Carbonic Anhydrase As Drug Target

Author : Daumantas Matulis
Publisher : Springer
ISBN 13 : 303012780X
Total Pages : 353 pages
Book Rating : 4.00/5 ( download)

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Download or read book Carbonic Anhydrase as Drug Target written by Daumantas Matulis and published by Springer. This book was released on 2019-05-21 with total page 353 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Author : W. Richard Chegwidden
Publisher : Springer Nature
ISBN 13 : 303079511X
Total Pages : 296 pages
Book Rating : 4.15/5 ( download)

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Download or read book The Carbonic Anhydrases: Current and Emerging Therapeutic Targets written by W. Richard Chegwidden and published by Springer Nature. This book was released on 2021-10-30 with total page 296 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume assembles and integrates the wealth of diverse information that is now accumulating in this burgeoning field. The existing and potential therapeutic applications of targeting CA cover a remarkably wide-range of diseases and disorders and have generated increasing and extensive interest in recent years. Its inter-disciplinary approach embraces both the most up-to-date therapeutic application of CA-targeting and the latest research data that will provide a platform for the development of novel applications. The interested audience comprises scientists and clinicians from many relevant disciplines within science and medicine.

Author : Susan C. Frost
Publisher : Springer Science & Business Media
ISBN 13 : 9400773595
Total Pages : 429 pages
Book Rating : 4.92/5 ( download)

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Download or read book Carbonic Anhydrase: Mechanism, Regulation, Links to Disease, and Industrial Applications written by Susan C. Frost and published by Springer Science & Business Media. This book was released on 2013-10-22 with total page 429 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Author : Yutaka Ito
Publisher : Royal Society of Chemistry
ISBN 13 : 1839160934
Total Pages : 322 pages
Book Rating : 4.36/5 ( download)

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Download or read book In-cell NMR Spectroscopy written by Yutaka Ito and published by Royal Society of Chemistry. This book was released on 2019-12-09 with total page 322 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Author : Claudiu T. Supuran
Publisher : MDPI
ISBN 13 : 3038978000
Total Pages : 184 pages
Book Rating : 4.08/5 ( download)

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Download or read book Carbonic Anhydrases and Metabolism written by Claudiu T. Supuran and published by MDPI. This book was released on 2019-04-08 with total page 184 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Author : Claudiu T. Supuran
Publisher : Academic Press
ISBN 13 : 0128167459
Total Pages : 560 pages
Book Rating : 4.58/5 ( download)

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Download or read book Carbonic Anhydrases written by Claudiu T. Supuran and published by Academic Press. This book was released on 2019-07-17 with total page 560 pages. Available in PDF, EPUB and Kindle. Book excerpt: Carbonic Anhydrases provides an interdisciplinary review of the burgeoning carbonic anhydrase (CA) research area, spanning from CAs classification (biochemical and structural features) to drug design and pharmacology of CA inhibitors and activators, finally touching on the biotechnological applications of these metalloenzymes. The book adopts a clear step-by-step approach and introduction to this intricate and highly interdisciplinary field. A diverse range of chapters from international experts speak to CA classification and distribution, the mechanisms of action and drug design of inhibitors and activators, the druggability of the various isoforms in the treatment of a multitude of diseases, and threats to human health. Carbonic Anhydrases provides biology, biochemistry, and medicinal chemistry students and researchers a thorough discussion and update on the evergreen and expanding research area of CAs. Offers a full overview of CAs’ biochemical and structural features, as well as drug design and pharmacology of inhibitors and activators Provides a thorough update on the newly identified isoforms, modulating chemotypes, and innovative biomedical applications Describes the current biotechnological applications of CAs, including processes for CO2 capture Features chapter contributions from international leaders in CA biology, medicinal chemistry, and pharmacology

Author : Claudiu T. Supuran
Publisher : John Wiley & Sons
ISBN 13 : 9780470508152
Total Pages : 1040 pages
Book Rating : 4.59/5 ( download)

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Download or read book Drug Design of Zinc-Enzyme Inhibitors written by Claudiu T. Supuran and published by John Wiley & Sons. This book was released on 2009-10-22 with total page 1040 pages. Available in PDF, EPUB and Kindle. Book excerpt: Brings together functional and structural informationrelevant to the design of drugs targeting zinc enzymes The second most abundant transition element in living organisms, zinc spans all areas of metabolism, with zinc-containing proteins offering both established and potential drug targets. Drug Design of Zinc-Enzyme Inhibitors brings together functional and structural information relevant to these zinc-containing targets. With up-to-date overviews of the latest developments field, this unique and comprehensive text enables readers to understand zinc enzymes and evaluate them in a drug design context. With contributions from the leaders of today's research, Drug Design of Zinc-Enzyme Inhibitors covers such key topics as: Major drug targets like carbonic anhydrases, matrix metalloproteinases, bacterial proteases, angiotensin-converting enzyme, histone deacetylase, and APOBEC3G Roles of recently discovered zinc-containing isozymes in cancer, obesity, epilepsy, pain management, malaria, and other conditions Cross reactivity of zinc-enzyme inhibitors and activators The extensive use of X-ray crystallography and QSAR studies for understanding zinc-containing proteins Clinical applications An essential resource for the discovery and development of new drug molecules, Drug Design of Zinc-Enzyme Inhibitors gives researchers, professionals, students, and academics the foundation to understand and work with zinc enzyme inhibitors and activators.

Author : Jean-Paul Renaud
Publisher : John Wiley & Sons
ISBN 13 : 1118900502
Total Pages : 1367 pages
Book Rating : 4.05/5 ( download)

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Download or read book Structural Biology in Drug Discovery written by Jean-Paul Renaud and published by John Wiley & Sons. This book was released on 2020-01-09 with total page 1367 pages. Available in PDF, EPUB and Kindle. Book excerpt: With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins

Author : Claudiu T. Supuran
Publisher : CRC Press
ISBN 13 : 1134400152
Total Pages : 588 pages
Book Rating : 4.57/5 ( download)

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Download or read book Carbonic Anhydrase written by Claudiu T. Supuran and published by CRC Press. This book was released on 2004-05-27 with total page 588 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

Author : Bernard Becker
Publisher :
ISBN 13 :
Total Pages : 532 pages
Book Rating : 4.79/5 ( download)

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Download or read book Becker-Shaffer's Diagnosis and Therapy of the Glaucomas written by Bernard Becker and published by . This book was released on 1970 with total page 532 pages. Available in PDF, EPUB and Kindle. Book excerpt: