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British Journal of Pharmacology

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https://www.readbyqxmd.com/read/28444744/dual-cdk4-6-inhibition-by-pd-0332991-induces-apoptosis-and-senescence-in-esophageal-squamous-cell-carcinoma-cells
#1
Liang Chen, Jingxuan Pan
BACKGROUND AND PURPOSE: Aberrant activation of Cyclin D1-CDK4/6-Rb signaling pathway is common in esophageal squamous cell carcinoma (ESCC). PD-0332991, a highly specific inhibitor of CDK4/6, has been showed potent antitumor activity against multiple types of cancer. The purpose of this study was to examine the in vitro and in vivo antineoplastic effect of PD-0332991 against the growth and metastasis in ESCC cells. EXPERIMENTAL APPROACH: Cell viability and synergy between PD-0332991 and 5-fluorouracil/Cisplatin were measured by MTS assay and CalcuSyn software, respectively...
April 25, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28444738/factors-influencing-biased-agonism-in-recombinant-cells-expressing-the-human-%C3%AE-1a-adrenoceptor
#2
Edilson Dantas da Silva Junior, Masaaki Sato, Jon Merlin, Natalie Broxton, Dana S Hutchinson, Sabatino Ventura, Bronwyn A Evans, Roger J Summers
BACKGROUND AND PURPOSE: Agonists acting at G protein-coupled receptors promote biased signalling via Gα or Gβγ subunits, G protein-coupled receptor kinases and β-arrestins. Since demonstration of biased agonism has implications for drug discovery, it is essential to consider confounding factors contributing to bias. We have examined bias at human α1A -adrenoceptors stably expressed at low levels in CHO-K1 cells, identifying off-target effects at endogenous receptors that contribute to ERK1/2 phosphorylation in response to the agonist oxymetazoline...
April 25, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28437860/chronic-inhibition-of-fatty-acid-amide-hydrolase-by-urb597-produces-differential-effects-on-cardiac-performance-in-normotensive-and-hypertensive-rats
#3
Anna Pedzinska-Betiuk, Jolanta Weresa, Marek Toczek, Marta Baranowska-Kuczko, Irena Kasacka, Ewa Harasim-Symbor, Barbara Malinowska
BACKGROUND AND PURPOSE: Fatty acid amide hydrolase (FAAH) inhibitors are postulated to possess anti-hypertensive potential, because their acute injection decreases blood pressure (BP) in spontaneously hypertensive rats (SHR) partially through normalization of cardiac contractile function. Here, we examined whether the potential hypotensive effect of chronic FAAH inhibition by URB597 in hypertensive rats correlates with changes in cardiac performance. EXPERIMENTAL APPROACH: Experiments were performed using perfused hearts and left atria isolated from 8-10 week old SHR, age-matched deoxycorticosterone acetate (DOCA-salt) rats and normotensive controls chronically treated with URB597 (1 mg kg(-1) ) or vehicle...
April 24, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28437857/influence-of-inflammation-and-nitric-oxide-upon-platelet-aggregation-following-deposition-of-diesel-exhaust-particles-in-the-airways
#4
E Smyth, A Solomon, M A Birrell, M J Smallwood, P G Winyard, T D Tetley, M Emerson
BACKGROUND AND PURPOSE: Exposure to nanoparticulate pollution has been implicated in platelet-driven thrombotic events such as myocardial infarction. Inflammation and impairment of nitric oxide (NO) bioavailability have been proposed as potential causative mechanisms. It is unclear, however, whether airways exposure to combustion-derived nanoparticles such as diesel exhaust particles (DEP) or carbon black (CB) can augment platelet aggregation in vivo and the underlying mechanisms remain undefined...
April 24, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28437839/semicarbazide-sensitive-amine-oxidase-vascular-adhesion-protein-1-inhibition-reduces-lipopolysaccharide-induced-neuroinflammation
#5
Serena Becchi, Alberto Buson, Jonathan Foot, Wolfgang Jarolimek, Bernard W Balleine
BACKGROUND AND PURPOSE: Neuroinflammation is initiated by a variety of stimuli including infections, sepsis, neurodegenerative diseases or traumatic brain injury and if not adequately controlled can lead to various degrees of neuronal damage and behavioural impairment. A critical event in the initial steps of inflammation is neutrophil extravasation. Semicarbazide sensitive amine oxidase (SSAO, also known as vascular adhesion protein 1 or VAP-1) regulates neutrophil adhesion and extravasation...
