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Pharmacology

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https://www.readbyqxmd.com/read/30242974/discovery-of-a-small-molecule-modulator-of-the-kv1-1-kv%C3%AE-1-channel-complex-that-reduces-neuronal-excitability-and-in-vitro-epileptiform-activity
#1
Isabelle Niespodziany, Brice Mullier, Véronique Marie André, Philippe Ghisdal, Eric Jnoff, David Moreno-Delgado, Dominique Swinnen, Zara Sands, Martyn Wood, Christian Wolff
AIMS: Kv1.1 (KCNA1) channels contribute to the control of neuronal excitability and have been associated with epilepsy. Kv1.1 channels can associate with the cytoplasmic Kvβ1 subunit resulting in rapid inactivating A-type currents. We hypothesized that removal of channel inactivation, by modulating Kv1.1/Kvβ1 interaction with a small molecule, would lead to decreased neuronal excitability and anticonvulsant activity. METHODS: We applied high-throughput screening to identify ligands able to modulate the Kv1...
September 21, 2018: CNS Neuroscience & Therapeutics
https://www.readbyqxmd.com/read/30242840/nha2-promotes-cyst-development-in-an-in-vitro-model-of-polycystic-kidney-disease
#2
Hari Prasad, Donna K Dang, Kalyan C Kondapalli, Niranjana Natarajan, Valeriu Cebotaru, Rajini Rao
We observed significant and selective up-regulation of the Na+ /H+ exchanger NHA2 (SLC9B2) in cysts of patients with autosomal dominant polycystic kidney disease. Using the MDCK model of cystogenesis, we find NHA2 increases cyst size. Silencing or pharmacological inhibition of NHA2 inhibits cyst formation in vitro. Polycystin-1 represses NHA2 expression via Ca2+ /NFAT signalling whereas the dominant negative membrane-anchored C-terminal fragment (PC1-MAT) increased NHA2 levels. Drugs (caffeine, theophylline) and hormones (vasopressin, aldosterone) known to exacerbate cysts elicit NHA2 expression...
September 22, 2018: Journal of Physiology
https://www.readbyqxmd.com/read/30242797/comparative-in-vivo-constituents-and-pharmacokinetic-study-in-rats-after-oral-administration-of-ultrafine-granular-powder-and-traditional-decoction-slices-of-chinese-salvia
#3
Haijuan Zhi, Zhenwei Li, Yanping Deng, Peng Qi, Jinjun Hou, Wen Deng, Jinle Cheng, Wanying Wu, Dean Guo
Salvia miltiorrhiza, one of the most famous herbal medicines, is commonly used for the treatment of coronary heart diseases in China. Besides traditional decoction pieces, another relatively new product of S. miltiorrhiza, Ultrafine Granular Powder (D90 < 45 μm), is also increasingly used nowadays. In this paper, a UHPLC-LTQ-Orbitrap MS technique was developed for metabolite profile study after oral administration of Ultrafine Granular Powder (UGP) and Traditional Decoction Slices (TDS) of S. miltiorrhiza...
September 21, 2018: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/30242764/evaluation-and-characterization-of-endothelial-cell-invasion-and-sprouting-behavior
#4
Jocelynda Salvador, George E Davis
Here, we describe highly reproducible methods to investigate human EC invasion and sprouting behavior in 3D collagen matrices. Two assay models are presented whereby ECs are induced to sprout from a monolayer surface or from aggregated ECs suspended within a collagen gel matrix. In each case, the assays are performed using serum-free defined media containing a combination of five growth factors (Factors): FGF-2, SCF, IL-3, SDF-1α, and insulin. In both models, marked EC sprouting occurs with leading EC tip cells over a 12-24 h period...
2018: Methods in Molecular Biology
https://www.readbyqxmd.com/read/30242717/measurement-of-the-multiple-activities-of-26s-proteasomes
#5
Hyoung Tae Kim, Galen Andrew Collins, Alfred L Goldberg
Because proteasomes catalyze most of the protein degradation in mammalian cells, and their functioning is essential for cellular homeostasis, proteasome structure, biochemical mechanisms, and regulation in normal and disease states are now widely studied and are of major importance. In addition, inhibitors of the proteasome's peptidase activity have proven to be very valuable as research tools and in the treatment of hematologic malignancies, and a number of newer pharmacological agents that alter proteasome function are being developed...
