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The Drug Target Atlas of Protein Kinase Inhibitors in Oncology
Bioseeker, Nov 2007, Pages: 300


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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, the author 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, the author 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, the author 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.


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