April 24, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28436023/activation-of-amp-activated-protein-kinase-by-metformin-ablates-angiotensin-ii-induced-endoplasmic-reticulum-stress-and-hypertension-in-mice-in-vivo
#6
Quanlu Duan, Ping Song, Ye Ding, Ming-Hui Zou
BACKGROUND AND PURPOSE: Metformin, one of the most frequently prescribed medications for type 2 diabetes, reportedly exerts blood pressure (BP)-lowering effects in patients with diabetes; however, the effects and underlying mechanisms of metformin on BP in non-diabetic condition remains to be determined. The aim of the present study was to determine the effects of metformin on angiotensin II (Ang II) infusion-induced hypertension in vivo. EXPERIMENTAL APPROACH: The effects of metformin on BP were investigated in wild-type (WT, C57BL/6 J) and AMP-activated protein kinase (AMPKα2) knockout (AMPKα2(-/-) ) mice with or without Ang II-infusion...
April 23, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28436014/a-critical-assessment-of-the-synthesis-and-biological-activity-of-p53-hdm2-stapled-peptide-inhibitors
#7
Rike Wallbrecher, Patrick Chène, Stephan Ruetz, Therese Stachyra, Thomas Vorherr, Roland Brock
BACKGROUND AND PURPOSE: Helix stapling enhances the activity of peptides that interact with a target protein in a helical conformation. These staples are also supposed to change the pharmacokinetics of the molecules and promote cytoplasmic targeting. We scrutinized to which degree the pharmacokinetic characteristics are a function of the staple and differ from those of the standard cationic cell-penetrating peptide nonaarginine for a peptide inhibiting the interaction of p53 with the human double minute 2 (Hdm2) protein...
April 23, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28432778/cross-species-studies-of-cognition-relevant-to-drug-discovery-a-translational-approach
#8
REVIEW
T W Robbins
This Review advances the case that bidirectional, cross-species translation of findings from experimental animals to and from humans is an important strategy for drug discovery. Animal models of mental disorders require appropriate behavioural or cognitive outcome variables that can be generalized cross-species. One example is the treatment of impulsive behaviour in attention deficit hyperactivity disorder (ADHD) with stimulant drugs. Performance on the stop signal reaction task as an index of impulsivity is improved both in healthy human volunteers and in patients with adult ADHD by stimulant drugs and also by the selective noradrenergic reuptake blocker atomoxetine...
April 22, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28432761/protein-s-sulfhydration-by-hydrogen-sulfide-in-cardiovascular-system
#9
REVIEW
Guoliang Meng, Shuang Zhao, Liping Xie, Yi Han, Yong Ji
Hydrogen sulfide (H2 S), independent on any specific transporters, plays a number of biological effects on cardiovascular systems. However, the detailed mechanism of H2 S is not yet clear until now. Recently, a novel post-translational modification induced by H2 S, named S-sulfhydration, has been proposed. S-sulfhydration is a chemical modification on specific cysteine residues of target proteins by H2 S. There are several methods for S-sulfhydration detection, such as modified biotin switch assay, maleimide assay with fluorescent thiol modifying regents, tag-switch method and mass spectrometry...
April 22, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28430359/sulfur-containing-gaseous-signal-molecules-ion-channels-and-cardiovascular-diseases
#10
REVIEW
Wen Yu, Hongfang Jin, Chaoshu Tang, Junbao Du, Zhiren Zhang
Sulfur-containing gaseous signal molecules including hydrogen sulfide (H2 S) and sulfur dioxide (SO2 ) were previously recognized as toxic gases. However, extensive studies have revealed that they can be generated in the cardiovascular system via a sulfur-containing amino acid metabolic pathway, playing an important part in cardiovascular physiology and pathophysiology. Ion channels are pore-forming membrane proteins present in the membrane of all biological cells; functions include establishing a resting membrane potential and controlling action potentials and other electrical signals by conducting ions across the cell membrane...
