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British Journal of Pharmacology

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https://www.readbyqxmd.com/read/28334417/pharmacovigilance-database-search-discloses-clc-k-channels-as-a-novel-target-of-the-at1-receptor-blockers-valsartan-and-olmesartan
#1
Paola Imbrici, Domenico Tricarico, Giuseppe Felice Mangiatordi, Orazio Nicolotti, Marcello Diego Lograno, Diana Conte, Antonella Liantonio
BACKGROUND AND PURPOSE: Human ClC-K chloride channels are highly attractive targets for drug discovery for their physiological role and association with genetic disorders. These channels are pivotal in the kidney as they control chloride reabsorption and water diuresis. In addition, loss-of-function mutations of CLCKNB and BSND genes cause Bartter's syndrome (BS), whereas CLCNKA and CLCKNB gain-of-function polymorphisms predispose to a rare form of salt sensitive hypertension. Both disorders lack a personalized therapy that is in most cases only symptomatic...
March 23, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28332701/the-epigenetic-landscape-related-to-reactive-oxygen-species-formation-in-the-cardiovascular-system
#2
REVIEW
Thomas Kietzmann, Andreas Petry, Antonina Shvetsova, Joachim M Gerhold, Agnes Görlach
Cardiovascular diseases are the leading cause of death worldwide. Reactive oxygen species (ROS) can act as damaging molecules but also represent central hubs in cellular signalling networks. Increasing evidence indicates that ROS play an important role in the pathogenesis of cardiovascular diseases, although the underlying mechanisms and consequences of pathophysiological elevated ROS in the cardiovascular system are still not completely resolved. More recently, alterations of the epigenetic landscape which can affect DNA methylation, post-translational histone modifications, ATP-dependent alterations to chromatin and non-coding RNA transcripts, have been considered to be of increasing importance in the pathogenesis of cardiovascular diseases...
March 23, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28326542/current-and-future-therapies-for-addressing-the-effects-of-inflammation-on-hdl-cholesterol-metabolism
#3
REVIEW
Fatima Iqbal, Wendy S Baker, Madiha I Khan, Shwetha Thukuntla, Kevin H McKinney, Nicola Abate, Demidmaa Tuvdendorj
Cardiovascular disease (CVD) is a major cause of morbidity and mortality worldwide. Inflammatory processes arising from metabolic abnormalities are known to precipitate the development of CVD. Several metabolic and inflammatory markers have been proposed for predicting the progression of CVD, including high density lipoprotein cholesterol (HDL-C). For ~50 years, HDL-C has been considered as the atheroprotective 'good' cholesterol because of its strong inverse association with the progression of CVD. Thus, interventions to increase the concentration of HDL-C have been successfully tested in animals; however, clinical trials were unable to confirm the cardiovascular benefits of pharmaceutical interventions aimed at increasing HDL-C levels...
March 22, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28320072/constitutive-androstane-receptor-regulates-the-intestinal-mucosal-response-to-injury
#4
Grace M Hudson, Kyle L Flannigan, Sarah L Erickson, Fernando A Vicentini, Alexandra Zamponi, Christina L Hirota, Laurie Alston, Christophe Altier, Subrata Ghosh, Kevin P Rioux, Sridhar Mani, Thomas K Chang, Simon A Hirota
BACKGROUND AND PURPOSE: The pathogenesis of the inflammatory bowel diseases(IBD), composed of Crohn's disease(CD) and ulcerative colitis(UC), involves aberrant interactions between a genetically susceptible individual, their microbiota and environmental factors. Alterations in xenobiotic receptor expression and function are associated with increased risk for IBD. In the current study, we assessed the role of the constitutive androstane receptor(CAR), a xenobiotic receptor closely related to the pregnane X receptor, in the regulation of intestinal mucosal homeostasis...
March 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28320070/dexpramipexole-improves-bioenergetics-and-outcome-in-experimental-stroke
#5
Mirko Muzzi, Elisabetta Gerace, Daniela Buonvicino, Elisabetta Coppi, Francesco Resta, Laura Formentini, Riccardo Zecchi, Laura Tigli, Daniele Guasti, Martina Ferri, Emidio Camaioni, Alessio Masi, Domenico E Pellegrini-Giampietro, Guido Mannaioni, Daniele Bani, Anna M Pugliese, Alberto Chiarugi
BACKGROUND AND PURPOSE: To investigate the effects of dexpramipexole, a drug recently tested in ALS patients able to bind F1Fo ATP synthase and increase mitochondrial ATP production, on experimental ischemic brain injury. EXPERIMENTAL APPROACH: The effects of dexpramipexole on bioenergetics, Ca(2+) fluxes, electrophysiological functions and death were evaluated in primary neural cultures and hippocampal slices exposed to oxygen-glucose deprivation (OGD). The drug's impact on infarct volumes and neurological functions was also evaluated in mice subjected to proximal or distal MCAo...
