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Protein Kinases as Drug Targets (Methods and Principles in Medicinal Chemistry, Band 49) - Bert Klebl, Gerhard Müller, Michael Hamacher, Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
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Bert Klebl, Gerhard Müller, Michael Hamacher, Raimund Mannhold, Hugo Kubinyi, Gerd Folkers:

Protein Kinases as Drug Targets (Methods and Principles in Medicinal Chemistry, Band 49) - gebunden oder broschiert

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Protein Kinases as Drug Targets (Methods and Principles in Medicinal Chemistry, Band 49) - Bert Klebl, Gerhard Müller, Michael Hamacher, Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
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Bert Klebl, Gerhard Müller, Michael Hamacher, Raimund Mannhold, Hugo Kubinyi, Gerd Folkers:
Protein Kinases as Drug Targets (Methods and Principles in Medicinal Chemistry, Band 49) - gebunden oder broschiert

ISBN: 3527317902

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Protein Kinases as Drug Targets (Methods and Principles in Medicinal Chemistry, Band 49) - Bert Klebl, Gerhard Müller, Michael Hamacher, Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
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Bert Klebl, Gerhard Müller, Michael Hamacher, Raimund Mannhold, Hugo Kubinyi, Gerd Folkers:
Protein Kinases as Drug Targets (Methods and Principles in Medicinal Chemistry, Band 49) - gebunden oder broschiert

ISBN: 3527317902

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Protein Kinases as Drug Targets (Methods and Principles in Medicinal Chemistry, Band 49) - Bert Klebl, Gerhard Müller, Michael Hamacher, Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
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Bert Klebl, Gerhard Müller, Michael Hamacher, Raimund Mannhold, Hugo Kubinyi, Gerd Folkers:
Protein Kinases as Drug Targets (Methods and Principles in Medicinal Chemistry, Band 49) - gebunden oder broschiert

ISBN: 3527317902

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Details zum Buch
Protein Kinases as Drug Targets (Methods and Principles in Medicinal Chemistry, Band 49)
Autor:
Titel:
ISBN-Nummer:

9783527317905


This timely guide to kinase inhibitor drug development is the first to cover the entire drug pipeline, from target identification to compound development and clinical application. Edited by the pioneers in the field, on the drug development side this ready reference discusses classical medicinal chemistry approaches as well as current chemical genomics strategies. On the clinical side, both current and future therapeutic application areas for kinase inhibitor drugs are addressed, with a strong focus on oncology drugs. Backed by recent clinical experience with first-generation drugs in the battle against various forms of cancer, this is crucial reading for medicinal, pharmaceutical and biochemists, molecular biologists, and oncologists, as well as those working in the pharmaceutical industry.

Detailangaben zum Buch - Protein Kinases as Drug Targets (Methods and Principles in Medicinal Chemistry, Band 49)


EAN (ISBN-13): 9783527317905
ISBN (ISBN-10): 3527317902
Gebundene Ausgabe
Erscheinungsjahr: 2011
Herausgeber: Wiley-VCH Verlag GmbH & Co. KGaA
373 Seiten
Gewicht: 0,892 kg
Sprache: eng/Englisch

Buch in der Datenbank seit 2007-02-04T01:42:38+01:00 (Vienna)
Detailseite zuletzt geändert am 2020-01-28T12:52:23+01:00 (Vienna)
ISBN/EAN: 9783527317905

ISBN - alternative Schreibweisen:
3-527-31790-2, 978-3-527-31790-5
Alternative Schreibweisen und verwandte Suchbegriffe:
Autor des Buches: hugo müller, gerd müller, michael müller, muller, hamacher, bert, gerhard müller, ham, kubinyi, gerd folkers
Titel des Buches: kina kina, target, tar

Daten vom Verlag:

Autor/in: Bert Klebl; Gerhard Müller; Michael Hamacher
Titel: Methods and Principles in Medicinal Chemistry; Protein Kinases as Drug Targets
Verlag: Wiley-VCH
374 Seiten
Erscheinungsjahr: 2011-02-09
Gewicht: 0,914 kg
Sprache: Englisch
142,00 € (DE)
Not available (reason unspecified)
170mm x 240mm x 24mm

BB; gebunden; Hardcover, Softcover / Chemie; Medizinische Chemie, Pharmazeutische Chemie; Verstehen; Medizin, Gesundheit; Drug Discovery & Development; Enzymes & Receptors; Cell & Molecular Biology; Biochemie; Pharmazeutische Chemie; Clinical Pharmacology & Therapeutics; Pharmacology & Pharmaceutical Medicine; Chemistry; Klinische Pharmakologie u. Therapie; Biowissenschaften; Medizin; Proteinkinase; Chemie; Life Sciences; Wirkstoffforschung u. -entwicklung; Enzyme u. Rezeptoren; Medical Science; Zell- u. Molekularbiologie; Pharmakologie u. Pharmazeutische Medizin; Pharmakologie u. Pharmazeutische Medizin; Klinische Pharmakologie u. Therapie; Wirkstoffforschung u. -entwicklung; Enzyme u. Rezeptoren; Zell- u. Molekularbiologie

