The Drug Target Atlas of Apoptopic Drugs in Oncology

Published by: BioSeeker Group AB

Published: Feb. 6, 2008 - 250+ Pages

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 Apoptopic Drug Compound Types and Sub-cellular Localizations of Targets

7 The Cancer Genome Project and Apoptopic Drug Targets

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

8 Protein Expression Profiles of Apoptopic 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 Pathway Analysis of Drug Targets of Apoptopic Drugs

10 Protein-Protein Interactions Between Identified Apoptopic Drug Targets

11 Available Biological Structure Data on Apoptopic Drug Targets

12 Drug Target Profiles of Apoptopic Drug Targets in Oncology

12.1.1 Auxiliary transport protein activity

12.1.2 Carboxy-lyase activity

12.1.3 Catalytic activity

12.1.4 Cell adhesion molecule activity

12.1.5 Chaperone activity

12.1.6 Complement activity

12.1.7 Cysteine-type peptidase activity

12.1.8 Cytokine activity

12.1.9 DNA topoisomerase activity

12.1.10 Glutathione transferase activity

12.1.11 Hormone activity

12.1.12 Hydrolase activity

12.1.13 Intracellular ligand-gated ion channel activity

12.1.14 Kinase activity

12.1.15 Kinase regulator activity

12.1.16 Ligase activity

12.1.17 Lipid kinase activity

12.1.18 Metallopeptidase activity

12.1.19 Molecular function unknown

12.1.20 Motor activity

12.1.21 Oxidoreductase activity

12.1.22 Peptide hormone

12.1.23 Peroxidase activity

12.1.24 Protein binding

12.1.25 Protein serine/threonine kinase activity

12.1.26 Protein threonine/tyrosine kinase activity

12.1.27 Protein-tyrosine kinase activity

12.1.28 Receptor activity

12.1.29 Receptor binding

12.1.30 Receptor signaling complex scaffold activity

12.1.31 Receptor signaling protein serine/threonine kinase activity

12.1.32 RNA binding

12.1.33 Structural constituent of cytoskeleton

12.1.34 Superoxide dismutase activity

12.1.35 T cell receptor activity

12.1.36 Transcription factor activity

12.1.37 Transcription regulator activity

12.1.38 Transferase activity

12.1.39 Translation regulator activity

12.1.40 Transmembrane receptor activity

12.1.41 Transmembrane receptor protein tyrosine kinase activity

12.1.42 Transporter activity

13 Apoptopic Drug Target Mix by Development Stage

14 Apoptopic Drug Target Mix by Cancer Indication

14.1 Basal Cell Cancer

14.2 Biliary Cancer

14.3 Bladder Cancer

14.4 Bone Cancer

14.5 Brain Cancer

14.6 Breast Cancer

14.7 Carcinoid Tumor

14.8 Cervical Cancer

14.9 Chemotherapy-induced Neutropenia

14.10 Colorectal Cancer

14.11 Endometrial Cancer

14.12 Fallopian Tube Cancer

14.13 Gastrointestinal Cancer

14.13.1 Gastrointestinal Stomach Cancer

14.13.2 Gastrointestinal Stromal Cancer

14.14 Head and Neck Cancer

14.15 Leukemia

14.15.1 Acute Lymphocytic Leukemia

14.15.2 Acute Myelogenous Leukemia

14.15.3 Chronic Lymphocytic Leukemia

14.15.4 Chronic Myelogenous Leukemia

14.16 Liver Cancer

14.17 Lung Cancer

14.17.1 Non-Small Cell Lung Cancer

14.17.2 Small Cell Lung Cancer

14.18 Lymphoma

14.18.1 B-cell Lymphoma

14.18.2 Hodgkin's Lymphoma

14.18.3 non-Hodgkin's Lymphoma

14.18.4 T-cell Lymphoma

14.19 Melanoma

14.20 Mesothelioma

14.21 Myelodysplastic Syndrome

14.22 Myeloma

14.23 Nasopharyngeal Cancer

14.24 Oesophageal Cancer

14.25 Oral Cancer

14.26 Ovarian Cancer

14.27 Pancreatic Cancer