March 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28320049/d-%C3%AE-hydroxybutyrate-promotes-functional-recovery-and-relieves-pain-hypersensitivity-in-mice-with-spinal-cord-injury
#6
Jiao Qian, Wenjun Zhu, Ming Lu, Bin Ni, Jun Yang
BACKGROUND AND PURPOSE: Spinal cord injury (SCI) leads to severe motor and sensory dysfunction and significantly reduces the quality of life. The aim of present work was to investigate the effect of administration of exogenous D-β-hydroxybutyrate (DBHB) on functional recovery and neuropathic pain in spinal-cord-injured mice. EXPERIMENTAL APPROACH: Mice were given a moderate-severe thoracic spinal contusion injury at the T9-10 level, and treated with exogenous DBHB...
March 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28320043/effects-of-ranolazine-in-a-model-of-doxorubicin-induced-left-ventricle-diastolic-dysfunction
#7
Donato Cappetta, Grazia Esposito, Raffaele Coppini, Elena Piegari, Rosa Russo, Loreta Pia Ciuffreda, Alessia Rivellino, Lorenzo Santini, Concetta Rafaniello, Cristina Scavone, Francesco Rossi, Liberato Berrino, Konrad Urbanek, Antonella De Angelis
BACKGROUND AND PURPOSE: Doxorubicin (DOXO) is a highly effective anticancer drug but its clinical application is impeded by cardiotoxicity. Asymptomatic diastolic dysfunction can be the earliest manifestation of DOXO cardiotoxicity. Therefore, a search for therapeutic intervention that can interfere with early manifestations and possibly prevent late cardiotoxicity is warranted. Increased DOXO-dependent reactive oxygen species may explain, in part, Ca(2+) and Na(+) overload that contributes to diastolic dysfunction and development of heart failure...
March 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28320042/calcium-channel-modulation-as-a-target-in-chronic-pain-control
#8
REVIEW
Ryan Patel, Carlota Montagut-Bordas, Anthony H Dickenson
Neuropathic pain remains poorly treated for large numbers of patients and little progress has been made in developing novel classes of analgesics. To redress this issue, ziconotide (Prialt(TM) ) was developed and approved as a first in class synthetic version of ω-conotoxin MVIIA, a Cav 2.2 peptide blocker. Unfortunately, the impracticalities of intrathecal delivery, low therapeutic index and severe neurological side effects associated with ziconotide has restricted its use to exceptional circumstances. Ziconotide exhibits no state or use dependent block of Cav 2...
March 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28319650/-monoclonal-antibodies-in-the-treatment-of-ms-emergence-of-b-cell-targeted-therapies
#9
REVIEW
Ai-Lan Nguyen, Melissa Gresle, Tessa Marshall, Helmut Butzkueven, Judith Field
Multiple sclerosis (MS) is a chronic inflammatory disease of the CNS, and one of the most common causes of disability in young adults. Over the last decade, new disease modifying therapies have rapidly emerged, including monoclonal antibodies (mAbs) that have provided highly targeted therapies with superior efficacy compared to platform therapies. In particular, monoclonal antibodies directed against CD20-positive B cells have shown remarkable results in recent clinical trials, and renewed interest in the mechanism of B-cell depleting therapies to ameliorate relapse activity and progression in MS...
March 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28317098/cgrp-receptor-activity-in-mice-with-global-expression-of-human-receptor-activity-modifying-protein-1
#10
Keegan J Bohn, Baolin Li, Xiaofang Huang, Bianca N Mason, Anne-Sophie Wattiez, Adisa Kuburas, Christopher S Walker, Peiyi Yang, Jianliang Yu, Beverly A Heinz, Kirk W Johnson, Andrew F Russo
BACKGROUND AND PURPOSE: CGRP is a potent vasodilator and nociceptive neuropeptide linked to migraine. CGRP receptors are heterodimers of receptor activity-modifying protein-1 (RAMP1) and either calcitonin receptor-like receptor (CLR), which forms the canonical CGRP receptor, or calcitonin receptor (CTR), which forms the amylin-1 (AMY1 ) receptor. The goal of this study was to test whether transgenic mice globally expressing human RAMP1 (hRAMP1) have increased CGRP receptor activity and whether the receptors are sensitive to the human selective antagonist telcagepant...
