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Targeting Protein Kinases for Cancer Therapy

by: Matthews, David J.; Gerritsen, Mary E.

Targeting Protein Kinases for Cancer Therapy

by: Matthews, David J.; Gerritsen, Mary E.

ISBN 13:
9780470229651
ISBN 10:
0470229659
Edition: 1st
Format: Hardcover
Copyright: 02/15/2010
Publisher: Wiley

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Summary

This book provides an overview of different protein kinases structure, function, regulation, and their role in cancer. It combines kinase biology with chemistry and pharmacology applications for discovery and development of cancer drugs. The text also describes existing and emerging kinase inhibitors, focusing mostly on small molecules but also alternative approaches like therapeutic antibodies. Provides an important resource that helps pharmaceutical researchers understand and work in this dynamic area of cancer drug research.

Preface	p. xi
Acknowledgments	p. xiii
Kinases and Cancer	p. 1
A Brief History of Protein Phosphorylation	p. 1
Kinases and Cancer	p. 3
A Tour of the Human Protein Kinase Superfamily	p. 8
Tyrosine Kinase Group	p. 12
TKL (Tyrosine Kinase-like) Group	p. 22
STE Group	p. 25
CSNK1 Group	p. 27
AGC Group	p. 28
CAMK Group	p. 30
CMGC Group	p. 32
RGC Group	p. 36
Others	p. 36
Atypical Protein Kinases	p. 41
Nonprotein Kinases	p. 41
Strategic Considerations for Selecting Kinases as Drug Targets	p. 46
Comparison of Kinase Inhibitor Therapeutic Strategies	p. 51
Small Molecule Versus Antibody-Directed Therapies	p. 51
Alternative Strategies for Kinase Inhibition	p. 51
References	p. 58
Protein Kinase Structure, Function and Regulation	p. 75
Ligand Binding to Receptor Tyrosine Kinases	p. 76
EGF: EGF Receptor Interactions	p. 76
Insulin: Insulin Receptor and IGF1:IGF1R	p. 78
FGF: FGF Receptor (Heparin/Heparan Sulfate) Interactions	p. 79
VEGF: VEGF Receptor Interactions	p. 80
Angiopoietin2: TIE2 Receptor Interactions	p. 80
Ephrin: EPH Receptor Interactions	p. 82
The Role of Transmembrane Domains	p. 82
Protein Kinase Domain Structure and Function	p. 83
Catalytic Activity of Protein Kinases	p. 87
Steady State Kinetics	p. 87
Chemistry of Protein Kinase Catalysis	p. 89
Protein Kinase Regulation	p. 91
Regulation Via Activation Segment Phosphorylation	p. 92
Regulation by N-Terminal Sequences and Domains	p. 96
C-Terminal Regulatory Regions	p. 98
Regulation by Other Domains and Partner Proteins	p. 102
References	p. 107
Receptor Tyrosine Kinases	p. 119
EGF/ERBB Receptors	p. 120
ERBB Receptors and Cancer	p. 128
Insulin/IGF Receptors	p. 130
Insulin/IGF Receptors and Cancer	p. 134
Anaplastic Lymphoma Kinase	p. 136
ALK and Cancer	p. 137
VEGF Receptors (VEGFR1, VEGFR2, VEGFR3)	p. 140
PDGF Receptors	p. 146
PDGFRs and Cancer	p. 149
FGF Receptors	p. 153
FGFRs and Cancer	p. 156
KIT	p. 158
KIT and Cancer	p. 160
FLT	p. 3165
FLT3 and Cancer	p. 167
RET	p. 168
RET and Thyroid Carcinoma	p. 169
MET and RON	p. 170
MET	p. 170
RON	p. 175
References	p. 177
Nonreceptor Tyrosine Kinases	p. 215
ABL	p. 216
ARG	p. 223
SRC and SRC Family Kinases	p. 224
SRC	p. 228
Cellular Roles of SRC	p. 232
SRC and Cancer	p. 234
FAK	p. 235
FAK and Cancer	p. 238
JAK	p. 238
Activation and Known Mutations and Fusions of the JAK Family of Tyrosine Kinases	p. 241
Further Roles of JAK2 in Tumor Growth	p. 243
References	p. 246
Intracellular Signal Transduction Cascades	p. 265
The PI3K/PTEN Pathway	p. 266
PI3K	p. 267
PDK1	p. 270
AKT	p. 271
Other AGC Kinases	p. 273
PI3K Pathway Activation in Cancer	p. 275
mTOR Signaling	p. 279
mTOR	p. 279
p70S6 Kinase	p. 282
mTOR Pathway Activation in Cancer	p. 283
MAPK Signaling Pathways	p. 284
ERK/MAPK Signaling	p. 285
