Servizio Comunitario di Informazione in materia di Ricerca e Sviluppo - CORDIS

FRET constructs mdm2-EGFP, p53-EYFP for protein inhibitor screens

These vectors, which contain donor and recipient markers for Flourescent Resonance and have been combined to the tow interacting proteins p53 and mdm2 will be useful in the design of a screen for small molecule or peptide based agents that interfere with this protein-protein interaction in cellular models. mdm2 binding to p53 is the pre-cursor signalling p53 for degradation via ubuiquitination. p53 is the most commonly de-regulated tumour suppressor in cancer. Interfering with this degradation signalling so often relied on by cancer cells has been an area of commercial interest for some time and several companies have been evaluating agents for their potential use clinically.

Since FRET itself as a platform as yet is not suitable for high through put screening, these materials nonetheless would be useful in employing secondary cellular screens to help pharmaceutical and biotechnology companies optimise their leads. Companies already in this field include, Roche (who designed the published Nutlin compounds), Cyclacel, AstraZeneca, De Novo, Ascenta Therapeutics, Novelix Pharmaceuticals and the USA institutions, MD Anderson

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UNIVERSITY OF TARTU
INSTITUTE OF MOLECULAR AND CELL BIOLOGY, 23 RIIA STR.
51010 TARTU
Estonia