The <i>seco</i>-steroid vitamin D3 (VD3) has been recognized as a hedgehog (Hh) signaling inhibitor in recent years. Initial studies in this area suggested that VD3 inhibited Hh signal transmission at the level of smoothened, a 7-transmembrane GPCR-like protein. Follow-up studies in our laboratory suggest that VD3 does not bind to the conventional small molecule binding site on the transmembrane domain of smoothened. In order to more clearly define the direct binding target(s) and to fully understand the relationship between VD3 and Hh inhibition, we have synthesized a series of VD3-based probe molecules. Herein, we report their synthesis and preliminary activity against the Hh pathway.<br/>

Synthesis and evaluation of vitamin D3-based probes for cellular target(s) verification

254th National Meeting (2017)

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