, Syed Benazir Alam, Elizabeth Das, Geetanjali Sundaram
The transcription factor Atf1 is known to promote cell survival during various stress conditions in Schizosaccharomyces pombe by activating the expression of appropriate genes. It can also activate transcription of other important genes responsible for cell cycle progression. An Atf1 dependent increase in the expression of cell division promoting genes will oppose activation of checkpoints necessary to ensure repairs and cell survival during stress. Hence selective inhibition of the cell cycle related functions of Atf1 would be indispensable for cellular survival during stress...
June 22, 2017: FEMS Microbiology Letters
https://www.readbyqxmd.com/read/28645128/-headache-news
#2
Hans-Christoph Diener, Charly Gaul, Dagny Holle-Lee, Lazaros Lazaridis, Steffen Nägel, Mark Obermann
A review of the latest and most relevant information on different disorders of head and facial pain is presented. News from epidemiologic studies regarding the relationship between migraine and patent foramen ovale, the cardiovascular risk in migraine, and migraine behavior during menopause, and the development of white matter lesions or migraine genetics are presented. Regarding pathophysiology there are very recent insights regarding the role of the hypothalamus during prodromal phase and the interplay of brain-stem and hypothalamus during the attack...
June 2017: Fortschritte der Neurologie-Psychiatrie
https://www.readbyqxmd.com/read/28645030/uptake-and-tissue-distributions-of-cadmium-selenium-and-zinc-in-striped-marsh-frog-tadpoles-exposed-during-early-post-embryonic-development
#3
Chantal M Lanctôt, Tom Cresswell, Steven D Melvin
Metals and metalloids released through anthropogenic activities can accumulate in aquatic organisms, resulting in adverse effects in sensitive species. We investigated the influence of feeding regime and exposure complexity (i.e., mixture) on bioaccumulation kinetics and body distribution of common metal(loid) pollutants in Limnodynastes peronii during early post-embryonic development. Tadpoles were exposed to radiolabelled (109)Cd, (75)Se and (65)Zn alone and in a mixture for 4 days, followed by 3 days depuration in clean water...
June 20, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/28645008/effect-of-microrna-129-5p-targeting-hmgb1-rage-signaling-pathway-on-revascularization-in-a-collagenase-induced-intracerebral-hemorrhage-rat-model
#4
Xin-Long Ma, Shu-Ya Li, Feng Shang
BACKGROUND: This study aimed at exploring the effect of microRNA-129-5p (miR-129-5p) targeting high mobility group box-1 (HMGB1)-receptor for advanced glycation end-products (RAGE) signaling pathway on the revascularization in a collagenase-induced intracerebral hemorrhage (ICH) rat model. METHODS: OX26-pGFAP-IL, an immunoliposome expressing miR-129-5p was constructed. The collagenase-induced ICH rat models were successfully established by 96 Sprague Dawley (SD) rats, which were categorized into the sham group, ICH group, miR-129-5p group, negative control (NC) group, ethyl pyruvate (EP, an inhibitor of HMGB1) group and N-benzyl-4-chloro-N-cyclohe-xylbenzamide (FPS-ZM1, a RAGE receptor antagonist) group...
June 20, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28644987/thiophene-thiazole-benzene-replacement-on-guanidine-derivatives-targeting-%C3%AE-2-adrenoceptors
#5
Aoife Flood, Cristina Trujillo, Goar Sanchez-Sanz, Brendan Kelly, Carolina Muguruza, Luis F Callado, Isabel Rozas
Searching for improved antagonists of α2-adrenoceptors, a thorough theoretical study comparing the aromaticity of phenyl-, pyridinyl-, thiophenyl- and thiazolylguanidinium derivatives has been carried out [at M06-2X/6-311++G(p,d) computational level] confirming that thiophene and thiazole will be good 'ring equivalents' to benzene in these guanidinium systems. Based on these results, a small but chemically diverse library of guanidine derivatives (15 thiophenes and 2 thiazoles) were synthesised to explore the effect that the bioisosteric change has on affinity and activity at α2-adrenoceptors in comparison with our previously studied phenyl derivatives...
