Chapter
1. Background and Scientific Overview:
Kinases Are Important
Cellular Signaling Enzymes
1.1 The Function of Kinases
1.2 Classifying Kinases
1.3 Kinases: Ubiquitous Drug Targets
The Established Link to Cancer
Targeting Receptor Tyrosine Kinases
Targeting Non-receptor Tyrosine Kinases
Targeting Serine-Threonine Kinases for Cancer
Targeting Serine-Threonine Kinases for Diseases Other than Cancer
1.4 Overview of the Field
Chapter 2. Kinase Inhibitors in Development:
Tapping
into a Wealth of Targets
2.1 Types of Kinase Inhibitors: Small Molecules and Their Alternatives
2.2 Receptor Tyrosine Kinase Inhibitors
EGFR Family
Split Kinase Domain Family
Targeting VEGF with RNAi for Opthalmic Diseases
2.3 Non-receptor Tyrosine Kinase Inhibitors
Abl
Tec Family Kinases
Syk
JAK
2.4 Serine-Threonine Kinase Inhibitors for Cancer
Ras-Raf-MEK-ERK Pathway
ALK5
PKC-α
PKC-ß
ROCK
PI3 Kinase Pathway
mTOR
CDK
Aurora
PLK
CHK
2.5 Serine-Threonine Kinase Inhibitors for Diseases Other than Cancer
PKC-δ
p38 MAP Kinase
JNK
MLK
NF-кB Pathway
PI3 Pathway
GSK3
mTOR
AMPK
PDHK
Chapter 3. Business and Strategic Outlook:
Market
Potential for Kinase-Targeted Drugs
3.1 Special Challenges in Developing Kinase Modulators
Target Relevance and Specificity
Resistance
Trial Design
Cost
3.2 Markets for Kinase-Based Drugs
Cancer
Age-Related Macular Degeneration
Immune and Inflammatory Diseases
Diabetic Complications
Chapter 4. Expert Commentaries
4.1 Shripad Bhagwat, PhD, SVP, Drug Discovery, Ambit Biosciences
4.2 Sean G. Buchanan, PhD, Senior Director, Biology, SGX Pharmaceuticals
4.3 K. Peter Hirth, Phd, CEO, Plexxikon
4.4 Tony Hunter, PhD, Professor, Salk Institute for Biological Studies
4.5 Michael Melnick, VP, Business and Corporate Development, Cell Signaling
Technology
Chapter 5. Company Profiles
5.1. Ambit Biosciences
5.2. Amgen
5.3. Amphora Discovery
5.4. ARIAD Pharmaceuticals
5.5. Astex Therapeutics
5.6. AstraZeneca
5.7. BioFocus
5.8. Bristol-Myers Squibb
5.9. Cell Signaling Technology
5.10 CGI Pharmaceuticals
5.11 Cyclacel Pharmaceuticals
5.12. Eli Lilly & Co.
5.13. Exelixis
5.14. Millennium Pharmaceuticals
5.15. Novartis
5.16. Pfizer
5.17. Rigel Pharmaceuticals
5.18. Sanofi-Aventis
5.19. Semafore Pharmaceuticals
5.20. SGX Pharmaceuticals
5.21. Sunesis Pharmaceuticals
5.22. Upstate
5.23. Vertex Pharmaceuticals
Appendix: Kinase Names
Company Index with Web Addresses
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