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Progress in medicinal chemistry
Frank D. King, G. Lawton
Specialiserad
ISBN 0080462103
utgivning
Amsterdam; London : Elsevier Science, 20061 online resource (405 p.)
Seriemedlemskap
Progress in medicinal chemistry ; 44editors, F.D. King and G. Lawton
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Pharmaceutical chemistry., Chemistry.Annat bärarformat
Progress in medicinal chemistry · ISBN 0-444-51737-5 (Print:)Sammanfattning
The perceived lack of drug discovery productivity in recent times has led to much debate in the pharmaceutical/biotechnology industry as escalating R&D costs are not being matched by increased output. Few observers doubt that selecting the right targets, ie those which are critical to disease pathology and are 'druggable', is the best starting point for improved productivity.The seven chapters of this volume describe recent progress towards drugs acting at a range of 'druggable' targets. One chapter addresses kinases, one covers an ion channel, two proteases are featured and three of t
Innehållsförteckning
Front cover; Title page; Copyright; Front matter; Preface; Table of contents; List of Contributors; Body; 1 Finding Protein Kinase Hits using Structural Information; Introduction; Screening by X-ray Crystallography; Screening by NMR; Fundamentals of NMR Spectroscopy; Using Chemical Shift Changes; Nuclear-Spin Relaxation; Nuclear Overhauser Effects; Exchange Phenomena; Applications of NMR in Screening; Target-Based Screening; Ligand-Based Screening; Examples of NMR Methods for Discovering Kinase Inhibitors; The Shapes Strategy; NMR Screening by Waterlogsy Method, NMR Screening of Protein Kinases by ATP-STD MethodNMR Backbone Assignment of a Kinase; Designing Novel Kinase Inhibitors from the NMR-Based Screening of Fragments; Design of Libraries for use in NMR Screening; In Silico Methods; Receptor-Based Screening; Compound Database and Receptor Preparation; Protein-Ligand Docking; Scoring Functions; Development and Evaluation of Docking and Scoring; Virtual Screening and Protein Kinases; Faults and Fixes for Virtual Screening; Consensus Scoring; Knowledge-Based Screening; Protein Flexibility and Induced Fit, High Throughput Docking as a Virtual Screening ToolAlternatives to High Throughput Docking; Comparative Homology Modelling; De Novo Design; Summary; References; 2 Blunting the Swiss Army Knife of Hepatitis C Virus: Inhibitors of NS3/4A Protease; Hepatitis C Infection; Introduction; The Hepatitis C Virus; Current Therapies for the Treatment of HCV Infections; The HCV NS3/4A Protease; Tools to Study NS3/4A Protease Inhibitors; Enzymatic Assays; Viral Replication; Cell culture models; The replicon; Animal models; Resistance studies; Inhibitors of the NS3/4A Serine Protease, Non-Covalent Peptidic InhibitorsCarboxylic acid containing inhibitors; BILN 2061; Phenethyl amide containing inhibitors; Non-covalent aza-peptide inhibitors; C-terminal acyl sulfonamide containing inhibitors; Prime-side inhibitors; Covalent Reversible Peptidic Inhibitors; Non-Peptidic Inhibitors; Summary and Outlook; References; 3 Peptide Deformylase Inhibitors; Introduction; Peptide Deformylase as a Novel Antibacterial Target; Function; Essentiality; Spectrum; Selectivity; Protein Structure of Peptide Deformylases; Three-Dimensional Structure; Metal-Binding Site; Fe2+-PDF, Comparison with Other MetalloproteasesSubstrate-Binding Pockets; S1' pocket; S2' pocket; S3' pocket; Design and SAR of Peptide Deformylase Inhibitors; Early Substrate-Based Inhibitors; SAR from substrate specificity studies; Thiols; H-phosphonates; Aldehydes; Pseudopeptidic Hydroxamic Acids and N-Formyl-N-Hydroxylamines; Actinonin; P2' t-Butyl containing inhibitors; P2' Proline-derived inhibitors; ß-Aminohydroxamic acids; Non-Peptidic Templates; Thyropropic acid analogues; Biaryl acids; ß-Sulfonyl- and ß-sulfinylhydroxamic acids; Benzamides and aryl ethers; Bicyclic hydroxamic acids, Isoxazoles
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Medverkan och funktion
Frank D. King, G. Lawtonklassifikation
615.19; 615.19082 (DDK-klassifikation)målgrupp
SpecialiseradIdentifikator
ISBN 0080462103Indirekt identifierad av
ISBN 0444517375har titel
Progress in medicinal chemistryupphovsuppgift
editors, F.D. King and G. Lawtonutgivning
Amsterdam; London : Elsevier Science, 2006omfång
1 online resource (405 p.)anmärkning
- Description based upon print version of record.
- Includes references and index.
Illustrativt innehåll
Illustrationer finns men typen specificeras ejAnnat bärarformat
Progress in medicinal chemistry · ISBN 0-444-51737-5 (Print:)Seriemedlemskap
Progress in medicinal chemistry ; 44kontrollnummer
15409125Resursens ID / Permalänk: https://libris.kb.se/5phn56qh27xtx9d#it
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