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(St. Jude Reference #)
|Discovery of a fluorescent vinblastine analog with high affinity to the human pregnane X receptor (hPXR) Ligand (SJ-13-0009)|
|Description||Researchers at St. Jude Children's Research Hospital have discovered a vinblastine analog with high affinity to the human pregnane X receptor (hPXR) that can be used as a fluorescent probe in assays to study the binding of compound to hPXR. This is the first fluorescent probe for hPXR binding with a disclosed chemical structure. Currently, one company offers a hPXR binding assay kit; but the chemical structure of the hPXR fluorescent probe included in the kit is not disclosed. Knowing the chemical structure is critical to understanding the ligand-PXR interaction, and would make this fluorescent hPXR binding probe preferable.|
|Keywords||vinblastine analog, pregnane X receptor (hPXR), fluorescent probe|
|Granted Patents or Published Applications|
|Related Scientific References||Lin, Wenwei and Chen, Taosheng, “A Vinblastine Fluorescent Probe for Pregnane X Receptor in a Time-Resolved Fluorescence Resonance Energy Transfer Assay,” Analytical Biochemistry, Sept. 14, 2013
|Licensing Opportunities||We are looking for a commercial partner to license this discovery and develop PXR binding assay kits and reagents. Binding to hPXR also risks inducing drug-drug interactions and failure of lead compounds in clinical trials; therefore many drug companies have a dedicated group whose function is evaluating the lead compounds' effect on hPXR binding and activation. Other benefits include a probe available in powder form, making it flexible to formulate appropriately and dissolve in solvent, which is important for high throughput screening. This fluorescent hPXR probe can also be used by drug companies in their binding assays to replace radioisotope-based binding assay.|
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Last update: August 2013