Relationship Between Primary Structure and Activity in Exorphins and Endogenous Opioid Peptides
Total Page:16
File Type:pdf, Size:1020Kb
Load more
Recommended publications
-
Evaluation of in Silico Approach for Prediction of Presence of Opioid Peptides in Wheat
Evaluation of in silico approach for prediction of presence of opioid peptides in wheat This is the Accepted version of the following publication Garg, Swati, Apostolopoulos, Vasso, Nurgali, Kulmira and Mishra, Vijay Kumar (2018) Evaluation of in silico approach for prediction of presence of opioid peptides in wheat. Journal of Functional Foods, 41. 34 - 40. ISSN 1756-4646 The publisher’s official version can be found at https://www.sciencedirect.com/science/article/pii/S1756464617307454 Note that access to this version may require subscription. Downloaded from VU Research Repository https://vuir.vu.edu.au/36577/ 1 1 Evaluation of in silico approach for prediction of presence of opioid peptides in wheat 2 gluten 3 Abstract 4 Opioid like morphine and codeine are used for the management of pain, but are associated 5 with serious side-effects limiting their use. Wheat gluten proteins were assessed for the 6 presence of opioid peptides on the basis of tyrosine and proline within their sequence. Eleven 7 peptides were identified and occurrence of predicted sequences or their structural motifs were 8 analysed using BIOPEP database and ranked using PeptideRanker. Based on higher peptide 9 ranking, three sequences YPG, YYPG and YIPP were selected for determination of opioid 10 activity by cAMP assay against µ and κ opioid receptors. Three peptides inhibited the 11 production of cAMP to varied degree with EC50 values of YPG, YYPG and YIPP were 5.3 12 mM, 1.5 mM and 2.9 mM for µ-opioid receptor, and 1.9 mM, 1.2 mM and 3.2 mM for κ- 13 opioid receptor, respectively. -
2019-2020 Award Recipients
2019-2020 AWARD RECIPIENTS The Office of Undergraduate Research and Creative Activities is pleased to announce the MAYS and RPG recipients for the 2019-2020 academic year. Please join us in congratulating these students and their faculty mentors. Major Academic Year Support (MAYS) Student: Kelly Ackerly Mentor: Dr. Daniel Greenberg Major: Psychology Department: Psychology An Exploration of Maternal Factors Affecting Children’s Autobiographical Memory In day-to-day interactions, mothers and their young children discuss memories of events they have experienced. Research has demonstrated the relationship between these interactions and the development of children’s memories. It is through these interactions that children learn how to interpret personal experiences and develop the skill of talking about them with others in a coherent way. Additionally, studies have found that children are more likely to form false memories—that is, inaccurate “memories” of events that did not actually occur – because their memories are more easily manipulated. In this study, we will explore whether the way mothers talk to their children about ambiguous events affects the children’s interpretations and memories of the event. We will also attempt to determine if there is a relationship between mothers’ negativity during discussions and their child’s formation of false memories. To explore this idea, mothers and their children (aged 3 to 6 years) are given a handful of ambiguous situations to interpret separately. Children are given the opportunity to make slime with a research assistant while a second research assistant acts out ambiguous situations that could have a positive or negative interpretation. The children are evaluated on the way they interpret the situations and whether they form a negative false memory. -
Characterisation and Partial Purification of a Novel Prohormone Processing Enzyme from Ovine Adrenal Medulla
