The Drug Target Atlas of Protein Kinase Inhibitors in Oncology

Table of Contents

1 Executive Summary

2 About Cancer Highlights

3 Methodologies

4 Table of Contents

• 4.1 List of Figures
• 4.2 List of Tables

5 Introduction

6 PKI Drug Compound Types and Sub-cellular Localizations of Targets

7 The Cancer Genome Project and Protein Kinase Inhibitors

• 7.1 PKI Drug Targets Present in the Cancer Gene Census and in the Catalogue of Somatic Mutations in Cancer

8 Protein Expression Profiles of PKI Drug Targets in Human

• 8.1 Expression in Normal Tissues and Cancer Tissues
• 8.2 Expression in Human Cancer Cell Lines and Primary Cells

9 Protein Kinase Inhibitors in Major Cell Signaling Pathways

• 9.1 Alpha6 Beta4 Integrin Signaling Pathway
• 9.2 Androgen Receptor Signaling Pathway
• 9.3 B Cell Receptor Signaling Pathway
• 9.4 EGFR1 Signaling Pathway
• 9.5 Hedgehog Signaling Pathway
• 9.6 ID Signaling Pathway
• 9.7 IL-1 Signaling Pathway
• 9.8 IL-2 Signaling Pathway
• 9.9 IL-3 Signaling Pathway
• 9.10 IL-4 Signaling Pathway
• 9.11 IL-5 Signaling Pathway
• 9.12 IL-6 Signaling Pathway
• 9.13 IL-7 Signaling Pathway
• 9.14 IL-9 Signaling Pathway
• 9.15 Kit Receptor Signaling Pathway
• 9.16 Notch Signaling Pathway
• 9.17 T Cell Receptor Signaling Pathway
• 9.18 TGF-beta Receptor Signaling Pathway
• 9.19 TNF-alpha Signaling Pathway
• 9.20 Wnt Signaling Pathway

10 Protein-Protein Interactions Between Identified PKI Drug Targets

11 Available Biological Structure Data on PKI Drug Targets

12 Drug Target Profiles of Protein Kinase Inhibitory Drug Targets in Oncology

• 12.1 Kinase Activity Target
  • 12.1.1 Kinase Activity
  • 12.1.2 Protein Serine/Threonine Kinase Activity
  • 12.1.3 Lipid Kinase Activity
  • 12.1.4 Protein Threonine/Tyrosine Kinase Activity
  • 12.1.5 Protein-Tyrosine Kinase Activity
  • 12.1.6 Receptor Activity
  • 12.1.7 Receptor Signaling Protein Serine/Threonine Kinase Activity
  • 12.1.8 Transmembrane Receptor Protein Tyrosine Kinase Activity
• 12.2 Non Kinase Activity Targets
  • 12.2.1 Carboxy-lyase Activity
  • 12.2.2 Cell Adhesion Molecule Activity
  • 12.2.3 Chaperone activity
  • 12.2.4 Cysteine-type Peptidase Activity
  • 12.2.5 DNA Topoisomerase Activity
  • 12.2.6 DNA-Directed DNA Polymerase Activity
  • 12.2.7 Growth Factor Activity
  • 12.2.8 Hormone Activity
  • 12.2.9 Hydrolase Activity
  • 12.2.10 Kinase Regulator Activity
  • 12.2.11 Ligase Activity
  • 12.2.12 Lipid Phosphatase Activity
  • 12.2.13 Oxidoreductase Activity
  • 12.2.14 Protein Binding
  • 12.2.15 Receptor Binding
  • 12.2.16 Receptor Signaling Complex Scaffold Activity
  • 12.2.17 RNA Binding
  • 12.2.18 Structural Constituent of Cytoskeleton
  • 12.2.19 Transcription Factor Activity
  • 12.2.20 Transcription Regulator Activity
  • 12.2.21 Translation Regulator Activity
  • 12.2.22 Transporter Activity