June 6, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28644924/intravenous-thrombolysis-for-acute-ischemic-stroke-a-bridge-between-two-centuries
#6
Georgios Tsivgoulis, Odysseas Kargiotis, Andrei Alexandrov
Intravenous tissue-plasminogen activator (tPA) remains the only approved systemic reperfusion therapy suitable for most patients presenting timely with acute ischemic stroke. Accumulating real-word experience for over 20 years regarding tPA safety and effectiveness lead to re-appraisal of original contraindications for intravenous thrombolysis (IVT). Areas covered: This narrative review focuses on fast yet appropriate selection of patients for safe administration of tPA per recently expanded indications. Novel strategies for rapid patient assessment will be discussed...
June 23, 2017: Expert Review of Neurotherapeutics
https://www.readbyqxmd.com/read/28644912/biofilm-formation-and-disinfectant-resistance-of-salmonella-spp-in-mono-and-dual-species-with-pseudomonas-aeruginosa
#7
Xinyi Pang, Yishan Yang, Hyun-Gyun Yuk
AIMS: This study aimed to evaluate the biofilm formation and disinfectant resistance of Salmonella cells in mono- and dual-species biofilms with Pseudomonas aeruginosa, and to investigate the role of extracellular polymeric substances (EPS) in protection of biofilms against disinfection treatment. METHODS AND RESULTS: The populations of Salmonella in mono- or dual-species biofilms with P. aeruginosa on stainless steel (SS) coupons were determined before and after exposure to commercial disinfectant, 50 μg ml(-1) chlorine or 200 μg ml(-1) Ecolab(®) Whisper(™) V (a blend of four effective quaternary ammonium compounds)...
June 23, 2017: Journal of Applied Microbiology
https://www.readbyqxmd.com/read/28644617/dynamic-covalent-chemistry-of-carbon-dioxide-opportunities-to-address-environmental-issues
#8
Jean Septavaux, Geoffroy Germain, Julien Leclaire
Extraction and purification of basic chemicals from complex mixtures has been a persistent issue throughout the development of the chemical sciences. The chemical industry and academic research have grown over the centuries by following a deconstruction-reconstruction approach, reminiscent of the metabolism process. Chemists have designed and optimized extraction, purification, and transformation processes of molecules from natural deposits (fossil fuels, biomass, ores), in order to reassemble them into complex adducts...
June 23, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28644561/the-redox-sensitive-module-of-cyclophilin-20-3-2-cysteine-peroxiredoxin-and-cysteine-synthase-integrates-sulfur-metabolism-and-oxylipin-signaling-in-the-high-light-acclimation-response
#9
Sara M Müller, Shanshan Wang, Wilena Telman, Michael Liebthal, Helena Schnitzer, Andrea Viehhauser, Carsten Sticht, Carolina Delatorre, Markus Wirtz, Rüdiger Hell, Karl-Josef Dietz
The integration of redox- and reactive oxygen species-dependent signaling and metabolic activities are fundamental to plant acclimation to biotic and abiotic stresses. Previous data suggest the existence of a dynamically interacting module in the chloroplast stroma consisting of cyclophilin 20-3 (Cyp20-3), O-acetylserine(thiol)lyase B (OASTL-B), 2-cysteine peroxiredoxins A/B (2-CysPrx) and serine acetyltransferase 2;1 (SERAT2;1). The functionality of this COPS module is influenced by redox stimuli and oxophytodienoic acid (OPDA) which is the precursor for jasmonic acid...
June 23, 2017: Plant Journal: for Cell and Molecular Biology
https://www.readbyqxmd.com/read/28644418/new-mt%C3%A2-melatonin-receptor-selective-ligands-agonists-and-partial-agonists
#10
Jean A Boutin, Anne Bonnaud, Chantal Brasseur, Olivier Bruno, Nolwenn Lepretre, Peter Oosting, Sophie Coumailleau, Philippe Delagrange, Olivier Nosjean, Céline Legros
The search for melatonin receptor agonists and antagonists specific towards one of the receptor subtypes will extend our understanding of the role of this system in relaying circadian information to the body. A series of compounds derived from a hit compound discovered in a screening process led to powerful agonists specific for one of the isoform of the melatonin receptor namely, MT₂. The compounds are based on a poorly explored skeleton in the molecular pharmacology of melatonin. By changing the steric hindrance of one substituent (i...
