Scientific Publications

A small molecule that binds Hedgehog and blocks its signaling in human cells.

Publication TypeJournal Article
AuthorsStanton, BZ, Peng LF, Maloof N., Nakai K., Wang X., Duffner JL, Taveras KM, Hyman JM, Lee SW, Koehler AN, Chen JK, Fox JL, Mandinova A., and Schreiber SL
AbstractSmall-molecule inhibition of extracellular proteins that activate membrane receptors has proven to be extremely challenging. Diversity-oriented synthesis and small-molecule microarrays enabled the discovery of robotnikinin, a small molecule that binds the extracellular Sonic hedgehog (Shh) protein and blocks Shh signaling in cell lines, human primary keratinocytes and a synthetic model of human skin. Shh pathway activity is rescued by small-molecule agonists of Smoothened, which functions immediately downstream of the Shh receptor Patched.
Year of Publication2009
JournalNature chemical biology
Date Published (YYYY/MM/DD)2009/03/01
ISSN Number1552-4450