14.28 Peritoneal Cancer

14.29 Prostate Cancer

14.30 Renal Cancer

14.31 Sarcoma

14.31.1 Leiomyo Sarcoma

14.32 Squamous Cell Cancer

14.33 Testicular Cancer

14.34 Thymoma Cancer

14.35 Thyroid Cancer

15 Apoptopic Drugs and their Targets by Companies

15.1 Australia

15.2 Canada

15.3 China

15.4 Denmark

15.5 Germany

15.6 Israel

15.7 Japan

15.8 South Korea

15.9 Spain

15.10 Switzerland

15.11 Taiwan

15.12 United Kingdom

15.13 USA

16 Disclaimer

17 Drug Index

18 Company Index

4.1 List of Figures

Figure 1: Distribution of Compound Types Among Apoptopic Drugs

Figure 2: Primary Sub-cellular Localization of Drug Targets

4.2 List of Tables

Table 1: Compound Type Versus Primary and Alternate Localization of Drug Target

Table 2: Drug Targets of Apoptopic Drugs Present in the Catalogue of Somatic Mutations in Cancer and in the Cancer Gene Census

Table 3: Available Protein Expression Profiles of Apoptopic Drug Targets

Table 4: Pathway Summary

Table 5: Drug Targets Without any Identified Assigned Pathways

Table 6: Pathway Profile According to BioCarta of the Drug Targets Belonging to Apoptopic Drugs

Table 7: Drug Targets Belonging to Apoptopic Pathways According to BioCarta

Table 8: Pathway Profile According to KEGG of the Drug Targets Belonging to Apoptopic Drugs

Table 9: Drug Targets within the Apoptosis Pathway According to KEGG

Table 10: Apoptopic Drugs Targeting Major Singaling Pathways

Table 11: Protein-Protein Interactions Between Identified Apoptopic Drug Targets

Table 12: Targets of Apoptopic Drugs without Protein-Protein Interaction with other Drug Targets

Table 13: Number of Available Biological Structures on Apoptopic Drug Targets

Table 14: Overview of Drug Target Profile Themes

Table 15: Fall Out in Terms of the Number of Drug Target Mixes, Drugs, and Developmental Projects by Developmental Stage

Table 16: Apoptopic Drug Target Mixes by Development

Table 17: Number of Unique Apoptopic Drug Target Mixes Reported by Cancer Indication

Table 18: Apoptopic Drug Target Mix for the Treatment of Basal Cell Cancer According to the Compound Type and Developmental Stage of Drug

Table 19: Apoptopic Drug Target Mix for the Treatment of Biliary Cancer According to the Compound Type and Developmental Stage of Drug

Table 20: Apoptopic Drug Target Mix for the Treatment of Bladder Cancer According to the Compound Type and Developmental Stage of Drug

Table 21: Apoptopic Drug Target Mix for the Treatment of Bone Cancer According to the Compound Type and Developmental Stage of Drug

Table 22: Apoptopic Drug Target Mix for the Treatment of Brain Cancer According to the Compound Type and Developmental Stage of Drug

Table 23: Apoptopic Drug Target Mix for the Treatment of Breast Cancer According to the Compound Type and Developmental Stage of Drug

Table 24: Apoptopic Drug Target Mix for the Treatment of Carcinoid Tumor According to the Compound Type and Developmental Stage of Drug

Table 25: Apoptopic Drug Target Mix for the Treatment of Cervical Cancer According to the Compound Type and Developmental Stage of Drug

Table 26: Apoptopic Drug Target Mix for the Treatment of Chemotherapy-induced Neutropenia According to the Compound Type and Developmental Stage of Drug

Table 27: Apoptopic Drug Target Mix for the Treatment of Colorectal Cancer According to the Compound Type and Developmental Stage of Drug