2018: Methods in Molecular Biology
https://www.readbyqxmd.com/read/30242716/methods-to-rapidly-prepare-mammalian-26s-proteasomes-for-biochemical-analysis
#6
Chueh-Ling Kuo, Galen Andrew Collins, Alfred L Goldberg
Rapid, gentle isolation of 26S proteasomes from cells or tissues is an essential step for studies of the changes in proteasome activity and composition that can occur under different physiological or pathological conditions and in response to pharmacological agents. We present here three different approaches to affinity purify or to prepare proteasome-rich cell fractions. The first method uses affinity tags fused to proteasome subunits and has been useful in several cell lines for studies of proteasome structure by cryo-electron microscopy and composition by mass spectrometry...
2018: Methods in Molecular Biology
https://www.readbyqxmd.com/read/30242673/determination-of-synthetic-pharmaceutical-adulterants-in-herbal-weight-gain-supplements-sold-in-herb-shops-tehran-iran
#7
Niosha Saberi, Maryam Akhgari, Leila Bahmanabadi, Elham Bazmi, Zahra Mousavi
BACKGROUND: Nowadays with the growing popularity of herbal remedies across the world, large sections of population rely on herbal drug practitioners for their primary care. Therefore there is a need to ensure about the safety of herbal drugs and to detect adulteration with undeclared active pharmaceutical ingredients. Herbal drugs are used as first-line drug therapy in some instances. Unfortunately even if there are claims as to be natural, undeclared active pharmaceutical ingredients have been detected in these supplements...
September 21, 2018: Daru: Journal of Faculty of Pharmacy, Tehran University of Medical Sciences
https://www.readbyqxmd.com/read/30242672/identification-and-anti-cancer-activity-in-2d-and-3d-cell-culture-evaluation-of-an-iranian-isolated-marine-microalgae-picochlorum-sp-rcc486
#8
Mohammad Haji Abolhasani, Maliheh Safavi, Mohammad Taghi Goodarzi, Seyed Mehrdad Kassaee, Mehrdad Azin
PURPOSE: Cancer disease is the second cause of death in the world. Now a days, high percentage of drugs, which are involved in treatment of cancers, have natural origin. Introduction of microalgae strains as anti-cancer drugs origin is a valuable approach for cancer therapy. METHODS: In the present study we describe the isolation, characterization, and anti-proliferative activity of a new microalga strain (Picochlorum sp. RCC486) from Iran. The cytotoxic activity of four different algal extracts including methanol, ethyl acetate, chloroform, and hexane were evaluated against MDA-MB-231, MCF-7, Hep-G2, and A-549 cell liens...
September 21, 2018: Daru: Journal of Faculty of Pharmacy, Tehran University of Medical Sciences
https://www.readbyqxmd.com/read/30242552/lessons-learned-in-attempting-catheter-based-interatrial-electrical-disconnection-for-nonpharmacologic-rate-control-of-atrial-fibrillation-or-flutter
#9
José Luis Ibáñez, Alicia Ibáñez, Teresa Barrio, Mercedes Ortiz, Raquel Ajo, Eduardo Castellanos, Santiago Heras, Thomas Brouzet, Jessica Sánchez, María Ajo, Enrique Garcia, Juan Gabriel Martínez, Francisco Sogorb, Jesús Almendral
PURPOSE: Ablation of atrioventricular (AV) conduction and pacemaker implantation is the therapy of last resort for symptomatic atrial tachyarrythmias when rhythm and rate control fail, but is far from ideal. To evaluate whether interatrial electrical disconnection as a result of catheter ablation is feasible and of potential clinical utility as a means of non-pharmacological heart rate control. METHODS: Eleven patients with medically refractory atrial fibrillation or left atrial flutter and symptomatic rapid ventricular response were included...
September 21, 2018: Journal of Interventional Cardiac Electrophysiology: An International Journal of Arrhythmias and Pacing
https://www.readbyqxmd.com/read/30242521/sex-differences-in-the-management-of-advanced-heart-failure
#10
REVIEW
Daniela R Crousillat, Nasrien E Ibrahim
PURPOSE OF REVIEW: Heart failure (HF) is prevalent among women and remains a leading cause of morbidity and mortality in the United States. Currently, 3 million women live with HF and the prevalence is projected to continue to increase. The purpose of this review is to highlight sex differences in the use and response to evidence-based pharmacological, device, and advanced HF therapies, as well as explore emerging areas of research in sex differences in the treatment of HF. RECENT FINDINGS: Under-representation of women in clinical HF trials has limited our understanding of sex-related differences in the treatment and outcomes of HF...
September 21, 2018: Current Treatment Options in Cardiovascular Medicine
https://www.readbyqxmd.com/read/30242519/migraine-and-cluster-headache-the-common-link
#11
Anne Luise Vollesen, Silvia Benemei, Francesca Cortese, Alejandro Labastida-Ramírez, Francesca Marchese, Lanfranco Pellesi, Michele Romoli, Messoud Ashina, Christian Lampl
Although clinically distinguishable, migraine and cluster headache share prominent features such as unilateral pain, common pharmacological triggers such glyceryl trinitrate, histamine, calcitonin gene-related peptide (CGRP) and response to triptans and neuromodulation. Recent data also suggest efficacy of anti CGRP monoclonal antibodies in both migraine and cluster headache. While exact mechanisms behind both disorders remain to be fully understood, the trigeminovascular system represents one possible common pathophysiological pathway and network of both disorders...
September 21, 2018: Journal of Headache and Pain
https://www.readbyqxmd.com/read/30242487/epigenetic-signature-of-maoa-and-maob-genes-in-mental-disorders
#12
REVIEW
Christiane Ziegler, Katharina Domschke
Epigenetic processes such as DNA methylation are considered key mechanisms at the crossroads between genetics and environment in the etiology of mental disorders. The monoamine oxidases A and B (MAOA/MAOB) are prime candidates for the investigation into the role of DNA methylation in mental disorders, given their pivotal role in the metabolism of monoamines and as pharmacological targets of potent antidepressant drugs such as tranylcypromine, phenelzine or moclobemide. The present mini-review aims at summarizing and critically discussing the growing body of the literature supporting a role of DNA methylation of the MAOA gene promoter/exon I/intron I region and its interaction with environmental factors in several mental disorders, i...
September 21, 2018: Journal of Neural Transmission
https://www.readbyqxmd.com/read/30242423/annals-on-call-oral-pharmacologic-therapy-in-type-2-diabetes-choosing-therapy-wisely
#13
Robert M Centor, Michael J Barry
No abstract text is available yet for this article.
September 18, 2018: Annals of Internal Medicine
https://www.readbyqxmd.com/read/30242258/notch2-controls-non-autonomous-wnt-signalling-in-chronic-lymphocytic-leukaemia
#14
Maurizio Mangolini, Frederik Götte, Andrew Moore, Tim Ammon, Madlen Oelsner, Gloria Lutzny-Geier, Ludger Klein-Hitpass, James C Williamson, Paul J Lehner, Jan Dürig, Michael Möllmann, Lívia Rásó-Barnett, Katherine Hughes, Antonella Santoro, Simón Méndez-Ferrer, Robert A J Oostendorp, Ursula Zimber-Strobl, Christian Peschel, Daniel J Hodson, Marc Schmidt-Supprian, Ingo Ringshausen
The Wnt signalling pathway, one of the core de-regulated pathways in chronic lymphocytic leukaemia (CLL), is activated in only a subset of patients through somatic mutations. Here we describe alternative, microenvironment-dependent mechanisms of Wnt activation in malignant B cells. We show that tumour cells specifically induce Notch2 activity in mesenchymal stromal cells (MSCs) required for the transcription of the complement factor C1q. MSC-derived C1q in turn inhibits Gsk3-β mediated degradation of β-catenin in CLL cells...
September 21, 2018: Nature Communications
https://www.readbyqxmd.com/read/30242175/vps34-mediated-macropinocytosis-in-tuberous-sclerosis-complex-2-deficient-cells-supports-tumorigenesis
#15
Harilaos Filippakis, Amine Belaid, Brian Siroky, Constance Wu, Nicola Alesi, Thomas Hougard, Julie Nijmeh, Hilaire C Lam, Elizabeth P Henske
Tuberous Sclerosis Complex (TSC), a rare genetic disorder with mechanistic target of rapamycin complex 1 (mTORC1) hyperactivation, is characterized by multi-organ hamartomatous benign tumors including brain, skin, kidney, and lung (Lymphangioleiomyomatosis). mTORC1 hyperactivation drives metabolic reprogramming including glucose and glutamine utilization, protein, nucleic acid and lipid synthesis. To investigate the mechanisms of exogenous nutrients uptake in Tsc2-deficient cells, we measured dextran uptake, a polysaccharide internalized via macropinocytosis...