13 Protein Kinase Inhibitor Drug Target Mix by Cancer Indications

• 13.1 Basal Cell Cancer
• 13.2 Biliary Cancer
• 13.3 Bladder Cancer
• 13.4 Bone Cancer
• 13.5 Brain Cancer
• 13.6 Breast Cancer
• 13.7 Carcinoid
• 13.8 Cervical Cancer
• 13.9 Cervical Dysplasia
• 13.10 Chemotherapy-induced Bone Marrow Anemia
• 13.11 CNS Cancer
• 13.12 Colorectal Cancer
• 13.13 Endometrial Cancer
• 13.14 Fallopian Tube Cancer
• 13.15 Gastrointestinal Cancer
• 13.15.1 Gastrointestinal Stomach Cancer
• 13.15.2 Gastrointestinal Stromal Cancer
• 13.16 Head and Neck Cancer
• 13.17 Leukemia
  • 13.17.1 Acute Lymphocytic Leukemia
  • 13.17.2 Acute Myelogenous Leukemia
  • 13.17.3 Chronic Lymphocytic Leukemia
  • 13.17.4 Chronic Myelogenous Leukemia
• 13.18 Liver Cancer
• 13.19 Lung Cancer
  • 13.19.1 Non-Small Cell Lung Cancer
  • 13.19.2 Small Cell Lung Cancer
• 13.20 Lymphoma
  • 13.20.1 B-cell Lymphoma
  • 13.20.2 Hodgkin' s Lymphoma
  • 13.20.3 Non-Hodgkin`s Lymphoma
  • 13.20.4 T-cell Lymphoma
• 13.21 Melanoma
• 13.22 Mesothelioma
• 13.23 Myelodysplastic syndrome
• 13.24 Myeloma
  • 13.24.1 Multiple Myeloma
• 13.25 Nasopharyngeal Cancer
• 13.26 Oesophageal Cancer
• 13.27 Ovarian Cancer
• 13.28 Pancreatic Cancer
• 13.29 Peritoneal Cancer
• 13.30 Prostate Cancer
• 13.31 Renal Cancer
  • 13.31.1 Renal Cell Carcinoma
• 13.32 Sarcoma
  • 13.32.1 Leiomyo Sarcoma
• 13.33 Squamous Cell Cancer
• 13.34 Testicular Cancer
• 13.35 Thymoma
• 13.36 Thyroid Cancer

14 Protein Kinase Inhibitor Drugs and Targets by Companies

• 14.1 Australia
• 14.2 Belgium
• 14.3 Canada
• 14.4 China
• 14.5 Cuba
• 14.6 Denmark
• 14.7 France
• 14.8 Germany
• 14.9 India
• 14.10 Italy
• 14.11 Japan
• 14.12 New Zealand
• 14.13 South Korea
• 14.14 Spain
• 14.15 Switzerland
• 14.16 United Kingdom
• 14.17 USA