April 21, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28430357/reactive-oxygen-species-key-regulators-in-vascular-health-and-diseases
#11
REVIEW
Qishan Chen, Qiwen Wang, Jianhua Zhu, Qingzhong Xiao, Li Zhang
Reactive oxygen species (ROS) are a group of small reactive molecules that play critical roles in the regulation of various cell functions and biological processes. In the vascular system, physiological levels of ROS are essential for normal vascular functions including endothelial homeostasis and smooth muscle cell contraction. In contrast, uncontrolled overproduction of ROS resulted from imbalance of ROS generation and elimination, leads to the development of vascular diseases. Excessive ROS cause vascular cell damages, recruitment of inflammatory cells, lipid peroxidation, activation of metalloproteinases, and deposition of extracellular matrix, collectively leading to vascular remodeling...
April 21, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28430355/does-endothelial-tetrahydrobiopterin-control-the-endothelial-nitric-oxide-coupling-state-in-arterial-resistance-arteries
#12
Thomas Münzel, Andreas Daiber
No abstract text is available yet for this article.
April 21, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28427114/h-lifestyle-use-of-drugs-by-healthy-people-for-enhancing-cognition-creativity-motivation-and-pleasure
#13
REVIEW
L-S Camilla d'Angelo, George Savulich, Barbara J Sahakian
Today there is continued, and in some cases growing, availability of psychoactive substances, including treatments for mental health disorders such as cognitive enhancers, which can enhance or restore brain function, but also 'recreational' drugs such as novel psychoactive substances (NPS). The use of psychoactive drugs has both benefits and risks: whilst new drugs to treat cognitive symptoms in neuropsychiatric or neurodegenerative disorders could have great benefits for many patient groups, the increasing ease of accessibility to recreational NPS and the increasing lifestyle use of cognitive enhancers by healthy people means that the effective management of psychoactive substances will be an issue of increasing importance...
April 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28423178/head-to-head-comparison-of-structurally-unrelated-dpp4-inhibitors-in-the-setting-of-renal-ischemia-reperfusion-injury
#14
Christoph Reichetzeder, Karoline von Websky, Oleg Tsuprykov, Azadeh Mohagheghi Samarin, Luise Gabriele Falke, Sulistyo Emantoko Dwi Putra, Ahmed Abdallah Hasan, Viktoriia Antonenko, Caterina Curato, Jörg Rippman, Thomas Klein, Berthold Hocher
BACKGROUND AND PURPOSE: Results regarding protective effects of DPP4 inhibitors in renal ischemia-reperfusion-injury (IRI) are conflicting. The current study performed a head-to-head comparison of structurally unrelated DPP4 inhibitors in the setting of renal IRI. EXPERIMENTAL APPROACH: IRI was induced in uninephrectomized male rats by renal artery clamping for 30 minutes. The sham group was uninephrectomized but not subjected to IRI. DPP4 inhibitors or vehicle were given p...
April 18, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28419419/the-isoprenoid-derivative-n6-benzyladenosine-cm223-exerts-antitumor-effect-in-glioma-patient-derived-primary-cells-through-the-mevalonate-pathway
#15
Elena Ciaglia, Manuela Grimaldi, Mario Abate, Mario Scrima, Manuela Rodriquez, Chiara Laezza, Roberta Ranieri, Simona Pisanti, Pierangela Ciuffreda, Clementina Manera, Patrizia Gazzerro, Anna Maria D'Ursi, Maurizio Bifulco
BACKGROUND AND PURPOSE: N6-Isopentenyladenosine (i6A) is a modified nucleoside exerting in vitro and in vivo antiproliferative effects. We previously demonstrated that the i6A action is correlated to farnesyl pyrophosphate synthase (FPPS) expression and activity, a key enzyme involved in the mevalonate (MVA) pathway, which is found aberrant in brain cancer. To develop new anti-glioma strategies, we looked for other valuable compounds exhibiting improved activity as compared to i6A. EXPERIMENTAL APPROACH: we designed and synthesized i6A derivatives characterized by the introduction of diverse chemical moieties in the N6 position of adenosine and tested for their efficacy in U87 and primary derived patient's glioma cell model...
