Words by GOLD newsdesk
A novel approach for the treatment of aggressive cancer has been developed by researchers from the University of North Carolina at Chapel Hill and the UNC LinebergerComprehensive Cancer Centre.
Based on the discovery of a new role of a chromatin-modulatory enzyme during cancer development, referred to as EZH2, the researchers developed a therapeutic approach called PROTAC by utilising a small-molecule inhibitor for the enzyme, designed in collaboration with chemical biologists at Icahn School of Medicine at Mount Sinai. The findings were published online in Nature Cell Biology. treatment will enable scientists to modulate cancer-cell-specific programs of gene expression and inhibit cancer growth.
“EZH2 plays a very important role during cancer progression and is a known target suitable for drug development,” said Greg Wang, PhD, associate professor of Biochemistry and Biophysics and Pharmacology at the UNC School of Medicine. “We are amazed by the efficiency of small-molecule PROTAC in simultaneously targeting EZH2 and cMyc in cancer cells.”
EZH2 has two alternate binding patterns on chromatin in acute leukaemia cells, which in turn produce two distinct gene-regulatory programs. Jun Wang, PhD, postdoctoral researcher at UNC Lineberger, noted that “this explains why the current small-molecule inhibitors of EZH2 cannot block EZH2 completely. PROTAC addresses this gap”.