Table 28: Apoptopic Drug Target Mix for the Treatment of Endometrial Cancer According to the Compound Type and Developmental Stage of Drug

Table 29: Apoptopic Drug Target Mix for the Treatment of Fallopian Tube Cancer According to the Compound Type and Developmental Stage of Drug

Table 30: Apoptopic Drug Target Mix for the Treatment of Gastrointestinal Cancer According to the Compound Type and Developmental Stage of Drug

Table 31: Apoptopic Drug Target Mix for the Treatment of Gastrointestinal Stomach Cancer According to the Compound Type and Developmental Stage of Drug

Table 32: Apoptopic Drug Target Mix for the Treatment of Gastrointestinal Stromal Cancer According to the Compound Type and Developmental Stage of Drug

Table 33: Apoptopic Drug Target Mix for the Treatment of Head and Neck Cancer According to the Compound Type and Developmental Stage of Drug

Table 34: Apoptopic Drug Target Mix for the Treatment of Leukemia (general) According to the Compound Type and Developmental Stage of Drug

Table 35: Apoptopic Drug Target Mix for the Treatment of Acute Lymphocytic Leukemia According to the Compound Type and Developmental Stage of Drug

Table 36: Apoptopic Drug Target Mix for the Treatment of Acute Myelogenous Leukemia According to the Compound Type and Developmental Stage of Drug

Table 37: Apoptopic Drug Target Mix for the Treatment of Chronic Lymphocytic Leukemia According to the Compound Type and Developmental Stage of Drug

Table 38: Apoptopic Drug Target Mix for the Treatment of Chronic Myelogenous Leukemia According to the Compound Type and Developmental Stage of Drug

Table 39: Apoptopic Drug Target Mix for the Treatment of Liver Cancer According to the Compound Type and Developmental Stage of Drug

Table 40: Apoptopic Drug Target Mix for the Treatment of Lung Cancer (general) According to the Compound Type and Developmental Stage of Drug

Table 41: Apoptopic Drug Target Mix for the Treatment of Non-Small Cell Lung Cancer According to the Compound Type and Developmental Stage of Drug

Table 42: Apoptopic Drug Target Mix for the Treatment of Small Cell Lung Cancer According to the Compound Type and Developmental Stage of Drug

Table 43: Apoptopic Drug Target Mix for the Treatment of Lymphoma (general) According to the Compound Type and Developmental Stage of Drug

Table 44: Apoptopic Drug Target Mix for the Treatment of B-cell Lymphoma According to the Compound Type and Developmental Stage of Drug

Table 45: Apoptopic Drug Target Mix for the Treatment of Hodgkin’s Lymphoma According to the Compound Type and Developmental Stage of Drug

Table 46: Apoptopic Drug Target Mix for the Treatment of non-Hodgkin’s Lymphoma According to the Compound Type and Developmental Stage of Drug

Table 47: Apoptopic Drug Target Mix for the Treatment of T-cell Lymphoma According to the Compound Type and Developmental Stage of Drug

Table 48: Apoptopic Drug Target Mix for the Treatment of Melanoma According to the Compound Type and Developmental Stage of Drug

Table 49: Apoptopic Drug Target Mix for the Treatment of Mesothelioma According to the Compound Type and Developmental Stage of Drug

Table 50: Apoptopic Drug Target Mix for the Treatment of Myelodysplastic Syndrome According to the Compound Type and Developmental Stage of Drug

Table 51: Apoptopic Drug Target Mix for the Treatment of Myeloma According to the Compound Type and Developmental Stage of Drug

Table 52: Apoptopic Drug Target Mix for the Treatment of Nasopharyngeal Cancer According to the Compound Type and Developmental Stage of Drug

Table 53: Apoptopic Drug Target Mix for the Treatment of Oesophageal Cancer According to the Compound Type and Developmental Stage of Drug

Table 54: Apoptopic Drug Target Mix for the Treatment of Oral Cancer According to the Compound Type and Developmental Stage of Drug

Table 55: Apoptopic Drug Target Mix for the Treatment of Ovarian Cancer According to the Compound Type and Developmental Stage of Drug

Table 56: Apoptopic Drug Target Mix for the Treatment of Pancreatic Cancer According to the Compound Type and Developmental Stage of Drug

Table 57: Apoptopic Drug Target Mix for the Treatment of Peritoneal Cancer According to the Compound Type and Developmental Stage of Drug

Table 58: Apoptopic Drug Target Mix for the Treatment of Prostate Cancer According to the Compound Type and Developmental Stage of Drug

Table 59: Apoptopic Drug Target Mix for the Treatment of Renal Cancer According to the Compound Type and Developmental Stage of Drug

Table 60: Apoptopic Drug Target Mix for the Treatment of Sarcoma (general) According to the Compound Type and Developmental Stage of Drug

Table 61: Apoptopic Drug Target Mix for the Treatment of Leiomyo Sarcoma According to the Compound Type and Developmental Stage of Drug

Table 62: Apoptopic Drug Target Mix for the Treatment of Squamous Cell Cancer According to the Compound Type and Developmental Stage of Drug

Table 63: Apoptopic Drug Target Mix for the Treatment of Testiculat Cancer According to the Compound Type and Developmental Stage of Drug

Table 64: Apoptopic Drug Target Mix for the Treatment of Thymoma Cancer According to the Compound Type and Developmental Stage of Drug

Table 65: Apoptopic Drug Target Mix for the Treatment of Thyroid Cancer According to the Compound Type and Developmental Stage of Drug

Table 66: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in Australia

Table 67: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in Canada

Table 68: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in China

Table 69: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in Denmark

Table 70: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in Germany

Table 71: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in Israel

Table 72: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in Japan

Table 73: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in South Korea

Table 74: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in Spain

Table 75: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in Switzerland

Table 76: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in Taiwan

Table 77: Apoptopic Drugs with Target Mix and Developmental Projects by Companies in United Kingdom

Table 78: Apoptopic Drugs with Target Mix and Developmental Projects by Company in USA

Abstract

Executive Summary

The ultimate goal of cancer research is to learn how to make cancer cells selectively die. Apoptosis is the type of death about whose genetically controlled pathways we know the most.

Apoptotic cell death can be triggered by many different cellular stimuli, resulting in activation of apoptotic signaling pathways including extrinsic, intrinsic, and mitochondrial pathways. The plethora of new potential therapeutic drugs has made selection and validation of novel molecular targets of paramount importance.

First in place, BioSeeker has surveyed apoptopic drugs in oncology and identified 119 drug targets, belonging to 114 drugs. This report, The Drug Target Atlas of Apoptopic Drugs in Oncology, is an open landscape of resources to build, fuel, and drive your scientific competitive vehicle for the advancement of new apoptopic drugs in oncology.

In the report, BioSeeker reports on 90 unique drug target combinations, each comprised of a different collection or mix of individually defined targets, for 114 apoptopic drugs designed for the treatment of 48 different cancer indications. The highest degree of distinctiveness among apoptopic drugs 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 targets of apoptopic drugs. No less than 452 protein-protein interactions were recognized among 96 of the 119 included apoptopic drug targets.

The report by the numbers

• 250+ pages, with almost a hundred different tables. Includes more than 1,500 active links to related resources on the Internet
• 114 apoptopic drugs, under development by 87 investigators, are included, covering more than 430 developmental projects in cancer
• 119 Unique, in-depth, drug target profiles, highlighting twelve themes about the drug target, i.e. protein-protein interaction with other apoptopic drug targets, linked cancer indications, drugs under development, compound types, presence in the Cancer Genome Project etc.
• 90 Unique drug target combinations of apoptopic drugs
• 452 protein-protein interactions among apoptopic drug targets

Extensive pathway analysis of drug targets

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.

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