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Natural Thiopeptides As a Privileged Scaffold for Drug Discovery and Therapeutic Development
– MEDICINAL Medicinal Chemistry Research (2019) 28:1063 1098 CHEMISTRY https://doi.org/10.1007/s00044-019-02361-1 RESEARCH REVIEW ARTICLE Natural thiopeptides as a privileged scaffold for drug discovery and therapeutic development 1 1 1 1 1 Xiaoqi Shen ● Muhammad Mustafa ● Yanyang Chen ● Yingying Cao ● Jiangtao Gao Received: 6 November 2018 / Accepted: 16 May 2019 / Published online: 29 May 2019 © Springer Science+Business Media, LLC, part of Springer Nature 2019 Abstract Since the start of the 21st century, antibiotic drug discovery and development from natural products has experienced a certain renaissance. Currently, basic scientific research in chemistry and biology of natural products has finally borne fruit for natural product-derived antibiotics drug discovery. A batch of new antibiotic scaffolds were approved for commercial use, including oxazolidinones (linezolid, 2000), lipopeptides (daptomycin, 2003), and mutilins (retapamulin, 2007). Here, we reviewed the thiazolyl peptides (thiopeptides), an ever-expanding family of antibiotics produced by Gram-positive bacteria that have attracted the interest of many research groups thanks to their novel chemical structures and outstanding biological profiles. All members of this family of natural products share their central azole substituted nitrogen-containing six-membered ring and are fi 1234567890();,: 1234567890();,: classi ed into different series. Most of the thiopeptides show nanomolar potencies for a variety of Gram-positive bacterial strains, including methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant enterococci (VRE), and penicillin-resistant Streptococcus pneumonia (PRSP). They also show other interesting properties such as antiplasmodial and anticancer activities. The chemistry and biology of thiopeptides has gathered the attention of many research groups, who have carried out many efforts towards the study of their structure, biological function, and biosynthetic origin. -
Brian O'neal Bachmann, Ph.D
Prepared: January 5, 2011 BRIAN O’NEAL BACHMANN, PH.D. Departments of Chemistry and Biochemistry Vanderbilt University Nashville, TN 37235-1822 Phone: (615) 322-8865; Fax: (615) 343-1234 E-mail: [email protected] http://www.vanderbilt.edu/AnS/Chemistry/BachmannGroup/ DEGREES EARNED 1995 – 2000 The Johns Hopkins University, Baltimore, Maryland. Ph.D. degree in Chemistry, December, 2000. Dissertation entitled: Identification and Characterization of β−Lactam Synthetase of Clavulanic Acid Biosynthesis. Advisor: Professor Craig. A. Townsend 1993 – 1994 Southern Methodist University, Dallas, Texas. M.S. degree in Chemistry, December 1994. Thesis entitled: Synthesis and Evaluation of Mechanism Based β−lactamase Inhibitors. Advisor: Professor John D. Buynak 1988 – 1992 Virginia Tech, Blacksburg, Virginia. B.S. degree in Chemistry, December 1992. Undergraduate Research Advisor: Tomas Hudlicky EMPLOYMENT HISTORY 2000 – 2001 Postdoctoral Fellow, The Johns Hopkins University Department of Chemistry, Baltimore, Maryland 2001 – 2002 Assistant Director of Chemistry, Ecopia Biosciences (now Thallion Pharmaceuticals), Montreal, Quebec, Canada 2002 – 2003 Director of Chemistry, Ecopia Biosciences (now Thallion Pharmaceuticals), Montreal, Quebec, Canada 2003 – current Assistant Professor of Chemistry, Vanderbilt University Department of Chemistry, Nashville, Tennessee 2000 – current Director, Board of Directors, Dymax Corporation, Torrington, Connecticut HONORS AND AWARDS • American Society of Chemists: Outstanding Graduate Student in Chemistry, -
Issn 0975-413X Coden (Usa): Pchhax
Available online a t www.derpharmachemica.com ISSN 0975-413X Der Pharma Chemica, 2016, 8(19):388-395 CODEN (USA): PCHHAX (http://derpharmachemica.com/archive.html) Design and Modification of Copper Oxide Electrodes for Improving Conversion Coefficient Indoors Lights (PV-Cell) Photocells Rahadian Zainul Department of Physical Chemistry, Universitas Negeri Padang, Padang, Indonesia _____________________________________________________________________________________________ ABSTRACT This research aims to investigate photocells reactor design can convert indoor lights energy into electrical energy. Indoor lights comes from sunlight entering into the room and fluorescent light irradiation. Design of photocells reactor use a panel of copper oxide (Cu 2O/CuO) of calcined Cu plate and filler electrolyte Na 2SO 4 0.5 N. Modification of electrode by n-p junction layer, which one of section (n) and the others section (p). Photocells reactor was constructed by thickness of the glass pane, the distance between the electrodes, the interface layer, layer and coating reflector panels. In this research there are three design of photocells reactor, The first design is R1, the thickness of the glass panel 3 mm thick reactor 15 mm without anti reflector. In this design, there are two type based on the difference at the junction of type n, (R 1a = plate Cu; R 1b = plate Aluminum) generate 182.82 2 2 mW/m and 21119644.3 NW/m . Than, the second design of photocells reactor is R2a (junction-type n = plate Cu) and R 2b (junction-type n = plate Al), a panel thickness of 15 mm and has a layer anti reflector provide power 214.95 2 2 mW/m and 24163298.3 NW/m . -
Cyanobacterial Peptide Toxins
CYANOBACTERIAL PEPTIDE TOXINS CYANOBACTERIAL PEPTIDE TOXINS 1. Exposure data 1.1 Introduction Cyanobacteria, also known as blue-green algae, are widely distributed in fresh, brackish and marine environments, in soil and on moist surfaces. They are an ancient group of prokaryotic organisms that are found all over the world in environments as diverse as Antarctic soils and volcanic hot springs, often where no other vegetation can exist (Knoll, 2008). Cyanobacteria are considered to be the organisms responsible for the early accumulation of oxygen in the earth’s atmosphere (Knoll, 2008). The name ‘blue- green’ algae derives from the fact that these organisms contain a specific pigment, phycocyanin, which gives many species a slightly blue-green appearance. Cyanobacterial metabolites can be lethally toxic to wildlife, domestic livestock and even humans. Cyanotoxins fall into three broad groups of chemical structure: cyclic peptides, alkaloids and lipopolysaccharides. Table 1.1 gives an overview of the specific toxic substances within these broad groups that are produced by different genera of cyanobacteria together, with their primary target organs in mammals. However, not all cyanobacterial blooms are toxic and neither are all strains within one species. Toxic and non-toxic strains show no predictable difference in appearance and, therefore, physicochemical, biochemical and biological methods are essential for the detection of cyanobacterial toxins. The most frequently reported cyanobacterial toxins are cyclic heptapeptide toxins known as microcystins which can be isolated from several species of the freshwater genera Microcystis , Planktothrix ( Oscillatoria ), Anabaena and Nostoc . More than 70 structural variants of microcystins are known. A structurally very similar class of cyanobacterial toxins is nodularins ( < 10 structural variants), which are cyclic pentapeptide hepatotoxins that are found in the brackish-water cyanobacterium Nodularia . -
4591-4603 Page 4591 Rohit J
Rohit J. Bhor*et al. /International Journal Of Pharmacy & Technology ISSN: 0975-766X CODEN: IJPTFI Available through Online Review Article www.ijptonline.com ESSENTIAL HYPERTENSION AND ITS TREATMENT BY ACE INHIBITORS A REVIEW ARTICLE Rohit J. Bhor1*, K.B.Kotade2. V.D. Wagh3 *1Department of Pharmaceutical Chemistry, PRES’s College of Pharmacy Chincholi, Tal-Sinner, Dist-Nasik, 422103, Maharashtra, India. 2Department of Pharmacology, PRES’s College of Pharmacy Chincholi, Tal-Sinner, Dist-Nasik, 422103, Maharashtra, India. 3Department of Pharmaceutics, PRES’s College of Pharmacy Chincholi, Tal-Sinner, Dist-Nasik, 422103, Maharashtra, India. Email: [email protected] Received on 17-07-2016 Accepted on 15-08-2016 Abstract: Hypertension (HTN) or hypertension, now and then called blood vessel hypertension, is a perpetual therapeutic condition in which the circulatory strain in the supply routes is hoisted. Hypertension is likewise a noteworthy danger variable for stroke, aneurysms of the conduits (e.g. aortic aneurysm), and fringe blood vessel sickness and is a reason for unending kidney illness. Systemic hypertension is a noteworthy danger variable for cardiovascular malady and is available in 69% of patients with a first myocardial dead tissue, in 77% of patients with a first stroke, in 74% of patients with incessant heart disappointment, and in 60% of patients with fringe blood vessel illness. Circulatory strain is abridged by two estimations, systolic and diastolic, which rely on upon whether the heart muscle is contracting (systole) or loose between pulsates (diastole). This equivalent the most extreme and least weight, individually. Typical circulatory strain very still is inside the scope of 100–140mmHg systolic and 60–90mmHg diastolic. -
