Histone Modification

Medicinal Chemistry Team Three

Section: Cancer Research UK Cancer Therapeutics Unit

Histones are the proteins around which DNA is coiled to form chromatin. Post-translational modification of histones by acetylation, phosphoryation and methylation forms the so-called histone code which regulates histone function and hence DNA transcription. We have a particular interest, in conjunction with Chroma Therapeutics, in histone methylation. The enzyme, histone lysine methyl transferase controls this process and we are screening for inhibitors of this protein using biological assays and virtual screening with our colleague in computational chemistry, Dr Johannes Reynisson. We plan to collaborate with Dr Jon Wilson, who has recently joined the Section of Structural Biology, and use his knowledge and experience of the SET7/9 enzymes to provide a new dimension to our work.