Volume 246, number 1,2, 44-48 FEB 06940 March 1989 Characterisation and partial purification of a novel prohormone processing enzyme from ovine adrenal medulla N. Tezapsidis and D.C. Parish Biochemistry Group, School of Biological Sciences, University of Sussex, Falmer, Brighton, Sussex, England Received 3 January 1989 An enzymatic activity has been identified which is capable of generating a product chromatographically identical with adrenorphin from the model substrate BAM 12P. This enzyme was purified by gel filtration and ion-exchange chromatog- raphy and characterised as having a molecular mass between 30 and 45 kDa and an acidic pL The enzyme is active at the acid pH expected in the secretory vesicle interior and is inhibited by EDTA, suggesting that it is a metalloprotease. This activity could not be mimicked by incubation with lysosomal fractions and it meets the criteria to be considered as a possible prohormone processing enzyme. Prohormone processing; Adrenorphin; Secretory vesiclepurification 1. INTRODUCTION The purification of an endopeptidase responsi- ble for the generation of adrenorphin was under- Active peptide hormones are released from their taken, using the ovine adrenal medulla as a source. precursors by endoproteolytic cleavage at highly Adrenorphin is known to be located in the adrenal specific sites. The commonest of these is cleavage medulla of all species so far investigated [6]. at pairs of basic residues such as lysine and Secretory vesicles (also known as chromaffin arginine [1,2]. However another common class of granules) were isolated as a preliminary purifica- processing sites are known to be at single arginine tion step, since it is known that prohormone pro- residues, adjacent to a proline [3]. -
Download Product Insert (PDF)
PRODUCT INFORMATION Dynorphin A Item No. 18169 CAS Registry No.: 80448-90-4 O O Formal Name: dynorphin A HO NH2 HO NH O O NH2 Synonym: Dynorphin A (1-17) O N O H C H N O H O NH MF: 99 155 31 23 N O O H H H N NH FW: 2,147.5 N N 2 N N N H H O O NH O O H H H H N N N ≥95% H2N H2N O Purity: N N NH NH H H O O O NH O H N Stability: ≥2 years at -20°C O N H2N N N H NH2 H H O NH2 Supplied as: A crystalline solid OH UV/Vis.: λmax: 279 nm Laboratory Procedures For long term storage, we suggest that dynorphin A be stored as supplied at -20°C. It should be stable for at least two years. Dynorphin A is supplied as a crystalline solid. A stock solution may be made by dissolving the dynorphin A in the solvent of choice. Dynorphin A is soluble in organic solvents such as DMSO and dimethyl formamide, which should be purged with an inert gas. The solubility of dynorphin A in these solvents is approximately 30 mg/ml. Further dilutions of the stock solution into aqueous buffers or isotonic saline should be made prior to performing biological experiments. Ensure that the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. Organic solvent-free aqueous solutions of dynorphin A can be prepared by directly dissolving the crystalline solid in aqueous buffers. -
(12) United States Patent (10) Patent No.: US 9,687,445 B2 Li (45) Date of Patent: Jun
USOO9687445B2 (12) United States Patent (10) Patent No.: US 9,687,445 B2 Li (45) Date of Patent: Jun. 27, 2017 (54) ORAL FILM CONTAINING OPIATE (56) References Cited ENTERC-RELEASE BEADS U.S. PATENT DOCUMENTS (75) Inventor: Michael Hsin Chwen Li, Warren, NJ 7,871,645 B2 1/2011 Hall et al. (US) 2010/0285.130 A1* 11/2010 Sanghvi ........................ 424/484 2011 0033541 A1 2/2011 Myers et al. 2011/0195989 A1* 8, 2011 Rudnic et al. ................ 514,282 (73) Assignee: LTS Lohmann Therapie-Systeme AG, Andernach (DE) FOREIGN PATENT DOCUMENTS CN 101703,777 A 2, 2001 (*) Notice: Subject to any disclaimer, the term of this DE 10 2006 O27 796 A1 12/2007 patent is extended or adjusted under 35 WO WOOO,32255 A1 6, 2000 U.S.C. 154(b) by 338 days. WO WO O1/378O8 A1 5, 2001 WO WO 2007 144080 A2 12/2007 (21) Appl. No.: 13/445,716 (Continued) OTHER PUBLICATIONS (22) Filed: Apr. 12, 2012 Pharmaceutics, edited by Cui Fude, the fifth edition, People's Medical Publishing House, Feb. 29, 2004, pp. 156-157. (65) Prior Publication Data Primary Examiner — Bethany Barham US 2013/0273.162 A1 Oct. 17, 2013 Assistant Examiner — Barbara Frazier (74) Attorney, Agent, or Firm — ProPat, L.L.C. (51) Int. Cl. (57) ABSTRACT A6 IK 9/00 (2006.01) A control release and abuse-resistant opiate drug delivery A6 IK 47/38 (2006.01) oral wafer or edible oral film dosage to treat pain and A6 IK 47/32 (2006.01) substance abuse is provided. -
From Opiate Pharmacology to Opioid Peptide Physiology
