91
Dual HKMT inhibitor_Cancer
Imperial College London
Small molecule
Oncology
Hit To Lead or Lead Optimization
EZH2 and EHMT2 Histone Methyltransferases are essential for cancer stem cell maintenance
• Existing EZH2 inhibitors have little activity in solid tumours that express wild type EZH2
• EZH2 and EHMT2 show increased copy number and high expression in wide variety of epithelial tumour types
• SiRNA double knock down of EZH2 and EHMT2 or pharmacological inhibition of both EZH2 and EHMT2 is more biologically effective at (Curry et al 2015)a
PCT-GB2013-050689