Journal article
A small molecule that binds Hedgehog and blocks its signaling in human cells
In
Nature Chemical Biology
—
2009, Volume 5, Issue 3, pp. 154-156
From
Broad Institute of Harvard and Massachusetts Institute of Technology, 7 Cambridge Center, Cambridge, Massachusetts 02142, USA.1
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.
| Language: | English |
|---|---|
| Publisher: | Nature Publishing Group US |
| Year: | 2009 |
| Pages: | 154-156 |
| ISSN: | 15524469 and 15524450 |
| Types: | Journal article |
| DOI: | 10.1038/nchembio.142 |