April 18, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28419415/allostery-at-opioid-receptors-modulation-with-small-molecule-ligands
#16
REVIEW
Kathryn E Livingston, John R Traynor
Opioid receptors are 7-transmembrane domain receptors that couple to heterotrimeric G proteins. The endogenous ligands for opioid receptors are peptides which bind to the orthosteric site on the receptors. The μ-opioid receptor is the target for opioid analgesics while the δ-opioid receptor has been suggested as a target for pain management, migraine, and depression. Similarly, κ-opioid receptors are involved in pain and depression and nociceptin receptors in pain and mood behaviors. However, exogenous orthosteric ligands for the opioid receptors cause a myriad of on-target side effects...
April 18, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28419410/selective-and-state-dependent-activation-of-tresk-background-potassium-channel-by-cloxyquin
#17
Miklós Lengyel, Alice Dobolyi, Gábor Czirják, Péter Enyedi
BACKGROUND AND PURPOSE: Cloxyquin (5-cloroquinolin-8-ol) has been previously described as an activator of TRESK (K2P 18.1, TWIK-related spinal cord K(+) channel) background potassium channel. We have examined the specificity of the drug by testing several K2P channels. We have investigated the mechanism of cloxyquin-mediated TRESK activation, focusing on the differences between the physiologically relevant regulatory states of the channel. EXPERIMENTAL APPROACH: Potassium currents were measured by two-electrode voltage clamp in Xenopus oocytes and by whole-cell patch clamp in mouse dorsal root ganglion (DRG) neurons...
April 18, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28409833/dietary-salt-blunts-vasodilation-by-stimulating-epithelial-sodium-channels-in-endothelial-cells-from-salt-sensitive-rats
#18
Zi-Rui Wang, Hui-Bin Liu, Ying-Ying Sun, Qing-Qing Hu, Yu-Xia Li, Wei-Wan Zheng, Chang-Jiang Yu, Xin-Yuan Li, Ming-Ming Wu, Bin-Lin Song, Jian-Jun Mu, Zu-Yi Yuan, Zhi-Ren Zhang, He-Ping Ma
BACKGROUND AND PURPOSE: Our recent studies show that the reduced activity of epithelial sodium channels (ENaC) in endothelial cells accounts for the adaptation of vasculature to salt in Sprague-Dawley (SD) rats. The present study examines a hypothesis that enhanced ENaC activity mediates the loss of vasorelaxation in Dahl salt-sensitive (SS) rats. EXPERIMENTAL APPROACH: We used the cell-attached patch-clamp technique to record ENaC activity in split-open mesenteric arteries...
April 13, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28409826/glycogen-phosphorylase-inhibition-improves-%C3%AE-cell-function
#19
Lilla Nagy, Judit Márton, András Vida, Gréta Kis, Éva Bokor, Sándor Kun, Mónika Gönczi, Tibor Docsa, Attila Tóth, Miklós Antal, Pál Gergely, Balázs Csóka, Pal Pacher, László Somsák, Péter Bai
BACKGROUND AND PURPOSE: Glycogen phosphorylase (GP) is the key enzyme for glycogen degradation. GP inhibitors (GPi-s) are glucose lowering agents trapping glucose in the liver as glycogen. Glycogen metabolism has implications in β-cell function; glycogen degradation can maintain cellular glucose levels, which feeds into catabolism to maintain insulin secretion, and elevated glycogen degradation levels contribute to glucotoxicity. The purpose of this study was to assess whether influencing glycogen metabolism in β-cells by GPi-s impacts β-cell function...
April 13, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28409825/targeting-inflammation-to-reduce-cardiovascular-disease-risk-a-realistic-clinical-prospect
#20
REVIEW
Paul Welsh, Gianluca Grassia, Shani Botha, Naveed Sattar, Pasquale Maffia
Data from basic science experiments is overwhelmingly supportive of the causal role of immune-inflammatory response(s) at the core of atherosclerosis, and therefore the theoretical potential to manipulate the inflammatory response to prevent cardiovascular events. However, extrapolation to humans requires care and we still lack definitive evidence to show that interfering in immune-inflammatory processes may safely lessen clinical atherosclerosis. In this review, we discuss key therapeutic targets in the treatment of vascular inflammation, placing basic research in to a wider clinical perspective, as well as identifying outstanding questions...
April 13, 2017: British Journal of Pharmacology
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