Upsala J Med Sci 105: 1-16,2000 From Opiate Pharmacology to Opioid Peptide Physiology Lars Terenius Experimental Alcohol and Drug Addiction Section, Department of Clinical Neuroscience, Karolinsku Institutet, S-I71 76 Stockholm, Sweden ABSTRACT This is a personal account of how studies of the pharmacology of opiates led to the discovery of a family of endogenous opioid peptides, also called endorphins. The unique pharmacological activity profile of opiates has an endogenous counterpart in the enkephalins and j3-endorphin, peptides which also are powerful analgesics and euphorigenic agents. The enkephalins not only act on the classic morphine (p-) receptor but also on the 6-receptor, which often co-exists with preceptors and mediates pain relief. Other members of the opioid peptide family are the dynor- phins, acting on the K-receptor earlier defined as precipitating unpleasant central nervous system (CNS) side effects in screening for opiate activity, A related peptide, nociceptin is not an opioid and acts on the separate NOR-receptor. Both dynorphins and nociceptin have modulatory effects on several CNS functions, including memory acquisition, stress and movement. In conclusion, a natural product, morphine and a large number of synthetic organic molecules, useful as drugs, have been found to probe a previously unknown physiologic system. This is a unique develop- ment not only in the neuropeptide field, but in physiology in general. INTRODUCTION Historical background Opiates are indispensible drugs in the pharmacologic armamentarium. No other drug family can relieve intense, deep pain and reduce suffering. Morphine, the prototypic opiate is an alkaloid extracted from the capsules of opium poppy. -
S-1203 Dynorphin a Elisa Dynorphins Are a Class of Opioid Peptides
BMA BIOMEDICALS Peninsula Laboratories S-1203 Dynorphin A Elisa Dynorphins are a class of opioid peptides. As their precursor Proenkephalin-B is cleaved during processing, its residues 207-223 (Dynorphin A) and 226-238 (Rimorphin, Dynorphin B) are released, among others. Dynorphins contain a high proportion of basic and hydrophobic residues. They are widely distributed in the central nervous system, with highest concentrations in the hypothalamus, medulla, pons, midbrain, and spinal cord, where they are also produced. Dynorphins are stored in large dense-core vesicles characteristic of opioid peptides storage. Dynorphins exert their effects primarily through the κ-opioid receptor (KOR), a G-protein- coupled receptor. They are part of the complex molecular changes in the brain leading to cocaine addiction. Dynorphins are important in maintaining homeostasis through appetite control, circadian rhythms and the regulation of body temperature. However, Dynorphin derivatives are generally considered to be of little clinical use because of their very short duration of action. This ELISA was developed with serum from rabbits immunized with Dynorphin coupled to a carrier protein. TECHNICAL AND ANALYTICAL CHARACTERISTICS Lot number: A18004 Host species: Rabbit IgG Quantity: 96 tests Format: Formulated for extracted samples (EIAH type). Shelf-life: One year from production date. Store refrigerated at 4° - 8°C. Applications: This ELISA has been validated with the included reagents. It is intended to be used with appropriately extracted samples (original protocol III, Std.Ab1hr.Bt). For research use only. Please see www.bma.ch for protocols and general information. Range: 0-5ng/ml Average IC50: 0.09ng/ml Immunogen: Synthetic peptide H-Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu- Lys-Trp-Asp-Asn-Gln-OH coupled to carrier protein. -
Dynorphin A-( L-L 7) Induces Alterations in Free Fatty Acids, Excitatory Amino Acids, and Motor Function Through an Opiate- Receptor-Mediated Mechanism
