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A small molecule that binds Hedgehog and blocks its signaling in human cells.
|Publication Type||Journal Article|
|Authors||Stanton, 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|
|Abstract||Small-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 Publication||2009|
|Journal||Nature chemical biology|
|Date Published (YYYY/MM/DD)||2009/03/01|