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Figure 1
Crystal structures of PPAR LBD–TIPP complexes. (a) Chemical formulae of TIPP-703, TIPP-401 and TIPP-204. The numbers indicate the EC50 (nM), the molar concentration of the compounds that affords 50% of the maximal reporter activity, in our PPAR-GAL4 chimeric reporter assays using transiently transfected HEK-293 cells (Kasuga et al., 2006BB18). Values in parentheses indicate the activities of the antipodal (R) isomers of TIPP-703 and TIPP-401. For the structures of the four complexes determined in this study, the columns in the table are coloured cyan (PPARα LBD–TIPP-703), green (PPARγ LBD–TIPP-703), orange (PPARδ LBD–TIPP-401) and magenta (PPARδ LBD–TIPP-204). This colouring is used throughout the manuscript. (b) Overall structures of the complexes. Proteins are represented as ribbon models and the ligands are depicted as space-filling models, with F, C, N and O atoms in aqua, yellow, blue and red, respectively.

Journal logoBIOLOGICAL
CRYSTALLOGRAPHY
ISSN: 1399-0047
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