June 23, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28644382/metal-ion-loaded-nanofibre-matrices-for-calcification-inhibition-in-polyurethane-implants
#11
Charanpreet Singh, Xungai Wang
Pathologic calcification leads to structural deterioration of implant materials via stiffening, stress cracking, and other structural disintegration mechanisms, and the effect can be critical for implants intended for long-term or permanent implantation. This study demonstrates the potential of using specific metal ions (MI)s for inhibiting pathological calcification in polyurethane (PU) implants. The hypothesis of using MIs as anti-calcification agents was based on the natural calcium-antagonist role of Mg(2+) ions in human body, and the anti-calcification effect of Fe(3+) ions in bio-prosthetic heart valves has previously been confirmed...
June 23, 2017: Journal of Functional Biomaterials
https://www.readbyqxmd.com/read/28644179/improving-heart-failure-patient-outcomes-utilizing-guideline-directed-therapy
#12
Beth Towery Davidson, Terri Lynn Allison
Heart failure (HF) prevalence continues to rise and remains a significant burden to patients, caregivers, providers, and the healthcare system. Guideline-directed medical therapy with standard neurohormonal blockade has been the cornerstone of medical management for many years. Despite aggressive utilization of angiotensin-converting enzyme inhibitors, angiotensin receptor blockers, beta-blockers, and aldosterone antagonists, HF hospitalizations and readmissions are common and residual mortality remains high...
July 21, 2017: Nurse Practitioner
https://www.readbyqxmd.com/read/28644160/calcitonin-gene-related-peptide-targeted-therapies-for-migraine-and-cluster-headache-a-review
#13
Nathaniel M Schuster, Alan M Rapoport
Calcitonin gene-related peptide (CGRP) is a signaling neuropeptide released from activated trigeminal sensory afferents in headache and facial pain disorders. There are a handful of CGRP-targeted therapies currently in phase 3 studies for migraine acute treatment or prevention. Currently, 4 monoclonal antibodies targeting either the CGRP ligand or receptor are being studied for migraine prevention: ALD403 (eptinezumab), AMG 334 (erenumab), LY2951742 (galcanezumab), and TEV-48125 (fremanezumab). Meanwhile, 1 small-molecule CGRP receptor antagonist (ubrogepant, MK-1602) is currently in phase 3 studies for the acute treatment of migraine...
June 21, 2017: Clinical Neuropharmacology
https://www.readbyqxmd.com/read/28644012/sigma-2-receptor-tmem97-agonists-produce-long-lasting-anti-neuropathic-pain-effects-in-mice
#14
James J Sahn, Galo L Mejia, Pradipta R Ray, Stephen F Martin, Theodore John Price
Neuropathic pain is an important medical problem with few effective treatments. The sigma 1 receptor (σ1R) is a potential target for neuropathic pain therapeutics, and antagonists for this receptor are effective in preclinical models and are currently in phase II clinical trials. Relatively little is known about the σ2R, which has recently been identified as transmembrane protein 97 (Tmem97). We generated a series of σ1R and σ2R/Tmem97 agonists and antagonists and tested them for efficacy in the mouse spared nerve injury (SNI) model...
June 23, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28643469/atra-signaling-regulates-the-expression-of-col9a1-through-bmp2-wnt4-runx1-pathway-in-antler-chondrocytes
#15
Hong-Liang Zhang, Bin Guo, Zhan-Qing Yang, Cui-Cui Duan, Shuang Geng, Kai Wang, Hai-Fan Yu, Zhan-Peng Yue
Although all-trans retinoic acid (ATRA) is involved in the regulation of cartilage growth and development, its regulatory mechanisms remain unknown. Here, we showed that ATRA could induce the expression of COL9A1 in antler chondrocytes. Silencing of cellular retinoic acid binding protein 2 (CRABP2) could impede the ATRA-induced upregulation of COL9A1, whereas overexpression of CRABP2 presented the opposite effect. RARα agonist Am80 induced the expression of COL9A1, whereas treatment with RARα antagonist Ro 41-5253 or RXRα small-interfering RNA (siRNA) caused an obvious blockage of ATRA on COL9A1...
