Synthesis and preliminary analysis of a P-glycoprotein-specific [3H]-benzophenone photoaffinity label based on (-)-stipiamide |
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| Authors: | Andrus M B Turner T M Sauna Z E Ambudkar S V |
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| Affiliation: | Brigham Young University, Department of Chemistry and Biochemistry, Provo, UT 84602-5700, USA. mbandrus@chemdept.byu.edu |
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| Abstract: | A benzophenone photoaffinity label 9 based on the polyene natural product (-)-stipiamide has been constructed using a diaminoethane spacer and the radioactive agent [3H]-BZDC (N-succinimidyl p-benzoyl-(2,3-3H)-dehydrocinnamate). Photoaffinity experiments show specific binding to human P-glycoprotein (Pgp) in the presence of cis-flupentixol but not with cyclosporin A. |
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