Author: Ruomeng WangPublisher:
ISBN:
Category :
Languages : en
Pages : 223
Book Description
Design, Synthesis and Evaluation of Novel Isozyme-selective Carbonic Anhydrase Inhibitors
Author: Ruomeng WangCarbonic Anhydrase
Author: Claudiu T. SupuranPublisher: CRC Press
ISBN: 1134400152
Category : Medical
Languages : en
Pages : 560
Book Description
Carbonic Anhydrase: Its Inhibitors and Activators provides a state-of-the-art overview of the latest developments and challenges in carbonic anhydrase research. Authors describe the mechanisms of action of specific inhibitors in relation to physiological function, and present previously unpublished research on CA activators. Written by a team of in
Carbonic Anhydrases and Metabolism
Author: Claudiu T. SupuranPublisher: MDPI
ISBN: 3038978000
Category : Science
Languages : en
Pages : 184
Book Description
Carbonic anhydrases (CAs; EC 4.2.1.1) are metalloenzymes present in all kingdoms of life, as they equilibrate the reaction between three simple but essential chemical species: CO2, bicarbonate, and protons. Discovered more than 80 years ago, in 1933, these enzymes have been extensively investigated due to the biomedical application of their inhibitors, but also because they are an extraordinary example of convergent evolution, with seven genetically distinct CA families that evolved independently in Bacteria, Archaea, and Eukarya. CAs are also among the most efficient enzymes known in nature, due to the fact that the uncatalyzed hydration of CO2 is a very slow process and the physiological demands for its conversion to ionic, soluble species is very high. Inhibition of the CAs has pharmacological applications in many fields, such as antiglaucoma, anticonvulsant, antiobesity, and anticancer agents/diagnostic tools, but is also emerging for designing anti-infectives, i.e., antifungal, antibacterial, and antiprotozoan agents with a novel mechanism of action. Mitochondrial CAs are implicated in de novo lipogenesis, and thus selective inhibitors of such enzymes may be useful for the development of new antiobesity drugs. As tumor metabolism is diverse compared to that of normal cells, ultimately, relevant contributions on the role of the tumor-associated isoforms CA IX and XII in these phenomena have been published and the two isoforms have been validated as novel antitumor/antimetastatic drug targets, with antibodies and small-molecule inhibitors in various stages of clinical development. CAs also play a crucial role in other metabolic processes connected with urea biosynthesis, gluconeogenesis, and so on, since many carboxylation reactions catalyzed by acetyl-coenzyme A carboxylase or pyruvate carboxylase use bicarbonate, not CO2, as a substrate. In organisms other than mammals, e.g., plants, algae, and cyanobacteria, CAs are involved in photosynthesis, whereas in many parasites (fungi, protozoa), they are involved in the de novo synthesis of important metabolites (lipids, nucleic acids, etc.). The metabolic effects related to interference with CA activity, however, have been scarcely investigated. The present Special Issue of Metabolites aims to fill this gap by presenting the latest developments in the field of CAs and their role in metabolism.
Carbonic Anhydrase: Mechanism, Regulation, Links to Disease, and Industrial Applications
Author: Susan C. FrostPublisher: Springer Science & Business Media
ISBN: 9400773595
Category : Medical
Languages : en
Pages : 429
Book Description
The study of carbonic anhydrase has spanned multiple generations of scientists. Carbonic anhydrase was first discovered in 1932 by Meldrum and Roughton. Inhibition by sulfanilamide was shown in 1940 by Mann and Keilin. Even Hans Krebs contributed to early studies with a paper in 1948 showing the relationship of 25 different sulfonamides to CA inhibition. It was he who pointed out the importance of both the charged and uncharged character of these compounds for physiological experiments. The field of study that focuses on carbonic anhydrase (CA) has exploded in recent years with the identification of new families and isoforms. The CAs are metalloenzymes which are comprised of 5 structurally different families: the alpha, beta, gamma, and delta, and epsilon classes. The alpha class is found primarily in animals with several isoforms associated with human disease. The beta CAs are expressed primarily in plants and are the most divergent. The gamma CAs are the most ancient. These are structurally related to the beta CAs, but have a mechanism more similar to the alpha CAs. The delta CAs are found in marine algae and diflagellates. The epsilon class is found in prokaryotes in which it is part of the carboxysome shell perhaps supplying RuBisCO with CO2 for carbon fixation. With the excitement surrounding the discovery of disease-related CAs, scientists have redoubled their efforts to better understand structure-function relationships, to design high affinity, isotype-specific inhibitors, and to delineate signaling systems that play regulatory roles over expression and activity. We have designed the book to cover basic information of mechanism, structure, and function of the CA families. The authors included in this book bring to light the newest data with regard to the role of CA in physiology and pathology, across phylums, and in unique environmental niches.
Instant Lessons in Music
Author: Michael RedmanPublisher:
ISBN: 9781865096513
Category : Music
Languages : en
Pages : 48
Book Description
Photocopiable pre-prepared lessons in music covering practical work and theory and includes games, research, revision and testing activities suitable for junior high school classes.
