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Scientific Report 2007

Scripps Florida

Molecular Therapeutics

Ribbon diagram of the ligand-binding domain of peroxisome proliferator-activated receptor γ (PPARγ) overlaid with differential hydrogen-deuterium exchange data. Ligand density is displayed as a surface representation. The 4 ligand-receptor complexes are PPAR ± MRL-20 (full agonist; A), MRL-24 (partial agonist; B), nTZDpa (partial agonist; C), and BVT.13 (intermediate agonist; D). The degree of stabilization of receptor dynamics as determined by hydrogen-deuterium exchange is shown in color; dark blue indicates the largest magnitude of stabilization. Cocrystal structures were obtained by John Bruning, Ph.D. Hydrogen-deuterium exchange data was obtained by Michael Chalmers, Ph.D., who also generated the figure. These data refute the previous model of for ligand activation of PPAR, in which H12 alone acts as the molecular switch, and suggest a secondary coactivator epitope in the β-sheet region of the receptor. Work done in the laboratory of Pat Griffin, Ph.D., professor.


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