Preface PART I: Hit Finding and Profiling for Protein Kinases: Assay Development and Screening, Libraries IN VITRO CHARACTERIZATION OF SMALL-MOLECULE KINASE INHIBITORS Introduction Optimization of a Biochemical Kinase Assay Measuring the Binding Affinity and Residence Time of Unusual Kinase Inhibitors Addressing ADME Issues of Protein Kinase Inhibitors in Early Drug Discovery SCREENING FOR KINASE INHIBITORS: FROM BIOCHEMICAL TO CELLULAR ASSAYS Introduction Factors that Influence Cellular Efficacy of Kinase Inhibitors Assays for Measurement of Cellular Kinase Activity Outlook DISSECTING PHOSPHORYLATION NETWORKS: THE USE OF ANALOGUE-SENSITIVE KINASES AND MORE SPECIFIC KINASE INHIBITORS AS TOOLS Introduction Chemical Genetics The Application of ASKA Technology in Molecular Biology Conclusions and Outlook PART II: Medicinal Chemistry RATIONAL DRUG DESIGN OF KINASE INHIBITORS FOR SIGNAL TRANSDUCTION THERAPY The Concept of Rational Drug Design 3D Structure-Based Drug Design Ligand-Based Drug Design Target Selection and Validation Personalized Therapy with Kinase Inhibitors The NCLtm Technology and Extended Pharmacophore Modeling (Prediction-Oriented QSAR) Non-ATP Binding Site-Directed or Allosteric Kinase Inhibitors The Master Keys for Multiple Target Kinase Inhibitors Conclusions KINASE INHIBITORS IN SIGNAL TRANSDUCTION THERAPY VEGFR (Vascular Endothelial Growth Factor Receptor) Flt3 (FMS-Like Tyrosine Kinase 3) Bcr-Abl (Breakpoint Cluster Region-Abelson Murine Leukemia Viral Oncogene Homologue) EGFR (Epidermal Growth Factor Receptor) IGFR (Insulin-Like Growth Factor Receptor) FGFR (Fibroblas Growth Factor Receptor) PDGFR (Platelet-Derived Growth Factor Receptor ) c-Kit Met (Mesenchymal-Epithelial Transition Factor) Src p38 MAPKs (Mitogen-Activated Protein Kinases) ERK1/2 JNK (c-Jun N-Terminal Kinase, MAPK8) PKC (Protein Kinase C) CDKs (Cyclin-Dependent Kinases) Auroras Akt/PKB (Protein Kinase B) Phosphoinositide 3-Kinases Syk (Spleen Tyrosind Kinase) JAK (Janus Kinase) Kinase Inhibitors in Inflammation and Infectious Diseases DESIGN PRINCIPLES OF DEEP POCKET-TARGETING PROTEIN KINASE INHIBITORS Introduction Classification of Protein Kinase Inhibitors Type II Inhibitors Common Features of Type II Inhibitors Design Strategies for Type II Inhibitors Comparative Analysis of the Different Design Strategies Conclusions and Outlook FROM DISCOVERY TO CLINIC: AURORA KINASE INHIBITORS AS NOVEL TREATMENTS FOR CANCER Introduction Biological Roles of the Aurora Kinases Aurora Kinases and Cancer In Vitro Phenotype of Aurora Kinase Inhibitors Aurora Kinase Inhibitors X-Ray Crystal Structures of Aurora Kinases Summary PART III: Application of Kinase Inhibitors to Therapeutic Indication Areas DISCOVERY AND DESIGN OF PROTEIN KINASE INHIBITORS: TARGETING THE CELL CYCLE IN ONCOLOGY Protein Kinase Inhibitors in Anticancer Drug Development Structure-Guided Design of Small-Molecule Inhibitors of the Cyclin-Dependent Kinases Catalytic Site Inhibitors ATP Site Specificity Alternate Strategies for Inhibiting CDKs Cyclin Groove Inhibitors (CGI) Inhibition of CDK-Cyclin Association Recent Developments in the Discovery and the Development of Aurora Kinase Inhibitors Development of Aurora Kinase Inhibitors through Screening and Structure-Guided Design Aurora Kinase Inhibitors in Clinical Trials Progress in the Identification of Potent and Selective Polo-Like Kinase Inhibitors Development of Small-Molecule Inhibitors of PLK1 Kinase Activty Discovery of Benzthiazole PLK1 Inhibitors Recent Structural Studies of the PLK1 Kinase Domain Additional Small-Molecule PLK1 Inhibitors Reported The Polo-Box Domain Future Developments MEDICINAL CHEMISTRY APPROACHES FOR THE INHIBITION OF THE p38 MAPK PATHWAY Introduction p38 MAP Kinase Basics p38 Activity and Inhibition First-Generation Inhibitors Pyridinyl-Imidazole Inhibitor: SB203580 N-Substituted Imidazole Inhibitors N,N'-Diarylurea-Based Inhibitors: BIRB796 Structurally Diverse Clinical Candidates Medicinal Chemistry Approach on VX-745-Like Compounds Conclusion and Perspective for the Future CELLULAR PROTEIN KINASES AS ANTIVIRAL TARGETS Introduction Antiviral Activities of the Pharmacological Cyclin-Dependent Kinase Inhibitors Antiviral Activities of the Inhibiors of Other Cellular Protein Kinases Conclusion PROSPECTS FOR TB THERAPEUTICS TARGETING MYCOBACTERIUM TUBERCULOSIS PHOSPHOSIGNALING NETWORKS Introduction Rationale for Ser/Thr Protein Kinases and Protein Phosphatases as Drug Targets Drug Target Validation by Genetic Inactivation STPK Mechanisms, Substrates, and Functions M. tuberculosis STPK Inhibitors Conclusions and Prospects

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