RAF Family Kinases	p. 286
MEK and ERK Kinases	p. 289
ERK/MAPK Pathway Activation in Cancer	p. 291
PIM Kinases	p. 293
Protein Kinase C	p. 294
PKC Activation	p. 295
Classical PKCs	p. 298
Novel PKCs	p. 299
Atypical PKCs	p. 300
Reference	p. 301
Cell Cycle Control	p. 327
Cyclin-Dependent Kinases (CDKs) and Cell Cycle Progression	p. 327
Introduction	p. 328
CDK4 and CDK6	p. 332
CDK2	p. 334
CDK3	p. 337
CDK1	p. 337
CDK10	p. 341
CCRK/CDCH/p42	p. 341
CDKs and mRNA Production	p. 342
Introduction	p. 342
CDK7	p. 344
CDK8	p. 346
CDK9	p. 347
CDK11	p. 348
CDK12 (CDC2-Related Kinase CRKRS)	p. 350
CDK13 (CDC2L5)	p. 351
Other CDK-Related Kinases	p. 352
CDK5	p. 352
GAK	p. 353
Mitotic Kinases	p. 354
PLKs	p. 356
Aurora Kinases	p. 359
Cell Cycle Checkpoint Kinases	p. 361
ATM, ATR, and DNAPK	p. 362
CHK1, CHK2, and MAPKAPK2	p. 364
References	p. 364
Structural Biochemistry of Kinase Inhibitors	p. 391
Strategies for Inhibitor Design	p. 392
Targeting the Active Versus Inactive Form	p. 392
ATP-Competitive Versus Noncompetitive Inhibitors	p. 393
Specific Versus Multitargeted Inhibitors	p. 394
Architecture of the ATP Binding Site: DFG-in	p. 396
Case Study: Inhibitors of CHK1	p. 399
Case Study: Inhibitors of CDK2	p. 407
Case Study: Inhibitors of SRC Family Kinases	p. 413
Case Study: EGF Receptor Inhibitors	p. 416
Targeting the Inactive Conformation	p. 420
Binding Mode of Imatinib	p. 421
Binding of BAY-43-9006 (Sorafenib) to the Inactive BRAF Kinase	p. 423
Noncompetitive Inhibition	p. 424
Kinase Inhibitor Specificity	p. 426
References	p. 429
Tyrosine Kinase Inhibitors	p. 435
BCR-ABL Inhibitors	p. 435
SRC Inhibitors	p. 446
JAK2 Inhibitors	p. 443
EGFR/ERBB Inhibitors	p. 452
Determinants of Response and Resistance to ERBB Inhibitors	p. 455
IGF1R Inhibitors	p. 470
FLT3 Inhibitors	p. 472
KIT Inhibitors	p. 480
MET/RON Inhibitors	p. 490
RET Inhibitors	p. 496
Other Inhibitors	p. 498
FAK	p. 498
TGFß Receptor	p. 499
References	p. 500
Angiokinase Inhibitors	p. 527
Introduction	p. 527
Angiokinase Inhibitors	p. 530
References	p. 555
Intracellular Signaling Kinase Inhibitors	p. 567
mTOR Inhibitors	p. 567
Clinical Pharmacodynamics and Tolerability of mTOR Inhibitors	p. 569
PI3K Inhibitors	p. 578
RAF Kinase Inhibitors	p. 582
MEK Inhibitors	p. 584
CDK Inhibitors	p. 587
Cell Cycle Checkpoint Kinase Inhibitors	p. 593
Mitotic Kinase Inhibitors	p. 597
PLK Inhibitors	p. 597
Aurora Kinase Inhibitors	p. 599
Protein Kinase C Inhibitors	p. 604
References	p. 605
Current Challenges and Future Directions	p. 623
Kinase Inhibitor Drug Resistance	p. 623
Efflux Pumps and Drug Transporters	p. 626
Other DMPK Factors	p. 627
Target Mutation	p. 628
Target Overexpression and Activation	p. 631
Downstream Pathway Activation	p. 632
Redundant Receptors/Pathways	p. 633
Combination Therapy With Kinase Inhibitors	p. 635
Angiogenesis Inhibitors and Chemotherapy	p. 637
Survival Pathway Inhibitors and Chemotherapy/Targeted Therapy	p. 638
DNA Damage Checkpoint Inhibitors and Chemotherapy	p. 639
RTK Switching: Targeting Receptor Redundancy	p. 640
Systems Biology and Translational Medicine	p. 641
Classification of Tumors and Prediction of Response: Expression Profiling	p. 642
Phosphoprotein Analysis, Kinomics, and Systems-Based Approaches	p. 645
Translational Medicine	p. 647
Conclusions	p. 652
References	p. 653
List of Abbreviations	p. 665
Index	p. 689
Table of Contents provided by Ingram. All Rights Reserved.

Amazon no longer offers textbook rentals. We do!

Targeting Protein Kinases for Cancer Therapy

Targeting Protein Kinases for Cancer Therapy

9780470229651

0470229659

Summary

Author Biography

Table of Contents

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