CORDIS Project
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The project aims to design inhibitors for the interaction between two components of the Polycomb repressive complex, which is crucial for gene regulation. Using computational methods, it seeks to develop new drugs that can modulate this epigenetic mechanism.
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 struct…
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