S. Borman
Apr 11, 2011
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Abstract
RESEARCHERS HAVE devised the first enantioselective synthesis of the small molecule nutlin-3, a key member of a family of compounds that are tools for cancer research and promising leads for anticancer drug discovery ( Chem. Sci., DOI: 10.1039/C1SC00061F). Nutlins were discovered by researchers at Hoffmann-La Roche, Nutley, N.J. ( Science, DOI: 10.1126/science.1092472). The company has a nutlin analog, RG7112, in clinical trials for leukemia and advanced solid tumors. The new synthesis currently produces only nutlin-3 but has the potential to be adapted for the synthesis of other nutlin derivatives. Nutlin-3 is widely used to study the role of the tumor-suppressing protein p53. In normal cells, p53 triggers apoptosis, a pathway by which damaged or unwanted cells initiate their own destruction for the good of the organism. But this p53-initiated apoptosis pathway is turned off in cancer cells, allowing them to divide without limit. Nutlin-3 binds the p53-regulating protein MDM2, causing p53 and apoptotic t...