Programme and Abstracts Book
Total Page:16
File Type:pdf, Size:1020Kb
Load more
Recommended publications
-
Multidimensional Analysis of Extended Molecular Dynamics Simulations Shows the Complexity of Signal
bioRxiv preprint doi: https://doi.org/10.1101/604793; this version posted April 18, 2019. The copyright holder for this preprint (which was not certified by peer review) is the author/funder. All rights reserved. No reuse allowed without permission. TITLE Multidimensional analysis of extended molecular dynamics simulations shows the complexity of signal transduction by the histamine H3 membrane receptor Short title: Molecular dynamics of signal transduction AUTHORS Herrera-Zuniga LD1,4, Moreno-Vargas LM2,4, Correa-Basurto J1,3, Prada D2, Curmi P1, Arrang, JM4, Maroun, RC1,4* 1 SABNP, UMR-S U1204, INSERM/Université d’Evry-Val d’Essonne/Université Paris-Saclay, 91025 Evry, FRANCE 2 Computational Biology and Drug Design Research Unit. Federico Gomez Children's Hospital of Mexico City, MEXICO 3 Laboratory for the Design and Development of New Drugs and Biotechnological Innovation) SEPI-ESM, MEXICO 4 INSERM U894, Paris, FRANCE *Corresponding author 1 bioRxiv preprint doi: https://doi.org/10.1101/604793; this version posted April 18, 2019. The copyright holder for this preprint (which was not certified by peer review) is the author/funder. All rights reserved. No reuse allowed without permission. ABSTRACT In this work, we study the mechanisms of activation and inactivation of signal transduction by the histamine H3 receptor (H3R), a 7TM GPCR through extended molecular dynamics (MD) simulations of the receptor embedded in a hydrated double layer of dipalmitoyl phosphatidyl choline (DPPC), a zwitterionic poly-saturated ordered lipid. Three systems were prepared: the apo H3R, representing the constitutively active receptor; and the holo-systems: the H3R coupled to an antagonist/inverse agonist (ciproxifan) and representing the inactive state of the receptor; and the H3R coupled to the endogenous agonist histamine and representing the active state of the receptor. -
Histamine Receptors
Tocris Scientific Review Series Tocri-lu-2945 Histamine Receptors Iwan de Esch and Rob Leurs Introduction Leiden/Amsterdam Center for Drug Research (LACDR), Division Histamine is one of the aminergic neurotransmitters and plays of Medicinal Chemistry, Faculty of Sciences, Vrije Universiteit an important role in the regulation of several (patho)physiological Amsterdam, De Boelelaan 1083, 1081 HV, Amsterdam, The processes. In the mammalian brain histamine is synthesised in Netherlands restricted populations of neurons that are located in the tuberomammillary nucleus of the posterior hypothalamus.1 Dr. Iwan de Esch is an assistant professor and Prof. Rob Leurs is These neurons project diffusely to most cerebral areas and have full professor and head of the Division of Medicinal Chemistry of been implicated in several brain functions (e.g. sleep/ the Leiden/Amsterdam Center of Drug Research (LACDR), VU wakefulness, hormonal secretion, cardiovascular control, University Amsterdam, The Netherlands. Since the seventies, thermoregulation, food intake, and memory formation).2 In histamine receptor research has been one of the traditional peripheral tissues, histamine is stored in mast cells, eosinophils, themes of the division. Molecular understanding of ligand- basophils, enterochromaffin cells and probably also in some receptor interaction is obtained by combining pharmacology specific neurons. Mast cell histamine plays an important role in (signal transduction, proliferation), molecular biology, receptor the pathogenesis of various allergic conditions. After mast cell modelling and the synthesis and identification of new ligands. degranulation, release of histamine leads to various well-known symptoms of allergic conditions in the skin and the airway system. In 1937, Bovet and Staub discovered compounds that antagonise the effect of histamine on these allergic reactions.3 Ever since, there has been intense research devoted towards finding novel ligands with (anti-) histaminergic activity. -
Aldrich Raman
