Diversity Oriented Synthesis of Protein Kinase Inhibitors

Projektinformationen

DOS PKI

ID Finanzhilfevereinbarung: 23214

Startdatum 1 November 2005

Enddatum 30 April 2006

Finanziert unter

• Human resources and Mobility in the specific programme for research, technological development and demonstration "Structuring the European Research Area" under the Sixth Framework Programme 2002-2006

Gesamtkosten € 0,00

EU-Beitrag € 149 670,00

Koordiniert durch

UNIVERSITE LOUIS PASTEUR, STRASBOURG I
France

Ziel

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.

Wissenschaftliches Gebiet

• 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

Schlüsselbegriffe

• Diversity Oriented Synthesis
• Natural Product Synthesis
• Protein Kinase Inhibitors
• Solid Phase Synthesis

Programm/Programme

• FP6-MOBILITY - Human resources and Mobility in the specific programme for research, technological development and demonstration "Structuring the European Research Area" under the Sixth Framework Programme 2002-2006

Thema/Themen

• MOBILITY-2.1 - Marie Curie Intra-European Fellowships (EIF)

Aufforderung zur Vorschlagseinreichung

FP6-2004-MOBILITY-5
Andere Projekte für diesen Aufruf anzeigen

Finanzierungsplan

SCF - Marie Curie actions-Series of events

Koordinator

UNIVERSITE LOUIS PASTEUR, STRASBOURG I

• EU-Beitrag: Keine Daten
• Adresse: Rue Blaise Pascal, 4 ; STRASBOURG ; Frankreich
• Gesamtkosten: Keine Daten