Objective
Protein kinases (PKs) are important regulators of cellular networks but our current understanding of the role of individual kinases is in part limited by our ability to measure and modulate their activity. In this respect, small molecule inhibitors are va luable tools. The project proposes to synthesize a focused library targeted towards PKs that is based on two potent and selective natural products, a MEK and a TAK1 inhibitor. These two kinases are important therapeutic targets as the activity of MEK has been identified in a number of cancers and TAK1 is important in the inflammation pathway. The library could prove valuable in improving the activity of these natural leads but perhaps more importantly, could extend to the discover of new inhibitors agains t "orphan kinases". First, a concise synthesis using solution phase and solid phase chemistry is proposed to access to both natural products from a common late stage intermediate. Importantly, the proposed chemistry is amenable to library synthesis. A strong emphasis will be put on the use of molecular modeling to evaluate library diversity and conformational diversity of the library. Second, based on the optimized chemistry developed towards the natural product, and the selected point of diversity ide ntified from modeling, the library will be synthesized. The host laboratory is developing microarray based profiling methods to assess kinase inhibitors on a proteomic scale. The library will be evaluated using this kinase profiling technology as well as a more traditional assay.
Fields of science (EuroSciVoc)
CORDIS classifies projects with EuroSciVoc, a multilingual taxonomy of fields of science, through a semi-automatic process based on NLP techniques. See: The European Science Vocabulary.
CORDIS classifies projects with EuroSciVoc, a multilingual taxonomy of fields of science, through a semi-automatic process based on NLP techniques. See: The European Science Vocabulary.
- natural sciences biological sciences biochemistry biomolecules proteins
- engineering and technology electrical engineering, electronic engineering, information engineering information engineering telecommunications telecommunications networks mobile network
- medical and health sciences clinical medicine oncology
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Keywords
Project’s keywords as indicated by the project coordinator. Not to be confused with the EuroSciVoc taxonomy (Fields of science)
Project’s keywords as indicated by the project coordinator. Not to be confused with the EuroSciVoc taxonomy (Fields of science)
Programme(s)
Multi-annual funding programmes that define the EU’s priorities for research and innovation.
Multi-annual funding programmes that define the EU’s priorities for research and innovation.
Topic(s)
Calls for proposals are divided into topics. A topic defines a specific subject or area for which applicants can submit proposals. The description of a topic comprises its specific scope and the expected impact of the funded project.
Calls for proposals are divided into topics. A topic defines a specific subject or area for which applicants can submit proposals. The description of a topic comprises its specific scope and the expected impact of the funded project.
Call for proposal
Procedure for inviting applicants to submit project proposals, with the aim of receiving EU funding.
Procedure for inviting applicants to submit project proposals, with the aim of receiving EU funding.
FP6-2004-MOBILITY-5
See other projects for this call
Funding Scheme
Funding scheme (or “Type of Action”) inside a programme with common features. It specifies: the scope of what is funded; the reimbursement rate; specific evaluation criteria to qualify for funding; and the use of simplified forms of costs like lump sums.
Funding scheme (or “Type of Action”) inside a programme with common features. It specifies: the scope of what is funded; the reimbursement rate; specific evaluation criteria to qualify for funding; and the use of simplified forms of costs like lump sums.
Coordinator
STRASBOURG
France
The total costs incurred by this organisation to participate in the project, including direct and indirect costs. This amount is a subset of the overall project budget.