15 Disclaimer

16 Drug Index

17 Company Index

18 Appendix I: PKI Drug Target Mix

List of Figures

• Figure 1: Distribution of Drug Compound Types Among Protein Kinase Inhibitors

List of Tables

• Table 1: Compound Type Versus Primary and Alternate Localization of Drug Target
• Table 2: Probability Ranking of Identified Drug Targeted Protein Kinases to Actually Carry ' Driver' Mutations Contributing to the Development of Cancers
• Table 3: PKI Drug Targets Present in the Catalogue of Somatic Mutations in Cancer and in the Cancer Gene Census
• Table 4: Available Protein Expression Profiles of PKI Drug Targets
• Table 5: Protein Kinase Inhibitors and Cell Signaling: An Overview
• Table 6: PKI Drug Targets in the Alpha6 Beta4 Integrin Signaling Pathway
• Table 7: PKI Drug Targets in the Androgen Receptor Signaling Pathway
• Table 8: PKI Drug Targets in the B Cell Receptor Signaling Pathway
• Table 9: PKI Drug Targets in the EGFR1 Signaling Pathway
• Table 10: PKI Drug Targets in the Hedgehog Signaling Pathway
• Table 11:PKI Drug Targets in the ID Signaling Pathway
• Table 12:PKI Drug Targets in the IL-1 Signaling Pathway
• Table 13:PKI Drug Targets in the IL-2 Signaling Pathway
• Table 14:PKI Drug Targets in the IL-3 Signaling Pathway
• Table 15:PKI Drug Targets in the IL-4 Signaling Pathway
• Table 16: PKI Drug Targets in the IL-5 Signaling Pathway
• Table 17: PKI Drug Targets in the IL-6 Signaling Pathway
• Table 18: PKI Drug Targets in the IL-7 Signaling Pathway
• Table 19: PKI Drug Targets in the IL-9 Signaling Pathway
• Table 20: PKI Drug Targets in the Kit Receptor Signaling Pathway
• Table 21: PKI Drug Targets in the Notch Signaling Pathway
• Table 22: PKI Drug Targets in the T Cell Receptor Signaling Pathway
• Table 23: PKI Drug Targets in the TGF-beta Receptor Signaling Pathway
• Table 24: PKI Drug Targets in the TNF-alpha Signaling Pathway
• Table 25: PKI Drug Targets in the Wnt Signaling Pathway
• Table 26: Protein-Protein Interactions Between Identified PKI Drug Targets
• Table 27: Number of Available Biological Structures on PKI Drug Targets
• Table 28: Overview of Drug Target Profile Themes
• Table 29: Number of Unique PKI Drug Target Mixes Reported by Cancer Indication
• Table 30: PKI Drug Target Mix for the Treatment of Basal Cell Cancer According to the Compound Type and Developmental Stage of Drug
• Table 31: PKI Drug Target Mix for the Treatment of Biliary Cancer According to the Compound Type and Developmental Stage of Drug
• Table 32: PKI Drug Target Mix for the Treatment of Bladder Cancer According to the Compound Type and Developmental Stage of Drug
• Table 33: PKI Drug Target Mix for the Treatment of Bone Cancer According to the Compound Type and Developmental Stage of Drug
• Table 34: PKI Drug Target Mix for the Treatment of Brain Cancer According to the Compound Type and Developmental Stage of Drug
• Table 35: PKI Drug Target Mix for the Treatment of Breast Cancer According to the Compound Type and Developmental Stage of Drug
• Table 36: PKI Drug Target Mix for the Treatment of Carcinoid According to the Compound Type and Developmental Stage of Drug
• Table 37: PKI Drug Target Mix for the Treatment of Cervical Cancer According to the Compound Type and Developmental Stage of Drug
• Table 38: PKI Drug Target Mix for the Treatment of Cervical Dysplasia According to the Compound Type and Developmental Stage of Drug
• Table 39: PKI Drug Target Mix for the Treatment of Chemotherapy-induced Bone Marrow Anemia According to the Compound Type and Developmental Stage of Drug
• Table 40: PKI Drug Target Mix for the Treatment of CNS Cancer According to the Compound Type and Developmental Stage of Drug
• Table 41: PKI Drug Target Mix for the Treatment of Colorectal Cancer According to the Compound Type and Developmental Stage of Drug
• Table 42: PKI Drug Target Mix for the Treatment of Endometrial Cancer According to the Compound Type and Developmental Stage of Drug
• Table 43: PKI Drug Target Mix for the Treatment of Fallopian Tube Cancer According to the Compound Type Developmental Stage of Drug
• Table 44: PKI Drug Target Mix for the Treatment of Gastrointestinal Cancer According to the Compound Type and Developmental Stage of Drug
• Table 45: PKI Drug Target Mix for the Treatment of Gastrointestinal, Stomach Cancer According to the Compound Type and Developmental Stage of Drug
• Table 46: PKI Drug Target Mix for the Treatment of Gastrointestinal, Stromal Cancer According to the Compound Type and Developmental Stage of Drug
• Table 47: PKI Drug Target Mix for the Treatment of Head and Neck Cancer According to the Compound Type and Developmental Stage of Drug
• Table 48: PKI Drug Target Mix for the Treatment of Leukemia According to the Compound Type and Developmental Stage of Drug
• Table 49: PKI Drug Target Mix for the Treatment of Acute Lymphocytic Leukemia According to the Compound Type and Developmental Stage of Drug
• Table 50: PKI Drug Target Mix for the Treatment of Acute Myelogenous Leukemia According to the Compound Type and Developmental Stage of Drug
• Table 51: PKI Drug Target Mix for the Treatment of Chronic Lymphocytic Leukemia According to the Compound Type and Developmental Stage of Drug
• Table 52: PKI Drug Target Mix for the Treatment of Chronic Myelogenous Leukemia According to the Compound Type and Developmental Stage of Drug
• Table 53: PKI Drug Target Mix for the Treatment of Liver Cancer According to the Compound Type and Developmental Stage of Drug