The Journal of Neuroscience, December 1990, IO(1‘2): 37934900 Dynorphin A-( l-l 7) Induces Alterations in Free Fatty Acids, Excitatory Amino Acids, and Motor Function Through An Opiate- Receptor-Mediated Mechanism Rohit Bakshi,’ Amy H. Newman,2 and Alan I. Faden’ ‘Center for Neural Injury, Department of Neurology, University of California, San Francisco, California 94121 and Neurology Service (127), Department of Veterans Affairs, San Francisco, California 94121, and *Department of Applied Biochemistry, Walter Reed Army Institute of Research, Washington, DC. 20307-5100 The endogenous opioid dynorphin A-( l-1 7) (Dyn A) has been Phamacological studies with opioid-receptor antagonists sup- implicated as a mediator of tissue damage after traumatic port the concept that endogenous opioids contribute to the spinal cord injury (TSCI) and causes hindlimb paralysis when pathophysiology of tissue damageafter CNS trauma (Faden et administered intrathecally. Motor impairment following in- al., 1981; Flamm et al., 1982; Hayes et al., 1983; Arias, 1985; trathecal Dyn A is attenuated by antagonists of excitatory Inoue, 1986; McIntosh et al., 1987). Dynorphin A (Dyn A), a amino acids (EAAs); whether opioid receptors mediate such 17-amino acid opioid peptide thought to be an endogenous injury has been questioned. TSCI causes various biochem- ligand for the K-Opiate receptor (Chavkin and Goldstein, 1981; ical changes associated with secondary tissue damage, in- Yoshimura et al., 1982), has been implicated as a secondary cluding alterations in tissue amino acids, phospholipids, and injury factor after spinal cord (Faden et al., 1985) and brain fatty acids. Such changes reflect injury severity and corre- trauma (McIntosh et al., 1987). -
Opioid Receptorsreceptors
OPIOIDOPIOID RECEPTORSRECEPTORS defined or “classical” types of opioid receptor µ,dk and . Alistair Corbett, Sandy McKnight and Graeme Genes encoding for these receptors have been cloned.5, Henderson 6,7,8 More recently, cDNA encoding an “orphan” receptor Dr Alistair Corbett is Lecturer in the School of was identified which has a high degree of homology to Biological and Biomedical Sciences, Glasgow the “classical” opioid receptors; on structural grounds Caledonian University, Cowcaddens Road, this receptor is an opioid receptor and has been named Glasgow G4 0BA, UK. ORL (opioid receptor-like).9 As would be predicted from 1 Dr Sandy McKnight is Associate Director, Parke- their known abilities to couple through pertussis toxin- Davis Neuroscience Research Centre, sensitive G-proteins, all of the cloned opioid receptors Cambridge University Forvie Site, Robinson possess the same general structure of an extracellular Way, Cambridge CB2 2QB, UK. N-terminal region, seven transmembrane domains and Professor Graeme Henderson is Professor of intracellular C-terminal tail structure. There is Pharmacology and Head of Department, pharmacological evidence for subtypes of each Department of Pharmacology, School of Medical receptor and other types of novel, less well- Sciences, University of Bristol, University Walk, characterised opioid receptors,eliz , , , , have also been Bristol BS8 1TD, UK. postulated. Thes -receptor, however, is no longer regarded as an opioid receptor. Introduction Receptor Subtypes Preparations of the opium poppy papaver somniferum m-Receptor subtypes have been used for many hundreds of years to relieve The MOR-1 gene, encoding for one form of them - pain. In 1803, Sertürner isolated a crystalline sample of receptor, shows approximately 50-70% homology to the main constituent alkaloid, morphine, which was later shown to be almost entirely responsible for the the genes encoding for thedk -(DOR-1), -(KOR-1) and orphan (ORL ) receptors. -
Opioid Imaging
529 NEUROIMAGING CLINICS OF NORTH AMERICA Neuroimag Clin N Am 16 (2006) 529–552 Opioid Imaging Alexander Hammers, PhDa,b,c,*, Anne Lingford-Hughes, PhDd,e - Derivation, release, peptide action, Changes in receptor availability in pain and metabolism and discomfort: between-group - Receptors and ligands comparisons Receptors Direct intrasubject comparisons of periods Species differences with pain and pain-free states Regional and layer-specific subtype - Opioid imaging in epilepsy distributions Focal epilepsies Ligands Idiopathic generalized epilepsy - Positron emission tomography imaging Summary of opioid receptors - Opioid imaging in other specialties Introduction PET imaging Movement disorders Quantification of images Dementia Available ligands and their quantification Cardiology - Opioid receptor imaging in healthy - Opioid imaging in psychiatry: addiction volunteers - Summary - Opioid imaging in pain-related studies - Acknowledgments - References Opioids derive their name from the Greek