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Structure. 2012 Jan 11;20(1):2-4. doi: 10.1016/j.str.2011.12.002.

Couple dynamics: PPARγ and its ligand partners.

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VARI-SIMM Center, Center for Structure and Function of Drug Targets, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, People's Republic of China.


Ligand-regulated transcriptional activity is the most important property of nuclear receptors, including PPARγ. In this issue of Structure, Hughes et al. determined how the dynamic conformations of ligands and the receptor contribute to the degree of ligand-dependent activation of PPARγ, which provide further insights into design of PPARγ-based anti-diabetic drugs.

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