Evaluation of enzyme inhibitors in drug discovery : a guide for medicinal chemists and pharmacologists / Robert A. Copeland.

Por: Copeland, Robert AllenTipo de material: TextoTextoSeries Methods of biochemical analysis ; v. 46Detalles de publicación: Hoboken, N.J. : Wiley-Interscience, 2005. Descripción: xvii, 271 p. : ill. ; 25 cmISBN: 0471686964 (cloth); 9780471686965 (cloth)Tema(s): Enzyme inhibitors -- Therapeutic use -- Testing | Drugs -- Design | Medicamentos | Enzimas -- Biotecnología | Química farmaceútica | Enzyme inhibitors -- Structure-activity relationships | Enzyminhibitoren | Enzyme Inhibitors -- therapeutic use | Drug Design | Enzyme Inhibitors -- chemistry | Antienzymes -- Emploi en thérapeutique -- Tests | Médicaments -- Conception | Antienzymes -- Relations structure-activitéClasificación CDD: 615/.19 Otra clasificación: 44.38
Contenidos:
Why enzymes as drug targets? -- Enzyme reaction mechanisms. -- Reversible modes of inhibitor interactions with enzymes. -- Assay considerations for compound library screening. -- Lead organization and structure-activity relationships for reversible inhibitors. -- Slow binding inhibitors. -- Tight binding inhibitors. -- Irreversible enzyme inactivators. -- Appendix 1. Kinetics if biochemical reactions. -- Appendix 2. Derivation of the enzyme-ligand binding isotherm equation. -- Appendix 3. Serial dilution schemes.
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Includes bibliographical references and index.

Why enzymes as drug targets? -- Enzyme reaction mechanisms. -- Reversible modes of inhibitor interactions with enzymes. -- Assay considerations for compound library screening. -- Lead organization and structure-activity relationships for reversible inhibitors. -- Slow binding inhibitors. -- Tight binding inhibitors. -- Irreversible enzyme inactivators. -- Appendix 1. Kinetics if biochemical reactions. -- Appendix 2. Derivation of the enzyme-ligand binding isotherm equation. -- Appendix 3. Serial dilution schemes.

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