MI-219 binds to MDM2 to prevent MDM2 from inhibiting p53. (Source: University of Michigan Comprehensive Cancer Center)

Researchers at the University of Michigan Comprehensive Cancer Center have designed a small molecule that is highly effective in cell cultures at inhibiting the interaction between this protein, called p53, and another protein that inactivates p53 in cancer.

The protein p53 normally helps suppress tumors, but it is inactivated in almost all human cancers. Often, a protein called human MDM2, binds to p53 and inhibits the tumor suppressor function of p53, promoting cancer development. Using a computer-assisted approach, U-M researchers designed a small molecule, called MI-219, that is highly effective in blocking the interaction of MDM2 and p53. MI-219 specifically kills tumor cells by harnessing the power of p53. In animal models of human cancer, MI-219 completely inhibited tumor growth and appeared to cause no toxicity to animals.

Published in Drug Discovery & Development magazine: Vol. 11, No. 3, March, 2008, p.42.