Objective The Polycomb repressive complex (PRC2) complex catalyzes the trimethylation of lysine 27 on histone H3 (H3K27me3), which is an important epigenetic mark for maintaining transcriptional repression. The interaction between the two of the components, EED and EZH2, of PRC2 is essential for the required histone lysine methyltransferase (HKMTase) activity that resides in the SET-domain of EZH2. We propose to design the inhibitors of EED-EZH2 interaction using the recently reported X-ray crystal structure of the complex and employing computational drug design methods. A stepwise rational approach will be employed that would involve, identifying a binding sites around the important amino acid residues of EED, structure-based pharmacophore generation, virtual screening, structure optimization and biological screening, in order to discovery the novel HKMTase inhibitors Fields of science engineering and technologymaterials engineeringcrystalsmedical and health sciencesbasic medicinemedicinal chemistrynatural scienceschemical sciencesorganic chemistryamines Programme(s) FP7-PEOPLE - Specific programme "People" implementing the Seventh Framework Programme of the European Community for research, technological development and demonstration activities (2007 to 2013) Topic(s) FP7-PEOPLE-2011-IIF - Marie Curie Action: "International Incoming Fellowships" Call for proposal FP7-PEOPLE-2011-IIF See other projects for this call Funding Scheme MC-IIF - International Incoming Fellowships (IIF) Coordinator IMPERIAL COLLEGE OF SCIENCE TECHNOLOGY AND MEDICINE EU contribution € 209 033,40 Address SOUTH KENSINGTON CAMPUS EXHIBITION ROAD SW7 2AZ LONDON United Kingdom See on map Region London Inner London — West Westminster Activity type Higher or Secondary Education Establishments Administrative Contact Brooke Alasya (Ms.) Links Contact the organisation Opens in new window Website Opens in new window Total cost No data