June 22, 2017: Journal of Experimental Zoology. Part B, Molecular and Developmental Evolution
https://www.readbyqxmd.com/read/28643444/how-media-exposure-relates-to-laypersons-understanding-of-psychopathy
#16
Michael E Keesler, David DeMatteo
While conceptualization of psychopathy has evolved, so too has the public's relationship with psychology changed. Concurrently, portrayal of psychopaths has made several shifts, both through nonfiction sources and in popular film and television. Psychopathic villains of the mid-20th century have made space for a growing cast of protagonist psychopaths. This study examined whether a relationship existed between exposure to fictional psychopaths and how lay individuals conceptualize psychopathy. Specifically, this study explored conceptualization differences based on exposure to antagonist versus protagonist fictional psychopaths...
June 23, 2017: Journal of Forensic Sciences
https://www.readbyqxmd.com/read/28643374/population-pharmacokinetic-and-pharmacodynamic-modeling-of-ly2510924-in-patients-with-advanced-cancer
#17
S Bihorel, E Raddad, J Fiedler-Kelly, J R Stille, J Hing, E Ludwig
The objectives of this study were to characterize the pharmacokinetics (PK) of LY2510924, a potent peptide antagonist of the CXCR4 receptor, after subcutaneous administration in patients with advanced cancer forms and quantify LY2510924 stimulatory effects on the mobilization of cells bearing the cluster of differentiation 34 (CD34) as an indirect reflection of the chemokine C-X-C motif ligand 12/CXCR4 axis inhibition. LY2510924 PK were best characterized by a 2-compartment model with first-order absorption and dose-dependent clearance predicting steady state after three daily doses and little accumulation (accumulation ratio <1...
June 23, 2017: CPT: Pharmacometrics & Systems Pharmacology
https://www.readbyqxmd.com/read/28643288/inhibitory-effect-of-fsllry-nh2-on-inflammatory-responses-induced-by-hydrogen-peroxide-in-hepg2-cells
#18
Yeon Joo Lee, Su Jin Kim, Kyoung Wan Kwon, Won Mo Lee, Wi Joon Im, Uy Dong Sohn
Proteinase activated receptor 2 (PAR2), which is localized in the GI tract, the respiratory system, and the kidney tubules is a G protein-coupled receptor associated with inflammation, metabolism, and disease. The aim of this study was to explore the role of PAR2 in hydrogen peroxide (H2O2)-induced HepG2 cells by using FSLLRY-NH2 a PAR2 antagonist. H2O2 treatment resulted in induction of PAR2 in esophageal, gastric, and liver cells, with the most robust response being in HepG2 cells. Furthermore, this effect was dose-dependent in HepG2 cells...
June 22, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28643219/triple-antithrombotic-therapy-in-atrial-fibrillation-patients-undergoing-pci-a-fading-role
#19
Dimitrios Alexopoulos, Panagiotis Vlachakis, John Lekakis
Triple antithrombotic therapy (TAT), consisting of aspirin, a P2Y12 receptor antagonist and oral anticoagulant (OAC) medication has been considered as an 'unavoidable' strategy for a 1-12 months for atrial fibrillation (AF) patients post acute coronary syndrome or percutaneous coronary angioplasty with stenting. However, TAT has rather poorly been adopted in real life practice, mainly because of an accompanying increased bleeding potential and lack of definitive results of randomized clinical trials. Several registries, meta-analyses and small randomized trials have so far provided the base of guidelines recommendations...
June 22, 2017: Cardiovascular Drugs and Therapy
https://www.readbyqxmd.com/read/28643146/helicobacter-pylori-induced-modulation-of-the-promoter-methylation-of-wnt-antagonist-genes-in-gastric-carcinogenesis
#20
Hyo-Joon Yang, Sang Gyun Kim, Joo Hyun Lim, Ji Min Choi, Woo Ho Kim, Hyun Chae Jung
BACKGROUND: This study aimed to investigate the changes in the promoter methylation and gene expression of multiple Wnt antagonists between the chronic infection and eradication of Helicobacter pylori (H. pylori) in gastric carcinogenesis. METHODS: The levels of methylation and corresponding mRNA expression of seven Wnt antagonist genes (SFRP1, -2, -5, DKK1, -2, -3, WIF1) were compared among the patients with H. pylori-positive gastric cancers (GCs), and H. pylori-positive and H...
June 22, 2017: Gastric Cancer
keyword
keyword
847
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"