Role of ligands for allosteric network of nuclear receptors

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Active vitamin D derivatives with 22-butyl substituent were found to be a new class of agonists and antagonists inducing the different pocket structure of the vitamin D receptor. Next, we synthesized vitamin D derivatives with 22-alkyl substituent and performed their SAR study. Then we tried X-ray crystallographic analysis of the complex of vitamin D receptor and ligand with particular activity. These results indicate that a ligand determines position of helix 12 via allosteric network and consequently expresses its particular activity.