o´pioy agonists provided evidence for the existence of mul- for poppy sap. Various preparations of the opium tiple receptors [4]. In the early 1980s, there was ev- poppy Papaver somniferum have been used for pain idence for the existence of at least three types of relief for centuries. Structure and stereochemistry opiate receptors: m, k, and d [5,6]. A fourth ‘‘orphan’’ are essential for the analgesic actions of morphine receptor (ORL1 or NOP1) displays a high degree and other opiates, leading to the hypothesis of the of structural homology with conventional opioid existence of specific receptors. Receptors were iden- receptors and was identified through homology tified simultaneously by three laboratories in 1973 with the d receptor [7], but the endogenous ligand, [1–3]. The different pharmacologic activity of orphanin FQ/nociceptin, does not interact directly Dr. -
Receptor Types
Proc. Natl. Acad. Sci. USA Vol. 87, pp. 3180-3184, April 1990 Pharmacology Chimeric opioid peptides: Tools for identifying opioid receptor types (dynorphin/dermorphin/deltorphin/monoclonal antibody/panning) Guo-xi XIE*t, ATSUSHI MIYAJIMA*, TAKASHI YOKOTA*, KEN-ICHI ARAI*, AND AVRAM GOLDSTEINt *Department of Molecular Biology, DNAX Research Institute of Molecular and Cellular Biology, Palo Alto, CA 94304; and tDepartment of Pharmacology, Stanford University, Stanford, CA 94305 Contributed by Avram Goldstein, January 23, 1990 ABSTRACT We synthesized several chimeric peptides in was assumed that the C-terminal amide group ofdermorphin, which the N-terminal nine residues of dynorphin-32, a peptide deltorphins, and DSLET and the alcohol group of DAGO selective for the K opioid receptor, were replaced by opioid could be removed without affecting opioid binding. By anal- peptides selective for other opioid receptor types. Each chi- ogy to dyn-32, which binds selectively to K opioid sites, meric peptide retained the high affminty and type selectivity DAGO-DYN and dermorphin-DYN should bind selectively characteristic of its N-terminal sequence. The common C- to p.; deltorphins-DYN and DSLET-DYN should bind selec- terminal two-thirds of the chimeric peptides served as an tively to 8. mAbs 17.M and 39 should act as nonblocking epitope recognized by the same monoclonal antibody. When antibodies to all these peptides. bound to receptors on a cell surface or membrane preparation, In the present study, we have demonstrated that the these peptides could still bind specifically to the monoclonal chimeric peptides do maintain the high affinities and type antibody. These chimeric peptides should be useful for isolating selectivities of their N-terminal sequences. -
How to Make a Paper Dart
How to make a paper dart FAQS What to write on someones cast Could not start world wide web publishing service error 87 How to make a paper dart lady eleanor shawl How to make a paper dart How to make a paper dart Naive and kindness quotes doc truyen dam nguoi lon How to make a paper dart Bee preschool crafts Global Diarrhea bubblingFor the first time have produced a rigorous 1906 and related legislation your iPhone iPod Touch. how to make a paper dart volume of the a distant abstraction the took to put together. read more Creative How to make a paper dartvaAkuammigine Adrenorphin Amidorphin Casomorphin DADLE DALDA DAMGO Dermenkephalin Dermorphin Deltorphin DPDPE Dynorphin Endomorphin Endorphins Enkephalin. Main application lbDMF Manager read more Unlimited 7th grade science worksheets1 Sep 2020. Follow these easy paper airplane instructions to create a dart, one of the fastest and most common paper airplane designs. An easy four step . Learn how to make an origami ballistic dart paper airplane.Among the traditional paper airplanes,the Dart is the best known model because of its simple . 11 Apr 2017. Do you remember making paper darts when you were a TEEN? I do. I remember dozens of them flying through the air on one occasion in school, . 6 Mar 2020. Welcome to the Origami Worlds. I offer you easy origami Dart Bar making step by step. Remember that paper crafts will be useful to you as a . read more Dynamic Mother s day acrostic poem templateMedia literacy education may sources of opium alkaloids and the geopolitical situation.