First Evidence of Production of the Lantibiotic Nisin P Enriqueta Garcia-Gutierrez1,2, Paula M
www.nature.com/scientificreports OPEN First evidence of production of the lantibiotic nisin P Enriqueta Garcia-Gutierrez1,2, Paula M. O’Connor2,3, Gerhard Saalbach4, Calum J. Walsh2,3, James W. Hegarty2,3, Caitriona M. Guinane2,5, Melinda J. Mayer1, Arjan Narbad1* & Paul D. Cotter2,3 Nisin P is a natural nisin variant, the genetic determinants for which were previously identifed in the genomes of two Streptococcus species, albeit with no confrmed evidence of production. Here we describe Streptococcus agalactiae DPC7040, a human faecal isolate, which exhibits antimicrobial activity against a panel of gut and food isolates by virtue of producing nisin P. Nisin P was purifed, and its predicted structure was confrmed by nanoLC-MS/MS, with both the fully modifed peptide and a variant without rings B and E being identifed. Additionally, we compared its spectrum of inhibition and minimum inhibitory concentration (MIC) with that of nisin A and its antimicrobial efect in a faecal fermentation in comparison with nisin A and H. We found that its antimicrobial activity was less potent than nisin A and H, and we propose a link between this reduced activity and the peptide structure. Nisin is a small peptide with antimicrobial activity against a wide range of pathogenic bacteria. It was originally sourced from a Lactococcus lactis subsp. lactis isolated from a dairy product1 and is classifed as a class I bacteri- ocin, as it is ribosomally synthesised and post-translationally modifed2. Nisin has been studied extensively and has a wide range of applications in the food industry, biomedicine, veterinary and research felds3–6. -
Ph Metric Investigation on Speciation Studies of 5-Sulfosalicylic Acid Complexes of Co(II), Ni(II) and Cu(II) in DMF-Water Mixtures
Available online a t www.derpharmachemica.com ISSN 0975-413X Der Pharma Chemica, 2016, 8(8):150-157 CODEN (USA): PCHHAX (http://derpharmachemica.com/archive.html) pH Metric Investigation on Speciation Studies of 5-Sulfosalicylic acid complexes of Co(II), Ni(II) and Cu(II) in DMF-Water Mixtures M. Balakrishna 1,2 , G. Srinivasa Rao 2*, M. Ramanaiah 1, B. Ramaraju 3 and G. Nageswara Rao 4 1Department of Chemistry, Aditya Institute of Technology and Management, Tekkali, A.P India 2Department of Chemistry, GITAM Institute of Science, GITAM University, Visakhapatnam, A.P, India 3School of Material Science and Engineering, Nanyang Technological University, Singapore 4Department of Inorganic & Analytical Chemistry, Andhra University, Visakhapatnam, A.P India _____________________________________________________________________________________________ ABSTRACT Speciation of Co(II), Ni(II) and Cu(II) complexes with 5-Sulfosalicylic acid (5-SSA) in the presence of N, N’- Dimethyl formamide-water mixtures(0.0-60% v/v) at an ionic strength of 0.16 mol dm -3 and temperature 303 K were investigated pH metrically. The existence of different binary complex species was established from modeling studies using the computer program MINIQUAD75. The increased stability of the complexes with increasing DMF was explained by electrostatic forces. The influence of the DMF on the chemical speciation is discussed based on the dielectric constant of the medium. Distribution diagrams of various species of the complexes in relation to pH are presented. Keywords: 5-Sulfo salicylic acid; Speciation; DMF-Water; Binary complexes; Dielectric constant. _____________________________________________________________________________________________ INTRODUCTION The toxicity, bioavailability, bioaccumulation, biodegradability, persistence, mobility, solubility, extractability and many other critical properties depend on the form and nature of the chemical species [1-3]. -
COMPENDEX Database Summary Sheet
