Protein kinase inhibitors in research and medicine:
Saved in:
| Other Authors: | |
|---|---|
| Format: | Book |
| Language: | English |
| Published: |
Amsterdam
Elsevier
2014
|
| Edition: | First edition |
| Series: | Methods in enzymology
Volume 548 |
| Subjects: | |
| Online Access: | Inhaltsverzeichnis |
| Physical Description: | XII, 241 Seiten, 21 ungezählte Blätter Illustrationen |
| ISBN: | 9780123979186 |
Staff View
MARC
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Record in the Search Index
| _version_ | 1804152836053794816 |
|---|---|
| adam_text | CONTENTS
Contributors ix
Preface xi
1. Catalytic Mechanisms and Regulation of Protein Kinases 1
Zhihong Wang and Philip A. Cole
1. Introduction 1
2. Kinetic Mechanism 2
3. Chemical Mechanism of Kinase Phosphoryl Transfer 4
4. Applications of Mechanistic Studies in Understanding Kinase Function and
Regulation 9
5. Summary and Outlook 16
References 17
2. A Structural Atlas of Kinases Inhibited by Clinically
Approved Drugs 23
Qi Wang, Julie A. Zorn, and John Kuriyan
1. Introduction 24
2. Kinase Structure and Catalytic Mechanism 26
3. Staurosporine: A Promiscuous ATP-Competitive Inhibitor 31
4. BCR-Abl Inhibitors 33
5. Tofacitinib (Xeljanz™) Binds to a DFG-in Conformation of Janus Kinase 41
6. Inhibition of Receptor Tyrosine Kinases 42
7. Vemurafenib (Zelboraf™) Binds to A DFG-in Conformation in the SerCThr
Kinase RAF 53
8. Inhibitors That Occupy Pockets Other Than the ATP-Binding Site 55
9. Summary 58
Acknowledgments 58
References 59
3. Fragment-Based Approaches to the Discovery of Kinase
Inhibitors 69
Paul N. Mortenson, Valerio Berdini, and Marc O Reilly
1. Introduction 70
2. Fragment-Based Drug Discovery 72
3. Identifying Fragment Hits 78
v
VI
Contents
4. From Fragments to Leads 80
5. Alternative Inhibition Strategies 83
6. Summary 86
Acknowledgments 88
References 88
4. Targeting Protein Kinases with Selective and Semipromiscuous
Covalent Inhibitors 93
Rand M. Miller and Jack Taunton
1. Introduction 94
2. Design of Irreversible Cysteine-Targeted Kinase Inhibitors 95
3. Targeting Noncataiytic Cysteines with Reversible Covalent Inhibitors 104
4. Semipromiscuous Covalent Inhibitors as Chemoproteomic Probes 109
5. Conclusions and Future Directions 113
References 114
5. The Resistance Tetrad: Amino Acid Hotspots for Kinome-Wide Exploitation of Drug-Resistant
Protein Kinase Alleles 117
Fiona P. Bailey, Veselin I. Andreev, and Patrick A. Eyers
1. Introduction 118
2. Protein Kinases and Kinase Inhibitors 119
3. Protein Kinase Inhibitors 119
4. Screening Approaches to Decipher Protein Kinase-Inhibitor Specificity 122
5. Random and Directed Mutagenesis Approaches Reveal Common
Resistance Mechanisms 124
6. A General Procedure for Directed (Nonrandom) Mutagenesis of dsDNA
Plasmids 126
7. The Resistance Tetrad Position 0: The Gatekeeper Residue 127
8. SB203580: A Paradigm for Gatekeeper-Mediated Drug Resistance
from Test Tube to Mouse 129
9. Expanding the Resistance Tetrad: +2 (Flydrophobtc) and +6/+7
Specificity Surfaces in Kinases 130
10. The Resistance Tetrad is a Selectivity Filter Applicable for Kinome-Wide
Drug-Resistance Studies 131
11. Engineering and Analysis of Logically Desigred Drug-Resistance
Mutations 132
12. Analysis of inhibitor Resistance Toward V T and DR Mutants in Vitro 134
Contents
vii
13. Oncogenic Gatekeeper Mutations: Unanticipated Mechanisms of
Gatekeeper Resistance Merit Biochemical Scrutiny of DR Mutants 1 35
14. Evaluation of Catalytic Behavior and KM[ATP] Value for WT and DR
Kinase Mutants In Vitro 136
15. Intact Cell Systems for Analyzing Drug Resistance and Target Validation 137
16. Generation of Stable, isogenic Cell Lines Expressing Tetracycline-Inducible
Kinases i 37
17. Analysis of Kinase Drug Resistance Toward a Cytotoxic Inhibitor: Ceil Growth
Assay Based on Colony Formation 139
18. Conclusions 139
References 140
6. FLiK: A Direct-Binding Assay for the Identification and Kinetic Characterization of Stabilizers of Inactive Kinase