• Table 54: PKI Drug Target Mix for the Treatment of Lung Cancer According to the Compound Type and Developmental Stage of Drug
• Table 55: PKI Drug Target Mix for the Treatment of Non-Small Cell Lung Cancer According to the Compound Type and Developmental Stage of Drug
• Table 56: PKI Drug Target Mix for the Treatment of Small Cell Lung Cancer According to the Compound Type and Developmental Stage of Drug
• Table 57: PKI Drug Target Mix for the Treatment of Lymphoma According to the Compound Type and Developmental Stage of Drug
• Table 58: PKI Drug Target Mix for the Treatment of B-cell Lymphoma According to the Compound Type and Developmental Stage of Drug
• Table 59: PKI Drug Target Mix for the Treatment of Hodgkin' s Lymphoma According to the Compound Type and Developmental Stage of Drug
• Table 60: PKI Drug Target Mix for the Treatment of Non-Hodgkin' s Lymphoma According to the Compound Type and Developmental Stage of Drug
• Table 61: PKI Drug Target Mix for the Treatment of T-cell Lymphoma According to the Compound Type and Developmental Stage of Drug
• Table 62: PKI Drug Target Mix for the Treatment of Melanoma According to the Compound Type and Developmental Stage of Drug
• Table 63: PKI Drug Target Mix for the Treatment of Mesothelioma According to the Compound Type and Developmental Stage of Drug
• Table 64: PKI Drug Target Mix for the Treatment of Myelodysplastic Syndrome According to the Compound Type and Developmental Stage of Drug
• Table 65: PKI Drug Target Mix for the Treatment of Myeloma According to the Compound Type and Developmental Stage of Drug
• Table 66: PKI Drug Target Mix for the Treatment of Multiple Myeloma According to the Compound Type and Developmental Stage of Drug
• Table 67: PKI Drug Target Mix for the Treatment of Nasopharyngeal Cancer According to the Compound Type and Developmental Stage of Drug
• Table 68: PKI Drug Target Mix for the Treatment of Oesophageal Cancer According to the Compound Type and Developmental Stage of Drug
• Table 69: PKI Drug Target Mix for the Treatment of Ovarian Cancer According to the Compound Type and Developmental Stage of Drug
• Table 70: PKI Drug Target Mix for the Treatment of Pancreatic Cancer According to the Compound Type and Developmental Stage of Drug
• Table 71: PKI Drug Target Mix for the Treatment of Peritoneal Cancer According to the Compound Type and Developmental Stage of Drug
• Table 72: PKI Drug Target Mix for the Treatment of Prostate Cancer According to the Compound Type and Developmental Stage of Drug
• Table 73: PKI Drug Target Mix for the Treatment of Renal Cancer According to the Compound Type and Developmental Stage of Drug
• Table 74: PKI Drug Target Mix for the Treatment of Renal Cell Carcinoma According to the Compound Type and Developmental Stage of Drug
• Table 75: PKI Drug Target Mix for the Treatment of Sarcoma According to the Compound Type and Developmental Stage of Drug
• Table 76: PKI Drug Target Mix for the Treatment of Leiomyo Sarcoma According to the Compound Type and Developmental Stage of Drug
• Table 77: PKI Drug Target Mix for the Treatment of Squamous Cell Cancer According to the Compound Type and Developmental Stage of Drug
• Table 78: PKI Drug Target Mix for the Treatment of Testicular Cancer According to the Compound Type and Developmental Stage of Drug
• Table 79: PKI Drug Target Mix for the Treatment of Thymoma According to the Compound Type and Developmental Stage of Drug
• Table 80: PKI Drug Target Mix for the Treatment of Thyroid Cancer According to the Compound Type and Developmental Stage of Drug
• Table 81: Protein Kinase Inhibitor Drugs with Target Mix and Developmental Projects by Companies in Australia
• Table 82: Protein Kinase Inhibitor Drugs with Target Mix and Developmental Projects by Companies in Belgium
• Table 83: Protein Kinase Inhibitor Drugs with Target Mix and Developmental Projects by Companies in Belgium
• Table 84: Protein Kinase Inhibitor Drugs with Target Mix and Developmental Projects by Companies in China
• Table 85: Protein Kinase Inhibitor Drugs with Target Mix and Developmental Projects by Companies in Cuba
• Table 86: Protein Kinase Inhibitor Drugs with Target Mix and Developmental Projects by Companies in Denmark
• Table 87: Protein Kinase Inhibitor Drugs with Target Mix and Developmental Projects by Companies in France
• Table 88: Protein Kinase Inhibitor Drugs with Target Mix and Developmental Projects by Companies in Germany
• Table 89: Protein Kinase Inhibitor Drugs with Target Mix and Developmental Projects by Companies in India
• Table 90: Protein Kinase Inhibitor Drugs with Target Mix and Developmental Projects by Companies in India
• Table 91: Protein Kinase Inhibitor Drugs with Target Mix and Developmental Projects by Companies in Japan
• Table 92: Protein Kinase Inhibitor Drugs with Target Mix and Developmental Projects by Companies in New Zealand
• Table 93: Protein Kinase Inhibitor Drugs with Target Mix and Developmental Projects by Companies in South Korea
• Table 94: Protein Kinase Inhibitor Drugs with Target Mix and Developmental Projects by Companies in Spain
• Table 95: Protein Kinase Inhibitor Drugs with Target Mix and Developmental Projects by Companies in Switzerland
• Table 96: Protein Kinase Inhibitor Drugs with Target Mix and Developmental Projects by Companies in United Kingdom
• Table 97: Protein Kinase Inhibitor Drugs with Target Mix and Developmental Projects by Companies in the USA