COMPENDEX (Ei Compendex) Subject • Civil and railroad engineering Coverage • Environmental and agricultural engineering • Geological and marine engineering • Mining and metallurgy • Chemical, petroleum, and fuel engineering • Bioengineering • Electrical engineering and electronics • Mechanical, automotive, and industrial engineering • Control devices and principles, instruments and measurement • Nuclear technology • Aerospace engineering • Heat and thermodynamics • Computers and data processing, communication engineering • Sounds and acoustical technology • Optics and optical devices File Type Bibliographic Features Thesaurus Controlled Term (/CT), Controlled Term in German (/CTDE) Alerts (SDIs) Weekly CAS Registry Page Images Number® Identifiers Keep & Share SLART Learning Database Structures Record Content • Bibliographic information, abstracts, and indexing • Cited references from journals, books, conference contributions, reports, and other non-conventional literature File Size More than 21.8 million records (09/20) Coverage 1970-present Updates Weekly Language English Database Elsevier (Engineering Information) Producer 360 Park Avenue South New York, NY 10010 USA Phone: 212-633-3895 Fax: 212-633-3680 Email: [email protected] Copyright Holder September 2020 2 COMPENDEX Database FIZ Karlsruhe Supplier STN Europe P.O. Box 2465 76012 Karlsruhe Germany Phone: +49-7247-808-555 Fax: +49-7247-808-259 Email: [email protected] Sources • Journals (over 5600) • Books • Reports • Conference contributions • Other non-conventional -
17Th Oct-2014 Revised: 15Th Nov-2014 Accepted: 16Th Nov-2014 Research Article
Volume-6, Issue-1, Jan-Mar-2015 Coden IJABFP-USA Copyrights@2015 Received: 17th Oct-2014 Revised: 15th Nov-2014 Accepted: 16th Nov-2014 Research article LIPID PEROXIDATION IN PREECLAMPSIA Dr. T.Sharmila Krishna*, Dr. D. Raja Rajeswari*, Dr. E. Venkat Rao**, Dr. Sk. Deepthi* and Dr.J.N.Naidu* *Department of Biochemistry, Narayana Medical College and General Hospital, Nellore-524003. ** Department of Community Medicine, Institute of Medical sciences and SUM Hospital, Bhubaneswar, Orissa. Corresponding author: Email address: [email protected] Phone number: 9908837280, 0861-2317963 extension 2596. ABSTRACT: Hypertension in pregnancy is a leading cause of both maternal and fetal mortality and morbidity. Preeclampsia is characterised by hypertension and proteinuria. Lipid peroxidation is an important factor in the pathophysiology of Preeclampsia. The present study was undertaken to determine Serum Malondialdehyde (MDA) levels , a product of lipid peroxidation , in clinically diagnosed Preeclamptic women(n=30) and the values were compared with that of Normotensive pregnant women (n=30) aged between 18-30yrs. All of them were in their third trimester and were primigravida. Serum MDA was estimated by TBARS (thiobarbituric acid reactive substances) method. We observed that Serum MDA levels were significantly increased in Preeclamptic women (p <0.000) as compared to that of Normotensive pregnant women . Increased levels of lipid peroxiation product - MDA may contribute to the pathophysiology of Preeclampsia. Key Words: MDA, Preeclampsia, Oxidative Stress INTRODUCTION Preeclampsia is a multisystem disorder characterised by hypertension to the extent of 140/90 mm of Hg or more , proteinuria ( ≥300mg/day) and edema induced by pregnancy after twentieth week (Pradnya Phalak et al, 2013). -
Enzyme Annotation for Orphan and Novel Reactions Using Knowledge of Substrate Reactive Sites
Enzyme annotation for orphan and novel reactions using knowledge of substrate reactive sites Noushin Hadadia,1, Homa MohammadiPeyhania,1, Ljubisa Miskovica, Marianne Seijoa,2, and Vassily Hatzimanikatisa,3 aLaboratory of Computational Systems Biology, Institute of Chemistry and Chemical Engineering, Ecole Polytechnique Fédérale de Lausanne, CH-1015 Lausanne, Switzerland Edited by Sang Yup Lee, Korea Advanced Institute of Science and Technology, Daejeon, South Korea, and approved March 6, 2019 (received for review November 5, 2018) Thousands of biochemical reactions with characterized activities metabolic engineering, synthetic biology applications, and the gap are “orphan,” meaning they cannot be assigned to a specific enzyme, filling of genome-scale models (19). A method for associating de leaving gaps in metabolic pathways. Novel reactions predicted by novo reactions to similarly occurring natural enzymatic reactions pathway-generation tools also lack associated sequences, limiting would allow for the direct experimental implementation of the protein engineering applications. Associating orphan and novel discovered novel reactions or assist in designing new proteins capable reactions with known biochemistry and suggesting enzymes to of catalyzing the proposed biotransformation. catalyze them is a daunting problem. We propose the method BridgIT Computational methods for identifying candidate genes of to identify candidate genes and catalyzing proteins for these re- orphan reactions have mostly been developed on the basis on actions. This method introduces information about the enzyme protein sequence similarity (3, 20–22). The two predominant binding pocket into reaction-similarity comparisons. BridgIT assesses classes of these sequence-based methods revolve around gene/ the similarity of two reactions, one orphan and one well-characterized genome analysis (22–25) and metabolic information (26, 27). -
