“This is a totally new approach to cancer therapy,” said Professor Patrick Gunning of chemical and physical sciences (University of Toronto). “Everything prior to this has targeted functionally relevant binding sites. Our approach inhibits the mobility of cancer-promoting proteins within cells — essentially, it’s like molecularly targeted glue.”
The “glue” is shaped like a dumbbell: at one end is an anchor that sticks to the membrane and at the other is a molecule that binds to the cancer-promoting proteins. The anchor is a cholesterol molecule that is well known to chemists for sticking to cell membranes. The protein recognition molecule is fairly picky about what it will bind to, reducing the risk of drug-related side effects.
Gunning said that by sticking the target proteins to the cell membrane, the glue-like substance interferes with how they cause cancer cells to multiply out of control. However, on a normal cell, the new therapy should have little effect.
“We are really excited about the potential for this type of drug,” said Gunning, who developed the concept along with Professor Claudiu Gradinaru at U of T Mississauga and Professor James Turkson at the University of Central Florida. “This is ready to move to preclinical studies and this treatment could slow or stop the explosive growth of cancerous tumours. And for patients, this might reduce the need for really powerful chemotherapy, which can be very hard to tolerate.”
Avadisian, M., Fletcher, S., Lui, B., Zhao, W., Zhang, X., Yue, P., Badali, D., Xu, W., Schimmer, A. D., Turkson, J., Gradinaru, C. C., Gunning, P. T.”Artificially Induced Protein-Membrane Anchorage with Cholesterol-based Recognition Agents: Towards a New Therapeutic Concept.” Angewandte Chemie Intl, 2011, in press, anie.201102486