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. Author manuscript; available in PMC: 2013 Sep 1.

Published in final edited form as: ChemMedChem. 2012 Sep;7(9):1551–1566. doi: 10.1002/cmdc.201200319

a) and b). Evaluation of potential RXR selective agonists via a mammalian two-hybrid assay in two different types of human colon cancer cells, Caco-2 (a) and HCT-116 (b), respectively. Both cell lines were transfected with pCMV-BD-hRXR binding domain vector (BD), pCMV-AD-hRXR activation domain (AD), pFR-Luc reporter gene containing BD-binding sites, and a renilla control plasmid. Cells were transfected for 7 hours utilizing a liposome-mediated transfection protocol then exposed to either the ethanol vehicle or 10⁻⁷ M compound 1 or the indicated analog. After 24 hours the cells were lysed and a luciferase assay was completed. Analog-dependent RXR binding and homodimerization, as measured by luciferase output, was compared to the parent compound 1 (value set to 1.0).

a) and b). Evaluation of potential RXR selective agonists via a mammalian two-hybrid assay in two different types of human colon cancer cells, Caco-2 (a) and HCT-116 (b), respectively. Both cell lines were transfected with pCMV-BD-hRXR binding domain vector (BD), pCMV-AD-hRXR activation domain (AD), pFR-Luc reporter gene containing BD-binding sites, and a renilla control plasmid. Cells were transfected for 7 hours utilizing a liposome-mediated transfection protocol then exposed to either the ethanol vehicle or 10⁻⁷ M compound 1 or the indicated analog. After 24 hours the cells were lysed and a luciferase assay was completed. Analog-dependent RXR binding and homodimerization, as measured by luciferase output, was compared to the parent compound 1 (value set to 1.0).