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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 |
| Volume | 5 |
| Issue | 3 |
| Pages | 154-6 |
| Date Published (YYYY/MM/DD) | 2009/03/01 |
| ISSN Number | 1552-4450 |
| DOI | 10.1038/nchembio.142 |
| PubMed | http://www.ncbi.nlm.nih.gov/pubmed/19151731?dopt=Abstract |
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