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(-) Arctigenin and (+) pinoresinol are antagonists of the human thyroid hormone receptor ?.


ABSTRACT: Lignans are important biologically active dietary polyphenolic compounds. Consumption of foods that are rich in lignans is associated with positive health effects. Using modeling tools to probe the ligand-binding pockets of molecular receptors, we found that lignans have high docking affinity for the human thyroid hormone receptor ?. Follow-up experimental results show that lignans (-) arctigenin and (+) pinoresinol are antagonists of the human thyroid hormone receptor ?. The modeled complexes show key plausible interactions between the two ligands and important amino acid residues of the receptor.

SUBMITTER: Ogungbe IV 

PROVIDER: S-EPMC4245177 | biostudies-literature | 2014 Nov

REPOSITORIES: biostudies-literature

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(-) Arctigenin and (+) pinoresinol are antagonists of the human thyroid hormone receptor β.

Ogungbe Ifedayo Victor IV   Crouch Rebecca A RA   Demeritte Teresa T  

Journal of chemical information and modeling 20141113 11


Lignans are important biologically active dietary polyphenolic compounds. Consumption of foods that are rich in lignans is associated with positive health effects. Using modeling tools to probe the ligand-binding pockets of molecular receptors, we found that lignans have high docking affinity for the human thyroid hormone receptor β. Follow-up experimental results show that lignans (-) arctigenin and (+) pinoresinol are antagonists of the human thyroid hormone receptor β. The modeled complexes s  ...[more]

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