March 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28306139/the-tir-bb-loop-mimetic-as-1-prevents-nonalcoholic-steatohepatitis-and-hepatic-insulin-resistance-by-inhibiting-nlrp3-asc-inflammasome-activation
#11
Xiaolu Wang, Yun Gao, Juan Song, Chao Tang, Man Wang, Linli Que, Li Liu, Guoqing Zhu, Qi Chen, Yong Yao, Yong Xu, Jiantao Li, Yuehua Li
BACKGROUND AND PURPOSE: Non-alcoholic steatohepatitis (NASH) is characterized by excessive intracellular lipid accumulation, inflammation and hepatic insulin resistance. Considering the rising prevalence of NASH worldwide, it is urgent to find novel interventional approaches. The pro-inflammatory cytokine IL-1β, generated and released from the Kupffer cells, is considered to be an initiating event in NASH. AS-1, a synthetic low-molecule mimetic to myeloid differentiation primary response gene 88 (MyD88), has been reported to disrupt the IL-1R-MyD88 interaction...
March 17, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28299790/tc-mps1-12-a-novel-mps1-inhibitor-suppresses-a-growth-of-hepatocellular-carcinoma-cells-via-accumulated-chromosomal-instability
#12
Minji Choi, Yoo Hong Min, Jaehyuk Pyo, Chang-Woo Lee, Chang-Young Jang, Ja-Eun Kim
BACKGROUND AND PURPOSE: Chromosomal instability is not only a hallmark of cancer, but also an attractive therapeutic target. A diverse set of mitotic kinases maintains chromosomal stability. One of these is monopolar spindle 1 (Mps1), which is essential for chromosome alignment and for the spindle assembly checkpoint (SAC). Pharmacological inhibition of Mps1 has been suggested as a cancer therapeutic; however, despite the existence of a novel Mps1 inhibitor, TC Mps1 12, no such studies have been performed...
March 15, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28299773/trafficking-and-other-regulatory-mechanisms-for-organic-anion-transporting-polypeptides-oatps-and-organic-anion-transporters-oats-that-modulate-cellular-drug-and-xenobiotic-influx-and-that-are-dysregulated-in-disease
#13
REVIEW
Michael Murray, Fanfan Zhou
Organic anion transporters (OATs) and organic anion-transporting polypeptides (OATPs), encoded by a number of SLC22A and SLCO genes, mediate the absorption and distribution of drugs and other xenobiotics. The regulation of OATs and OATPs is complex, comprising both transcriptional and post-translational mechanisms. Plasma membrane expression is required for cellular substrate influx by OATs/OATPs. Thus, interest in post-translational regulatory processes, including membrane targeting, endocytosis, recycling and degradation of transporter proteins, is increasing because these are critical for plasma membrane expression...
March 15, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28299772/immunology-provides-a-great-success-for-treating-systemic-autoimmune-diseases-a-perspective-on-immunopharmacology-iuphar-review-x
#14
REVIEW
Masaru Ishii
Recent advances in the bioengineering of monoclonal antibodies (mAbs) have revolutionized the treatment of several immunological and rheumatic diseases. mAbs exhibit high specificity and affinity, and are very effective targeting agents, associated with minimal off-target adverse effects. Of several relevant immunological diseases, rheumatoid arthritis was the condition initially treated with mAbs, with great success. Currently, many immunological disorders are targeted and successfully treated using such novel approaches; these include inflammatory bowel diseases, multiple sclerosis, lupus, and psoriasis...
March 15, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28294304/il-21-promotes-myocardial-ischemia-reperfusion-injury-through-the-modulation-of-neutrophil-infiltration
#15
Kejing Wang, Shuang Wen, Jiao Jiao, Tingting Tang, Xin Zhao, Min Zhang, Bingjie Lv, Yuzhi Lu, Xingdi Zhou, Jingyong Li, Shaofang Nie, Yuhua Liao, Qing Wang, Xin Tu, Ziad Mallat, Ni Xia, Xiang Cheng
BACKGROUND AND PURPOSE: The immune system plays important roles in driving the acute inflammatory response following myocardial ischemia/reperfusion injury (MIRI). Interleukin-21 (IL-21) is a pleiotropic cytokine with multiple immunomodulatory effects and its role in MIRI remains unknown. EXPERIMENTAL APPROACH: Myocardial injury, neutrophil infiltration and expressions of neutrophil chemokines keratinocyte-derived chemokine (KC) and macrophage inflammatory protein-2 (MIP-2) were studied in a mouse model of MIRI...
