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Carbonic Anhydrase as Drug Target

Thermodynamics and Structure of Inhibitor Binding

  • Book
  • © 2019

Overview

Editors:
  1. Daumantas Matulis

    1. Department of Biothermodynamics and Drug Design, Vilnius University, Life Sciences Center, Institute of Biotechnology, Vilnius, Lithuania

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  • Numerous X-ray crystallographic structures of human carbonic anhydrases and their complexes with inhibitors
  • Compares methods to determine inhibitor binding
  • Provides information on intrinsic thermodynamics of inhibitor binding to carbonic anhydrases

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Table of contents (22 chapters)

  1. Front Matter

    Pages i-xxvi
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  2. Carbonic Anhydrases—Preparation, Activity, Inhibition

    1. Front Matter

      Pages 1-1
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    2. Overview of Human Carbonic Anhydrases

      • Lina Baranauskienė, Daumantas Matulis
      Pages 3-14

    3. Recombinant Production of 12 Catalytically Active Human CA Isoforms

      • Aurelija Mickevičiūtė, Vaida Juozapaitienė, Vilma Michailovienė, Jelena Jachno, Jurgita Matulienė, Daumantas Matulis
      Pages 15-37

    4. Catalytic Activity and Inhibition of Human Carbonic Anhydrases

      • Lina Baranauskienė, Daumantas Matulis
      Pages 39-49

    5. Characterization of Carbonic Anhydrase Thermal Stability

      • Asta Zubrienė, Daumantas Matulis
      Pages 51-59

  3. Thermodynamics and Kinetics of Compound Binding to Carbonic Anhydrases

    1. Front Matter

      Pages 61-61
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    2. Inhibitor Binding to Carbonic Anhydrases by Fluorescent Thermal Shift Assay

      • Vytautas Petrauskas, Asta Zubrienė, Matthew J. Todd, Daumantas Matulis
      Pages 63-78

    3. Inhibitor Binding to Carbonic Anhydrases by Isothermal Titration Calorimetry

      • Vaida Paketurytė, Asta Zubrienė, Wen-Yih Chen, Sandro Keller, Margarida Bastos, Matthew J. Todd et al.
      Pages 79-95

    4. Change in Volume Upon Inhibitor Binding to Carbonic Anhydrases by Fluorescent Pressure Shift Assay

      • Gediminas Skvarnavičius, Daumantas Matulis, Vytautas Petrauskas
      Pages 97-106

    5. Observed Versus Intrinsic Thermodynamics of Inhibitor Binding to Carbonic Anhydrases

      • Asta Zubrienė, Daumantas Matulis
      Pages 107-123

    6. Kinetic Analysis of Carbonic Anhydrase–Sulfonamide Inhibitor Interactions

      • Vladimir O. Talibov, Vaida Linkuvienė, U. Helena Danielson, Daumantas Matulis
      Pages 125-140

  4. Structure–Thermodynamics/Kinetics Correlations of Compound Binding to Carbonic Anhydrases

    1. Front Matter

      Pages 141-141
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    2. Organic Synthesis of Substituted Chlorinated Benzenesulfonamides as Selective Inhibitors of Several CA Isoforms

      • Edita Čapkauskaitė, Daumantas Matulis
      Pages 143-152

    3. Organic Synthesis of Substituted Fluorinated Benzenesulfonamides as Selective Inhibitors of CA IX and Other Isoforms

      • Virginija Dudutienė, Daumantas Matulis
      Pages 153-161

    4. Carbonic Anhydrase Inhibitors with Dual Targeting

      • Peteris Trapencieris, Anete Parkova, Ineta Vendina-Birzniece
      Pages 163-178

    5. Structures of Human Carbonic Anhydrases and Their Complexes with Inhibitors

      • Alexey Smirnov, Elena Manakova, Saulius Gražulis, Robert McKenna, Daumantas Matulis
      Pages 179-202

    6. X-Ray Crystallographic Structures of High-Affinity and High-Selectivity Inhibitor Complexes with CA IX That Plays a Special Role in Cancer

      • Kaspars Tars, Daumantas Matulis
      Pages 203-213

    7. In Silico Modeling of Inhibitor Binding to Carbonic Anhydrases

      • Visvaldas Kairys, Kliment Olechnovič, Vytautas Raškevičius, Daumantas Matulis
      Pages 215-232

    8. Maps of Correlations Between Compound Chemical Structures and Thermodynamics of Binding to 12 Human Carbonic Anhydrases: Towards Isoform-Selective Inhibitors

      • Asta Zubrienė, Vaida Linkuvienė, Daumantas Matulis
      Pages 233-247
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Keywords

About this book

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 typesand chemical synthesis of CA inhibitors, the use of antibodies against CAs as well as inhibitor application in animals are discussed.  

Editors and Affiliations

  • Department of Biothermodynamics and Drug Design, Vilnius University, Life Sciences Center, Institute of Biotechnology, Vilnius, Lithuania

    Daumantas Matulis

About the editor

Prof. Dr. Daumantas Matulis

Vilnius University

Life Sciences Center

Institute of Biotechnology

Department of Biothermodynamics and Drug Design

Sauletekio 7, 10257 Vilnius

Lithuania

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