Aldrich Raman Library Listing – 14,033 spectra This library represents the most comprehensive collection of FT-Raman spectral references available. It contains many common chemicals found in the Aldrich Handbook of Fine Chemicals. To create the Aldrich Raman Condensed Phase Library, 14,033 compounds found in the Aldrich Collection of FT-IR Spectra Edition II Library were excited with an Nd:YVO4 laser (1064 nm) using laser powers between 400 - 600 mW, measured at the sample. A Thermo FT-Raman spectrometer (with a Ge detector) was used to collect the Raman spectra. The spectra were saved in Raman Shift format. Aldrich Raman Index Compound Name Index Compound Name 4803 ((1R)-(ENDO,ANTI))-(+)-3- 4246 (+)-3-ISOPROPYL-7A- BROMOCAMPHOR-8- SULFONIC METHYLTETRAHYDRO- ACID, AMMONIUM SALT PYRROLO(2,1-B)OXAZOL-5(6H)- 2207 ((1R)-ENDO)-(+)-3- ONE, BROMOCAMPHOR, 98% 12568 (+)-4-CHOLESTEN-3-ONE, 98% 4804 ((1S)-(ENDO,ANTI))-(-)-3- 3774 (+)-5,6-O-CYCLOHEXYLIDENE-L- BROMOCAMPHOR-8- SULFONIC ASCORBIC ACID, 98% ACID, AMMONIUM SALT 11632 (+)-5-BROMO-2'-DEOXYURIDINE, 2208 ((1S)-ENDO)-(-)-3- 97% BROMOCAMPHOR, 98% 11634 (+)-5-FLUORODEOXYURIDINE, 769 ((1S)-ENDO)-(-)-BORNEOL, 99% 98+% 13454 ((2S,3S)-(+)- 11633 (+)-5-IODO-2'-DEOXYURIDINE, 98% BIS(DIPHENYLPHOSPHINO)- 4228 (+)-6-AMINOPENICILLANIC ACID, BUTANE)(N3-ALLYL)PD(II) CL04, 96% 97 8167 (+)-6-METHOXY-ALPHA-METHYL- 10297 ((3- 2- NAPHTHALENEACETIC ACID, DIMETHYLAMINO)PROPYL)TRIPH 98% ENYL- PHOSPHONIUM BROMIDE, 12586 (+)-ANDROSTA-1,4-DIENE-3,17- 99% DIONE, 98% 13458 ((R)-(+)-2,2'- 963 (+)-ARABINOGALACTAN BIS(DIPHENYLPHOSPHINO)-1,1'- -
1 Abietic Acid R Abrasive Silica for Polishing DR Acenaphthene M (LC
1 abietic acid R abrasive silica for polishing DR acenaphthene M (LC) acenaphthene quinone R acenaphthylene R acetal (see 1,1-diethoxyethane) acetaldehyde M (FC) acetaldehyde-d (CH3CDO) R acetaldehyde dimethyl acetal CH acetaldoxime R acetamide M (LC) acetamidinium chloride R acetamidoacrylic acid 2- NB acetamidobenzaldehyde p- R acetamidobenzenesulfonyl chloride 4- R acetamidodeoxythioglucopyranose triacetate 2- -2- -1- -β-D- 3,4,6- AB acetamidomethylthiazole 2- -4- PB acetanilide M (LC) acetazolamide R acetdimethylamide see dimethylacetamide, N,N- acethydrazide R acetic acid M (solv) acetic anhydride M (FC) acetmethylamide see methylacetamide, N- acetoacetamide R acetoacetanilide R acetoacetic acid, lithium salt R acetobromoglucose -α-D- NB acetohydroxamic acid R acetoin R acetol (hydroxyacetone) R acetonaphthalide (α)R acetone M (solv) acetone ,A.R. M (solv) acetone-d6 RM acetone cyanohydrin R acetonedicarboxylic acid ,dimethyl ester R acetonedicarboxylic acid -1,3- R acetone dimethyl acetal see dimethoxypropane 2,2- acetonitrile M (solv) acetonitrile-d3 RM acetonylacetone see hexanedione 2,5- acetonylbenzylhydroxycoumarin (3-(α- -4- R acetophenone M (LC) acetophenone oxime R acetophenone trimethylsilyl enol ether see phenyltrimethylsilyl... acetoxyacetone (oxopropyl acetate 2-) R acetoxybenzoic acid 4- DS acetoxynaphthoic acid 6- -2- R 2 acetylacetaldehyde dimethylacetal R acetylacetone (pentanedione -2,4-) M (C) acetylbenzonitrile p- R acetylbiphenyl 4- see phenylacetophenone, p- acetyl bromide M (FC) acetylbromothiophene 2- -5- -
Biomedical Applications of Polymeric Cryogels
applied sciences Review Biomedical Applications of Polymeric Cryogels Monireh Bakhshpour 1, Neslihan Idil 2, I¸sıkPerçin 2 and Adil Denizli 1,* 1 Department of Chemistry, Faculty of Science, Hacettepe University, Ankara 06800, Turkey; [email protected] 2 Department of Biology, Faculty of Science, Hacettepe University, Ankara 06800, Turkey; [email protected] (N.I.); [email protected] (I.P.) * Correspondence: [email protected]; Tel.: +90-312-297-7983 Received: 31 December 2018; Accepted: 4 February 2019; Published: 7 February 2019 Featured Application: This study presents the comprehensive applications of polymeric cryogels in the field of biomedicine. To the best of our knowledge, this review is one of the most pioneering paper comparatively explains the biomedical applications of cryogels in detail. Abstract: The application of interconnected supermacroporous cryogels as support matrices for the purification, separation and immobilization of whole cells and different biological macromolecules has been well reported in literature. Cryogels