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The Drug Target Atlas of Protein Kinase Inhibitors in Oncology

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Published Date Nov 5, 2007
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This report is an open landscape of resources to build, fuel, and drive your scientific competitive vehicle for the advancement of new protein kinase inhibitor drugs in oncology.

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All cancers arise as a result of the acquisition of a series of fixed DNA sequence abnormalities, mutations, many of which ultimately confer a growth advantage upon the cells in which they have occurred. Protein kinases have been implicated in many aspects of tumorigenesis and protein kinase inhibitors (PKIs) have there of arisen as a major therapeutic class of compounds for the treatment of cancer. The plethora of new potential therapeutic drugs have made selection and validation of novel molecular targets of paramount importance.
First in place, BioSeeker has surveyed protein kinase inhibitors in oncology and identified 110 drug targets, belonging to 210 protein kinase inhibitor drugs. This report, The Drug Target Atlas of Protein Kinase Inhibitors in Oncology, is an open landscape of resources to build, fuel, and drive your scientific competitive vehicle for the advancement of new protein kinase inhibitor drugs in oncology.
In the report, BioSeeker reports on 139 unique drug target combinations, each comprised of a different collection or mix of individually defined targets, for 210 PKI drugs designed for the treatment of more than 50 different cancer indications. The highest degree of distinctiveness among PKIs is achieved by sorting each of them according to targeted cancer indication, drug target mix, and drug compound type. At the same time we are also identifying peer groups of drugs, that is, drugs we consider suitable for head-to-head comparison during drug development.
To fuel the scientific and competitive thinking, BioSeeker opens the gate into the presence and relevance of protein-protein interactions between identified PKI drug targets. No less than 519 protein-protein interactions were recognized among 98 of the 110 included PKI drug targets.

The report by the numbers:

  • 300+ pages, with almost a hundred different tables. Includes close to 1,000 active links to related resources on the Internet
  • 210 Protein kinase inhibitor drugs, under development by 107 investigators, are included, covering more than 600 developmental projects in cancer
  • 110 Unique, in-depth, drug target profiles, highlighting twelve themes about the drug target, i.e. protein-protein interaction with other PKI drug targets, linked cancer indications, presence in the Cancer Genome Project etc.
  • 139 Unique drug target combinations of PKI drugs
  • 519 protein-protein interactions among PKI drug targets
  • 20 Major signaling pathways covered

This report serves as a serious reference for any professional interested in the development of oncology drug targets and the selection/validation of targeting strategies.

1 Executive Summary
2 About Cancer Highlights

3 Methodologies

4 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

4.1 List of Figures
Figure 1: Distribution of Drug Compound Types Among Protein Kinase Inhibitors

4.2 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 and 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

- 4SC
- AB Science
- Abbott
- Adnexus Therapeutics
- Aeterna Zentaris
- Aida Pharmaceuticals
- Alethia Biotherapeutics
- Alfacell
- Ambit Biosciences
- Amgen
- Amphora
- Ariad
- Ark Therapeutics
- ArQule
- Array BioPharma
- Astex Therapeutics
- AstraZeneca
- Avalon
- Bayer
- BioImage
- Biomira
- Biotica Technology
- Boehringer Ingelheim
- Bristol-Myers Squibb
- BTG
- Callisto Pharmaceuticals
- Cancer Research Technology
- Celldex
- Center of Molecular Immunology
- Cephalon
- Chlorogen
- Chroma Therapeutics
- Cyclacel
- Cylene Pharmaceuticals
- Cytokine PharmaSciences
- Dainippon Sumitomo Pharma
- DeveloGen
- Dyax
- Ecopia BioSciences
- Eisai
- Eli Lilly
- EntreMed
- ESBATech
- Exelixis
- Galapagos
- Genentech
- Generex
- Genmab
- GlaxoSmithKline
- GlycoGenesys
- Hemispherx Biopharma
- Hoffmann-La Roche
- Idera Pharmaceuticals
- ImClone Systems
- ImmunoGen
- Insmed
- Johnson & Johnson
- Kalypsys
- Kirin Brewery
- Kyowa Hakko
- Locus Pharmaceuticals
- Medarex
- MedImmune
- Merck & Co
- Merck KGaA
- MethylGene
- Millennium
- Nerviano Medical Sciences
- Neuren
- Nicholas Piramal
- NIH
- Nippon Shinyaku
- Novartis
- Novogen
- Onconova
- OSI Pharmaceuticals
- Peregrine Pharmaceuticals
- Pfizer
- Pharmacyclics
- PharmaGap
- PharmaMar
- Pharmexa
- Pierre Fabre
- PIramed
- Plexxikon
- Reata Pharmaceuticals
- Rexahn
- Rigel
- Sanofi-Aventis
- Semafore Pharmaceuticals
- SGX Pharmaceuticals
- SR Pharma
- Sunesis
- SuperGen
- Surface Logix
- Switch Pharma
- Targa Therapeutics
- Telik
- TopoTarget
- Trion Pharma
- UCB
- VasGene Therapeutics
- Velacor Therapeutics
- Vertex Pharmaceuticals
- ViroMed
- Wyeth
- Zenyaku Kogyo

Request Sample Pages or Access via 1stOncology™

  • You can request Free Sample Pages to The Drug Target Atlas of Protein Kinase Inhibitors in Oncology.
    To find out more about The Drug Target Atlas of Protein Kinase Inhibitors in Oncology, please read the product description below.
    We also are happy to email you out free sample pages which contain screen shots and more information on the methodology behind the product.

    Did you know that The Drug Target Atlas of Protein Kinase Inhibitors in Oncology is part of the 1stOncology™ platform and can be accessed at no extra cost?

    1stOncology™ allows you to always stay on top of what is really going on in the world of cancer drug development and have an edge when it comes to Search & Evaluation, Indication Selection & Expansion, Target Scouting, First-in-Class analysis and much, much more.


    Or

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