March 14, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28294298/proteins-and-chemical-chaperones-involved-in-neuronal-nicotinic-receptor-expression-and-function-an-update
#16
REVIEW
Arianna Crespi, Sara Francesca Colombo, Cecilia Gotti
Neuronal nicotinic acetylcholine receptors (nAChRs) are a family of acetylcholine-(ACh) gated cation channels and their homeostasis or proteostasis is essential for the correct physiology of the central and peripheral nervous systems. The proteostasis network regulates the folding, assembly, degradation and trafficking of nAChRs in order to ensure their efficient functional cell surface expression. However, as nAChRs are multisubunit, multispan, integral membrane proteins, the folding and assembly is a very inefficient process, and only a small portion of subunits can form functional pentamers...
March 13, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28276575/mathematical-modeling-of-the-drug-release-from-an-ensemble-of-coated-pellets
#17
Diego Caccavo, Gaetano Lamberti, Maria Margherita Cafaro, Anna Angela Barba, Jurgita Kazlauske, Anette Larsson
BACKGROUND AND PURPOSE: Coated pellets are widely used as oral drug delivery systems, being highly accepted by patients and with several advantages with respect to single unit devices. The understanding of their behavior is therefore needed to improve the formulation effectiveness and to reduce the production costs. In spite of such an importance, not many mathematical modeling attempts have been made, mostly due to the complexities arising from the system polydispersity (non homogeneous multiple-unit particulate systems), which has been scarcely investigated with the aid of mechanistic models...
March 9, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28268256/cannabidiol-regulation-of-emotion-and-emotional-memory-processing-relevance-for-treating-anxiety-related-and-substance-abuse-disorders
#18
REVIEW
Jonathan L C Lee, Leandro J Bertoglio, Francisco S Guimarães, Carl W Stevenson
Learning to associate cues or contexts with potential threats or rewards is adaptive and enhances survival. Both aversive and appetitive memories are therefore powerful drivers of behaviour, but the inappropriate expression of conditioned responding to fear- and drug-related stimuli can develop into anxiety-related and substance abuse disorders respectively. These disorders are associated with abnormally persistent emotional memories and inadequate treatment, often leading to symptom relapse. Studies show that cannabidiol, the main non-psychotomimetic phytocannabinoid found in Cannabis sativa, reduces anxiety via 5-HT1A and (indirect) cannabinoid receptor activation in paradigms assessing innate responses to threat...
March 7, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28266020/insights-into-the-function-of-opioid-receptors-from-molecular-dynamics-simulations-of-available-crystal-structures
#19
REVIEW
Kristen A Marino, Yi Shang, Marta Filizola
The opioid receptors (ORs) are key targets in the treatment of acute and chronic pain, and the development of novel analgesics with reduced side effects is crucial in the search for more effective medications. The crystal structures of ORs have provided a wealth of knowledge on many aspects of OR pharmacology and function, including ligand binding poses, location of the sodium allosteric binding site, conformational changes associated with activation, and putative dimeric interfaces. These crystal structures also offer a starting point for molecular dynamics (MD) simulations to capture one aspect of drug design that static structures cannot resolve, namely protein dynamics...
March 7, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28264149/hippocampal-%C3%AE-7-nicotinic-acetylcholine-receptors-contribute-to-modulation-of-depression-like-behavior-in-c57bl-6%C3%A2-j-mice
#20
Yann S Mineur, Tenna N Mose, Sam Blakeman, Marina R Picciotto
BACKGROUND AND PURPOSE: Clinical studies have identified links between cholinergic signaling and depression in human subjects. Increased cholinergic signaling in hippocampus also increases behaviors related to anxiety and depression in mice, which can be reversed by acetylcholine receptor antagonists. EXPERIMENTAL APPROACH: Since the α7 subunit of the nicotinic acetylcholine receptor (nAChR) is highly expressed in hippocampus, we determined whether blocking α7 nAChRs could reverse effects of increased ACh signaling in anxiety- and depression-related behaviors in mice...
March 6, 2017: British Journal of Pharmacology
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