Iminosugars
Author: Philippe CompainPublisher: John Wiley & Sons
ISBN: 9780470517444
Category : Medical
Languages : en
Pages : 482
Book Description
Iminosugars form undoubtedly the most attractive of carbohydrate mimics reported so far. In these structures, the substitution of the endocyclic oxygen of sugars by a basic nitrogen atom leads to remarkable biological properties and raises many challenges in organic synthesis. Since the discovery of their biological activity as glycosidase inhibitors in the 1970’s, these polyvalent molecules have progressively made their way from the laboratory to the clinic. The impressive series of discoveries in the field over the past ten years indicates clearly that it is “a boom time” for iminosugar chemistry and biology. The scope of their profile as inhibitors has been extended to a number of enzymes such as phosphorylases, glycosyltransferases or metalloproteinases, and iminosugars now constitute lead compounds for the development of new therapeutic agents for a wide range of diseases including diabetes, viral infections, lysosomal storage disorders and tumor metastasis. Latest developments, from iminosugar synthesis to their use in clinical studies, are presented in this book, which contains contributions from over fifteen of the major chemists, biochemists and drug developers in this rapidly expanding field. An extensive table correlating the structures of more than 600 iminosugars of therapeutic interest with their biological activities is also included in the book and should prove particularly useful to aid with the design and the discovery of novel bioactive substances. Iminosugars: From Synthesis to Therapeutic Application provides a unique resource for academic and industrial researchers working in the field of iminosugars and glycomimetics of biological and/or therapeutic interest: organic chemists, medicinal chemists, carbohydrate chemists and medical scientists.
Carbonic Anhydrase as Drug Target
Author: Daumantas MatulisPublisher: Springer
ISBN: 303012780X
Category : Science
Languages : en
Pages : 358
Book Description
This book offers deep insights into the thermodynamics and molecular structures of the twelve catalytically active isoforms of human carbonic anhydrase (CA) with a particular focus on inhibitor binding for drug design. X-ray crystallographic structures in combination with enzyme kinetic testing provide information on the interaction of CAs and their inhibitors, knowledge which is crucial for rational drug design. CAs are zinc carrying enzymes that catalyse the reversible interconversion of carbon dioxide and bicarbonate and are involved in numerous cellular processes. They are therefore a common target for drugs. The suppression of CA activities through inhibitory compounds has found application for example in diuretics and in glaucoma therapy. In this book methods used to determine binding thermodynamics of inhibitory compounds (Isothermal titration calorimetry, Fluorescent thermal shift assay/differential scanning fluorimetry and others) will be compared in detail. Also types and chemical synthesis of CA inhibitors, the use of antibodies against CAs as well as inhibitor application in animals are discussed.
Carbonic Anhydrases as Biocatalysts
Author: Claudiu T. SupuranPublisher: Elsevier
ISBN: 0444632638
Category : Technology & Engineering
Languages : en
Pages : 398
Book Description
Carbonic anhydrases (CAs, EC 4.2.1.1) are ubiquitous metalloenzymes, present throughout most living organisms and encoded by five evolutionarily unrelated gene families. The Carbonic Anhydrases as Biocatalysts: From Theory to Medical and Industrial Applications presents information on the growing interest in the study of this enzyme family and their applications to both medicine and biotechnology. - Offers comprehensive coverage of the carbonic anhydrases enzyme family and their properties as biocatalysts - Includes current applications of carbonic anhydrases in biotechnology on the basis of their catalytic efficiency, including new technologies for CO2 capture processes - Identifies new targets for drug design studies - Provides a selectivity profile for the different carbonic anhydrases and their related biomedical applications
More Synthetic Approaches to Nonaromatic Nitrogen Heterocycles, 2 Volume Set
Author: Ana Maria Faisca PhillipsPublisher: John Wiley & Sons
ISBN: 1119757142
Category : Science
Languages : en
Pages : 759
Book Description
More Synthetic Approaches to Nonaromatic Nitrogen Heterocycles An authoritative collection of resources discussing the latest trends in the synthesis of nonaromatic nitrogen heterocycles Widely distributed in nature, nitrogen heterocycles are extremely common in synthetic substances found in pharmaceuticals, agrochemicals, and materials. The literature is evolving rapidly and explores newly emerging structures and medicines. More Synthetic Approaches to Nonaromatic Nitrogen Heterocycles offers R&D professionals the opportunity to easily access a collection of the latest relevant research in the area. In the second two-volume set of this practical reference distinguished researcher Dr. Ana Maria M. M. Faisca Phillips delivers a collection of resources focusing on the newest and most widely applicable trends emerging in synthetic strategies for nonaromatic nitrogen heterocycles. With coverage of topics including organocatalysis, cascade reactions, flow chemistry in synthesis, cycloaddition reactions, metathesis, cross-coupling reactions, and electrochemistry, the book provides quick access to critical new avenues of synthesis. More Synthetic Approaches to Nonaromatic Nitrogen Heterocycles: Volume 1 and 2 also offers readers: A thorough introduction to recent advances in the design and synthesis of cyclic peptidomimetics Comprehensive explorations of fused heterocycles and transition metal promoted synthesis of isoindoline derivatives Practical discussions of 1,4-diazepane ring-based systems and recent advances in the synthesis of azepane-based compounds In-depth examinations of strained aziridinium ions, asymmetric organocatalysis in alternative media, and the electrochemical synthesis of non-aromatic N-heterocycles Perfect for academic and industrial researchers in organic chemistry and synthesis, organometallic chemistry, pharmaceutical chemistry catalysis, and sustainable chemistry, More Synthetic Approaches to Nonaromatic Nitrogen Heterocycles: Volume 1 and 2 is an indispensable reference for anyone seeking an authoritative source of information on new and emerging trends in synthesis.
In-cell NMR Spectroscopy
Author: Yutaka ItoPublisher: Royal Society of Chemistry
ISBN: 1839160934
Category : Science
Languages : en
Pages : 322
Book Description
In-cell NMR spectroscopy is a relatively new field. Despite its short history, recent in-cell NMR-related publications in major journals indicate that this method is receiving significant general attention. This book provides the first informative work specifically focused on in-cell NMR. It details the historical background of in-cell NMR, host cells for in-cell NMR studies, methods for in-cell biological techniques and NMR spectroscopy, applications, and future perspectives. Researchers in biochemistry, biophysics, molecular biology, cell biology, structural biology as well as NMR analysts interested in biological applications will all find this book valuable reading.