The practice of medicinal chemistry /
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| Další autoři: | , , , |
|---|---|
| Typ dokumentu: | Kniha |
| Jazyk: | Angličtina |
| Vydáno: |
Amsterdam :
Elsevier,
[2015]
|
| Vydání: | Fourth edition |
| Témata: | |
| On-line přístup: | Elektronická verze přístupná pouze pro studenty a pracovníky MU |
| Příbuzné jednotky: | Tištěná verze::
Practice of medicinal chemistry. |
Obsah:
- Front Cover; The Practice of Medicinal Chemistry; Copyright Page; Contents; List of Contributors; Foreword; Preface to the Fourth Edition; Preface to the Third Edition; Preface to the Second Edition; Preface to the First Edition; I. General Aspects of Medicinal Chemistry; 1 Medicinal Chemistry: Definitions and Objectives, Drug Activity Phases, Drug Classification Systems; I. Definitions and Objectives; A Medicinal Chemistry and Related Disciplines and Terms; B Drugs and Drug Substances; C Stages of Drug Development; II. Drug Activity Phases; A The Pharmaceutical Phase.
- B The Pharmacokinetic PhaseC The Pharmacodynamic Phase; D The Road to Successful Drug Development?; III. Drug Classification Systems; A Classification by Target and Mechanism of Action; 1 Targets; 2 Mechanisms of Action; B Other Classification Systems; References; 2 Evaluation of the Biological Activity of Compounds: Techniques and Mechanism of Action Studies; I. Introduction; II. Drug Discovery Approaches and Screening Cascades; A Target Based Screening; B Phenotypic Screening; III. In Vitro Assays; A Primary Assays; Glossary; 1 Binding assays; 2 Binding Studies: Principles and Analysis.
- 3 Enzyme Assays4 Types of Enzyme Inhibition and Their Analysis; A Reversible Inhibitors; B Irreversible Inhibitors; C Competitive Inhibitors; D Noncompetitive Inhibitors; E Uncompetitive Inhibitors; 5 Functional Assays; 6 Functional Studies and Their Analysis; A Agonist Concentration-Effect (E/[A]) Curves; B Full Agonists, Partial Agonists, and Inverse Agonists; C Optimizing Agonists; D Analysis of Antagonists; Competitive Antagonists; Irreversible, Noncompetitive, and Allosteric Antagonists; B Compound Interference in Primary Assays: Artifacts and False Positives; C Assay Biostatistics.
- D Selectivity, Cytotoxicity, and Species Cross-over. 1 Selectivity; 2 Cytotoxicity; 3 Species Crossover; E Cellular and Tissue Functional Responses; IV. Ex Vivo Assays; V. In Vivo Assays; A Pharmacokinetic Models; B Efficacy Models; C Safety Testing; Acknowledgements; References; 3 Drug Targets, Target Identification, Validation, and Screening; I. Introduction; II. What is a Drug Target?; III. The Purpose of Target Identification; A Target-Based Screening; B Phenotypic Screening; C Fast Follower Strategy; IV. Target Options and Treatment Options; V. Target Deconvolution and Target Discovery.
- VI. Methods for Target Identification and ValidationA Affinity Chromatography; B Genetic Methods; C Haploinsufficiency Profiling in Yeast; D Analysis of Resistant Mutants; E siRNA for Target Validation; F Yeast Three-Hybrid System; G DNA Microarrays; H Comparative Profiling; I Analysis of the Pathophysiology; J The Study of Existing Drugs; K Systems Biology; L In Silico Simulation of the Human Patient; VII. Target Validation; VIII. Conclusion; References; II. Lead Compound Discovery Strategies; 4 Strategies in the Search for New Lead Compounds or Original Working Hypotheses; I. Introduction.