have advantages over traditional gel carriers in the field of biochromatography and related biomedical applications. These matrices nearly mimic the three-dimensional structure of native tissue extracellular matrix. In addition, mechanical, osmotic and chemical stability of cryogels make them attractive polymeric materials for the construction of scaffolds in tissue engineering applications and in vitro cell culture, separation materials for many different processes such as immobilization of biomolecules, capturing of target molecules, and controlled drug delivery. The low mass transfer resistance of cryogel matrices makes them useful in chromatographic applications with the immobilization of different affinity ligands to these materials. Cryogels have been introduced as gel matrices prepared using partially frozen monomer or polymer solutions at temperature below zero. -
Phytochem Referenzsubstanzen
High pure reference substances Phytochem Hochreine Standardsubstanzen for research and quality für Forschung und management Referenzsubstanzen Qualitätssicherung Nummer Name Synonym CAS FW Formel Literatur 01.286. ABIETIC ACID Sylvic acid [514-10-3] 302.46 C20H30O2 01.030. L-ABRINE N-a-Methyl-L-tryptophan [526-31-8] 218.26 C12H14N2O2 Merck Index 11,5 01.031. (+)-ABSCISIC ACID [21293-29-8] 264.33 C15H20O4 Merck Index 11,6 01.032. (+/-)-ABSCISIC ACID ABA; Dormin [14375-45-2] 264.33 C15H20O4 Merck Index 11,6 01.002. ABSINTHIN Absinthiin, Absynthin [1362-42-1] 496,64 C30H40O6 Merck Index 12,8 01.033. ACACETIN 5,7-Dihydroxy-4'-methoxyflavone; Linarigenin [480-44-4] 284.28 C16H12O5 Merck Index 11,9 01.287. ACACETIN Apigenin-4´methylester [480-44-4] 284.28 C16H12O5 01.034. ACACETIN-7-NEOHESPERIDOSIDE Fortunellin [20633-93-6] 610.60 C28H32O14 01.035. ACACETIN-7-RUTINOSIDE Linarin [480-36-4] 592.57 C28H32O14 Merck Index 11,5376 01.036. 2-ACETAMIDO-2-DEOXY-1,3,4,6-TETRA-O- a-D-Glucosamine pentaacetate 389.37 C16H23NO10 ACETYL-a-D-GLUCOPYRANOSE 01.037. 2-ACETAMIDO-2-DEOXY-1,3,4,6-TETRA-O- b-D-Glucosamine pentaacetate [7772-79-4] 389.37 C16H23NO10 ACETYL-b-D-GLUCOPYRANOSE> 01.038. 2-ACETAMIDO-2-DEOXY-3,4,6-TRI-O-ACETYL- Acetochloro-a-D-glucosamine [3068-34-6] 365.77 C14H20ClNO8 a-D-GLUCOPYRANOSYLCHLORIDE - 1 - High pure reference substances Phytochem Hochreine Standardsubstanzen for research and quality für Forschung und management Referenzsubstanzen Qualitätssicherung Nummer Name Synonym CAS FW Formel Literatur 01.039. -
Untersuchungen Zur Transmission Des Über Den Histamin-4-Rezeptor Induzierten Juckreizsignals
Tierärztliche Hochschule Hannover Untersuchungen zur Transmission des über den Histamin-4-Rezeptor induzierten Juckreizsignals INAUGURAL - DISSERTATION zur Erlangung des Grades einer Doktorin der Veterinärmedizin - Doctor medicinae veterinariae - (Dr. med. vet.) vorgelegt von Jenny Wilzopolski Brunsbüttel Hannover 2017 Wissenschaftliche Betreuung: Prof. Dr. med. vet. Manfred Kietzmann Institut für Pharmakologie, Toxikologie und Pharmazie 1. Gutachter: Prof. Dr. med. vet. Manfred Kietzmann 2. Gutachter: Prof. Dr. med. vet. Reinhard Mischke Tag der mündlichen Prüfung: 06.11.2017 Die Arbeit wurde gefördert durch die Deutsche Forschungsgemeinschaft. I "Leicht ist das Leben für keinen von uns. Doch was nützt das, man muß Ausdauer haben und Zutrauen zu sich selbst. Man muß daran glauben, für eine bestimmte Sache begabt zu sein, und diese Sache muß man erreichen, koste es was es wolle." -Marie Curie- Für meine Familie II III Inhaltsverzeichnis Inhaltsverzeichnis Inhaltsverzeichnis ...................................................................................................................... iv Abbildungsverzeichnis ............................................................................................................ viii Tabellenverzeichnis .................................................................................................................... x Abkürzungsverzeichnis ............................................................................................................ xii 1. Einleitung ............................................................................................................................. -
G Protein-Coupled Receptors
S.P.H. Alexander et al. The Concise Guide to PHARMACOLOGY 2015/16: G protein-coupled receptors. British Journal of Pharmacology (2015) 172, 5744–5869 THE CONCISE GUIDE TO PHARMACOLOGY 2015/16: G protein-coupled receptors Stephen PH Alexander1, Anthony P Davenport2, Eamonn Kelly3, Neil Marrion3, John A Peters4, Helen E Benson5, Elena Faccenda5, Adam J Pawson5, Joanna L Sharman5, Christopher Southan5, Jamie A Davies5 and CGTP Collaborators 1School of Biomedical Sciences, University of Nottingham Medical School, Nottingham, NG7 2UH, UK, 2Clinical Pharmacology Unit, University of Cambridge, Cambridge, CB2 0QQ, UK, 3School of Physiology and Pharmacology, University of Bristol, Bristol, BS8 1TD, UK, 4Neuroscience Division, Medical Education Institute, Ninewells Hospital and Medical School, University of Dundee, Dundee, DD1 9SY, UK, 5Centre for Integrative Physiology, University of Edinburgh, Edinburgh, EH8 9XD, UK Abstract The Concise Guide to PHARMACOLOGY 2015/16 provides concise overviews of the key properties of over 1750 human drug targets with their pharmacology, plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. The full contents can be found at http://onlinelibrary.wiley.com/doi/ 10.1111/bph.13348/full. G protein-coupled receptors are one of the eight major pharmacological targets into which the Guide is divided, with the others being: ligand-gated ion channels, voltage-gated ion channels, other ion channels, nuclear hormone receptors, catalytic receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. -
G Protein‐Coupled Receptors
S.P.H. Alexander et al. The Concise Guide to PHARMACOLOGY 2019/20: G protein-coupled receptors. British Journal of Pharmacology (2019) 176, S21–S141 THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein-coupled receptors Stephen PH Alexander1 , Arthur Christopoulos2 , Anthony P Davenport3 , Eamonn Kelly4, Alistair Mathie5 , John A Peters6 , Emma L Veale5 ,JaneFArmstrong7 , Elena Faccenda7 ,SimonDHarding7 ,AdamJPawson7 , Joanna L Sharman7 , Christopher Southan7 , Jamie A Davies7 and CGTP Collaborators 1School of Life Sciences, University of Nottingham Medical School, Nottingham, NG7 2UH, UK 2Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, Victoria 3052, Australia 3Clinical Pharmacology Unit, University of Cambridge, Cambridge, CB2 0QQ, UK 4School of Physiology, Pharmacology and Neuroscience, University of Bristol, Bristol, BS8 1TD, UK 5Medway School of Pharmacy, The Universities of Greenwich and Kent at Medway, Anson Building, Central Avenue, Chatham Maritime, Chatham, Kent, ME4 4TB, UK 6Neuroscience Division, Medical Education Institute, Ninewells Hospital and Medical School, University of Dundee, Dundee, DD1 9SY, UK 7Centre for Discovery Brain Sciences, University of Edinburgh, Edinburgh, EH8 9XD, UK Abstract The Concise Guide to PHARMACOLOGY 2019/20 is the fourth in this series of biennial publications. The Concise Guide provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. Although the Concise Guide represents approximately 400 pages, the material presented is substantially reduced compared to information and links presented on the website. -
Protein Modification and Catabolic Fates of Lipid
PROTEIN MODIFICATION AND CATABOLIC FATES OF LIPID PEROXIDATION PRODUCTS by CHUAN SHI Submitted in partial fulfillment of the requirements for the Degree of Doctor of Philosophy Dissertation Advisor: Gregory P. Tochtrop, Ph.D. Department of Chemistry CASE WESTERN RESERVE UNIVERSITY January 2017 CASE WESTERN RESERVE UNIVERSITY SCHOOL OF GRADUATE STUDIES We hereby approve the dissertation of ______________________________________________________Chuan Shi candidate for the Doctor of Philosophy degree *. Rajesh Viswanathan (signed)_______________________________________________ (chair of the committee) Anthony Pearson ________________________________________________ Michael Zagorski ________________________________________________ Henri Brunengraber ________________________________________________ Gregory Tochtrop ________________________________________________ ________________________________________________ (date) _______________________Dec. 8, 2016 *We also certify that written approval has been obtained for any