September 21, 2018: Scientific Reports
https://www.readbyqxmd.com/read/30242159/alpha-enolase-regulates-the-malignant-phenotype-of-pulmonary-artery-smooth-muscle-cells-via-the-ampk-akt-pathway
#16
Jingbo Dai, Qiyuan Zhou, Jiwang Chen, Megan L Rexius-Hall, Jalees Rehman, Guofei Zhou
The molecular mechanisms underlying the metabolic shift toward increased glycolysis observed in pulmonary artery smooth muscle cells (PASMC) during the pathogenesis of pulmonary arterial hypertension (PAH) are not fully understood. Here we show that the glycolytic enzyme α-enolase (ENO1) regulates the metabolic reprogramming and malignant phenotype of PASMC. We show that ENO1 levels are elevated in patients with associated PAH and in animal models of hypoxic pulmonary hypertension (HPH). The silencing or inhibition of ENO1 decreases PASMC proliferation and de-differentiation, and induces PASMC apoptosis, whereas the overexpression of ENO1 promotes a synthetic, de- differentiated, and apoptotic-resistant phenotype via the AMPK-Akt pathway...
September 21, 2018: Nature Communications
https://www.readbyqxmd.com/read/30242135/hypoxia-inducible-factor-1-dependent-expression-of-adenosine-receptor-2b-promotes-breast-cancer-stem-cell-enrichment
#17
Jie Lan, Haiquan Lu, Debangshu Samanta, Shaima Salman, You Lu, Gregg L Semenza
Breast cancer stem cells (BCSCs), which are characterized by a capacity for unlimited self-renewal and for generation of the bulk cancer cell population, play a critical role in cancer relapse and metastasis. Hypoxia is a common feature of the cancer microenvironment that stimulates the specification and maintenance of BCSCs. In this study, we found that hypoxia increased expression of adenosine receptor 2B (A2BR) in human breast cancer cells through the transcriptional activity of hypoxia-inducible factor 1...
September 21, 2018: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/30242130/the-scaffolding-protein-zo-1-coordinates-actomyosin-and-epithelial-apical-specializations-in-vitro-and-in-vivo
#18
Matthew A Odenwald, Wangsun Choi, Wei-Ting Kuo, Gurminder Singh, Anne Sailer, Yitang Wang, Le Shen, Alan S Fanning, Jerrold R Turner
Polarized epithelia assemble into sheets that compartmentalize organs and generate tissue barriers by integrating apical surfaces into a single, unified structure. This tissue organization is shared across organs, species, and developmental stages. The processes that regulate development and maintenance of apical epithelial surfaces are, however, undefined. Here, using an intestinal epithelial-specific knockout (KO) mouse and cultured epithelial cells, we show that the tight junction scaffolding protein zonula occludens-1 (ZO-1) is essential for development of unified apical surfaces in vivo and in vitro...
September 21, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/30242129/complex-formation-of-sphingomyelin-synthase-1-with-glucosylceramide-synthase-increases-sphingomyelin-and-decreases-glucosylceramide-levels
#19
Yasuhiro Hayashi, Yoko Nemoto-Sasaki, Naoki Matsumoto, Kotaro Hama, Takashi Tanikawa, Saori Oka, Tadaaki Saeki, Tatsuya Kumasaka, Takanori Koizumi, Seisuke Arai, Ikuo Wada, Kazuaki Yokoyama, Takayuki Sugiura, Atsushi Yamashita
Sphingolipids, including sphingomyelin (SM) and glucosylceramide (GlcCer), are generated by the addition of a polar head group to ceramide (Cer). Sphingomyelin synthase 1 (SMS1) and glucosylceramide synthase (GCS) are key enzymes that catalyze the conversion of Cer to SM and GlcCer, respectively. GlcCer synthesis has been postulated to occur mainly in cis-Golgi, and SM synthesis is thought to occur in medial/trans-Golgi; however, SMS1 and GCS are known to partially colocalize in cisternae, especially in medial/trans-Golgi...
September 21, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/30242115/the-creatine-kinase-system-as-a-therapeutic-target-for-myocardial-ischaemia-reperfusion-injury
#20
REVIEW
Fang Cao, Sevasti Zervou, Craig A Lygate
Restoring blood flow following an acute myocardial infarction saves lives, but results in tissue damage due to ischaemia-reperfusion injury (I/R). Ameliorating this damage is a major research goal to improve recovery and reduce subsequent morbidity due to heart failure. Both the ischaemic and reperfusion phases represent crises of cellular energy provision in which the mitochondria play a central role. This mini-review will explore the rationale and therapeutic potential of augmenting the creatine kinase (CK) energy shuttle, which constitutes the primary short-term energy buffer and transport system in the cardiomyocyte...
September 20, 2018: Biochemical Society Transactions
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