Conformations 147
Jeffrey R. Simard and Daniel Rauh
1. Introduction 148
2. Design and Preparation of Kinases for FLiK 152
3. Labeling of p38cx MAP Kinase with Acrylodan 55
4. Assay Characterization and Validation 156
5. H~H5 with FLiK 1 64
6. Summary 169
Acknowledgments 170
References 170
7. Discovery of Allosteric Bcr-Abl Inhibitors from Phenotypic
Screen to Clinical Candidate 173
Nathanael S. Gray and Doriano Fabbro
1. Development of ATP-Site-Directed Inhibitors of BCR -ABL for the Treatment
of CML 1 74
2. Discovery and Characterization of Non-ATP-Site-Directed BCR-ABL
Inhibitors 176
3. Characterization of the Binding of the Non-ATP-Site-Directed BCR ABL
inhibitor GNF-2 179
4. Therapeutic Potential of First-Generation myr-Pocket Binders 83
5. Combinations of Second-Generation A^P-Site Inhibitors with
Second-Generator mvr-Pocket Ligands 85
Ac k r ov 1 ed g m e r t s 8 5
References 85
Contents
viii
8. The Logic and Design of Analog-Sensitive Kinases and Their
Small Molecule Inhibitors 189
Michael S. Lopez, Joseph I. Kliegman, and Kevan M. Shokat
1. Introduction 190
2. Constructing AS Kinases 193
3. AS Kinase Inhibitors 197
4. AS Kinases in Cells 207
5. AS Kinases in Living Multicellular Organisms 209
6. Summary 210
References 211
Author Index 215
Subject Index 235
|
| any_adam_object | 1 |
| author2 | Shokat, Kevan M. |
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| ctrlnum | (OCoLC)900486177 (DE-599)BVBBV042274796 |
| discipline | Chemie / Pharmazie Biologie |
| edition | First edition |
| format | Book |
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| isbn | 9780123979186 |
| language | English |
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| spelling | Protein kinase inhibitors in research and medicine edited by Kevan M. Shokat First edition Amsterdam Elsevier 2014 XII, 241 Seiten, 21 ungezählte Blätter Illustrationen txt rdacontent n rdamedia nc rdacarrier Methods in enzymology Volume 548 Proteinkinasen (DE-588)4175996-5 gnd rswk-swf Kinasen (DE-588)4268693-3 gnd rswk-swf Enzyminhibitor (DE-588)4152479-2 gnd rswk-swf Inhibitor (DE-588)4027007-5 gnd rswk-swf (DE-588)4143413-4 Aufsatzsammlung gnd-content Proteinkinasen (DE-588)4175996-5 s Enzyminhibitor (DE-588)4152479-2 s DE-604 Kinasen (DE-588)4268693-3 s Inhibitor (DE-588)4027007-5 s 1\p DE-604 Shokat, Kevan M. edt Methods in enzymology Volume 548 (DE-604)BV000000938 548 Digitalisierung UB Regensburg - ADAM Catalogue Enrichment application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=027712290&sequence=000002&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis 1\p cgwrk 20201028 DE-101 https://d-nb.info/provenance/plan#cgwrk |
| spellingShingle | Protein kinase inhibitors in research and medicine Methods in enzymology Proteinkinasen (DE-588)4175996-5 gnd Kinasen (DE-588)4268693-3 gnd Enzyminhibitor (DE-588)4152479-2 gnd Inhibitor (DE-588)4027007-5 gnd |
| subject_GND | (DE-588)4175996-5 (DE-588)4268693-3 (DE-588)4152479-2 (DE-588)4027007-5 (DE-588)4143413-4 |
| title | Protein kinase inhibitors in research and medicine |
| title_auth | Protein kinase inhibitors in research and medicine |
| title_exact_search | Protein kinase inhibitors in research and medicine |
| title_full | Protein kinase inhibitors in research and medicine edited by Kevan M. Shokat |
| title_fullStr | Protein kinase inhibitors in research and medicine edited by Kevan M. Shokat |
| title_full_unstemmed | Protein kinase inhibitors in research and medicine edited by Kevan M. Shokat |
| title_short | Protein kinase inhibitors in research and medicine |
| title_sort | protein kinase inhibitors in research and medicine |
| topic | Proteinkinasen (DE-588)4175996-5 gnd Kinasen (DE-588)4268693-3 gnd Enzyminhibitor (DE-588)4152479-2 gnd Inhibitor (DE-588)4027007-5 gnd |
| topic_facet | Proteinkinasen Kinasen Enzyminhibitor Inhibitor Aufsatzsammlung |
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