proprietary material contained therein. This thesis is dedicated to my parents in the deepest appreciation and gratitude for their unconditional love, endless support and continuous encouragement throughout every step in my life TABLE OF CONTENTS Table of Contents ................................................................................................................. i List of Figures ......................................................................................................................v List of Schemes ................................................................................................................ -
International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors
1521-0081/67/3/601–655$25.00 http://dx.doi.org/10.1124/pr.114.010249 PHARMACOLOGICAL REVIEWS Pharmacol Rev 67:601–655, July 2015 Copyright © 2015 by The American Society for Pharmacology and Experimental Therapeutics ASSOCIATE EDITOR: ELIOT H. OHLSTEIN International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors Pertti Panula, Paul L. Chazot, Marlon Cowart, Ralf Gutzmer, Rob Leurs, Wai L. S. Liu, Holger Stark, Robin L. Thurmond, and Helmut L. Haas Department of Anatomy, and Neuroscience Center, University of Helsinki, Finland (P.P.); School of Biological and Biomedical Sciences, University of Durham, United Kingdom (P.L.C.); AbbVie, Inc. North Chicago, Illinois (M.C.); Department of Dermatology and Allergy, Hannover Medical School, Hannover, Germany (R.G.); Department of Medicinal Chemistry, Amsterdam Institute of Molecules, Medicines and Systems, VU University Amsterdam, The Netherlands (R.L.); Ziarco Pharma Limited, Canterbury, United Kingdom (W.L.S.L.); Institute of Pharmaceutical and Medical Chemistry (H.S.) and Institute of Neurophysiology, Medical Faculty (H.L.H.), Heinrich-Heine-University Duesseldorf, Germany; and Janssen Research & Development, LLC, San Diego, California (R.L.T.) Abstract ....................................................................................602 Downloaded from I. Introduction and Historical Perspective .....................................................602 II. Histamine H1 Receptor . ..................................................................604 A. Receptor Structure -
Histamine Inhibits the Production of Interleukin-12 Through Interaction with H2 Receptors
Histamine inhibits the production of interleukin-12 through interaction with H2 receptors. T C van der Pouw Kraan, … , R Leurs, L A Aarden J Clin Invest. 1998;102(10):1866-1873. https://doi.org/10.1172/JCI3692. Research Article IL-12 is essential for T helper 1 (Th1) development and inhibits the induction of Th2 responses. Atopic diseases, which are characterized by Th2 responses, are associated with the overproduction of histamine. Here we present evidence that histamine, at physiological concentrations, strongly inhibits human IL-12 p40 and p70 mRNA and protein production by human monocytes. The use of specific histamine receptor antagonists reveals that this inhibition is mediated via the H2 receptor and induction of intracellular cAMP. The inhibition of IL-12 production is independent of IL-10 and IFN-gamma. The observation that histamine strongly reduces the production of the Th1-inducing cytokine IL-12 implies a positive feedback mechanism for the development of Th2 responses in atopic patients. Find the latest version: https://jci.me/3692/pdf Histamine Inhibits the Production of Interleukin-12 through Interaction with H2 Receptors Tineke C.T.M. van der Pouw Kraan,* Alies Snijders,‡ Leonie C.M. Boeije,* Els R. de Groot,* Astrid E. Alewijnse,§ Rob Leurs,§ and Lucien A. Aarden* *CLB, Sanquin Blood Supply Foundation, Department of Auto-Immune Diseases, Laboratory for Experimental and Clinical Immunology, Academic Medical Centre, University of Amsterdam, 1066CX Amsterdam, The Netherlands; ‡Laboratory of Cell Biology and Histology, Academic Medical Centre, 1105 AZ Amsterdam, The Netherlands; and §Department of Pharmacochemistry, Free University, Leiden/Amsterdam Centre for Drug Research, 1081 HV Amsterdam, The Netherlands Abstract a Th2 response (4–6), while various organ-specific autoim- mune diseases are characterized by Th1-like responses (7).