JOURNAL of TRACE ELEMENTS in MEDICINE and BIOLOGY Journal of the Federation of European Societies on Trace Elements and Minerals - FESTEM
JOURNAL OF TRACE ELEMENTS IN MEDICINE AND BIOLOGY Journal of the Federation of European Societies on Trace Elements and Minerals - FESTEM AUTHOR INFORMATION PACK TABLE OF CONTENTS XXX . • Description p.1 • Audience p.1 • Impact Factor p.1 • Abstracting and Indexing p.2 • Editorial Board p.2 • Guide for Authors p.4 ISSN: 0946-672X DESCRIPTION . The journal provides the reader with a thorough description of theoretical and applied aspects of trace elements in medicine and biology and is devoted to the advancement of scientific knowledge about trace elements and trace element species. Trace elements play essential roles in the maintenance of physiological processes. During the last decades there has been an important progress in scientific investigation about the function and binding of trace elements. The Journal of Trace Elements in Medicine and Biology focuses on the description and dissemination of scientific results concerning the biological role and action of trace elements including different fields such as analytical methods, biochemistry, patho-biochemistry of metabolic processes, molecular biology, nutrition, toxicology, environmental toxicology, epidemiology, clinical applications in diagnosis, therapy, food chain and veterinary medicine. Progress in the knowledge of the biological role of trace elements depends, however, on advances in trace elements chemistry. The Journal of Trace Elements in Medicine and Biology publishes high quality, evidence-based research and includes only those studies that base their results on proven analytical methods and in which the quality assurance regarding the execution of experiments and achievement of results is guaranteed. AUDIENCE . Laboratory physicians, biochemists, pathobiochemists, clinical practising chemists, physiologists, toxicologists, veterinarians, epidemiologists, pharmacologists, ecologists, researchers in nutrition, environmental and industrial medicine. -
Web of Science (Wos) and Scopus: the Titans of Bibliographic Information in Today's Academic World
publications Review Web of Science (WoS) and Scopus: The Titans of Bibliographic Information in Today’s Academic World Raminta Pranckute˙ Scientific Information Department, Library, Vilnius Gediminas Technical University, Sauletekio˙ Ave. 14, LT-10223 Vilnius, Lithuania; [email protected] Abstract: Nowadays, the importance of bibliographic databases (DBs) has increased enormously, as they are the main providers of publication metadata and bibliometric indicators universally used both for research assessment practices and for performing daily tasks. Because the reliability of these tasks firstly depends on the data source, all users of the DBs should be able to choose the most suitable one. Web of Science (WoS) and Scopus are the two main bibliographic DBs. The comprehensive evaluation of the DBs’ coverage is practically impossible without extensive bibliometric analyses or literature reviews, but most DBs users do not have bibliometric competence and/or are not willing to invest additional time for such evaluations. Apart from that, the convenience of the DB’s interface, performance, provided impact indicators and additional tools may also influence the users’ choice. The main goal of this work is to provide all of the potential users with an all-inclusive description of the two main bibliographic DBs by gathering the findings that are presented in the most recent literature and information provided by the owners of the DBs at one place. This overview should aid all stakeholders employing publication and citation data in selecting the most suitable DB. Keywords: WoS; Scopus; bibliographic databases; comparison; content coverage; evaluation; citation impact indicators Citation: Pranckute,˙ R. Web of Science (WoS) and Scopus: The Titans 1.