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    J Med Chem. 2007 Nov 1;50(22):5269-80. Epub 2007 Oct 5.

    Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships.

    Arnold LA, Kosinski A, Estébanez-Perpiñá E, Fletterick RJ, Guy RK.

    Source

    Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, 332 N. Lauderdale, Memphis, Tennessee 38105, USA.

    Abstract

    The modulation of gene regulation by blocking the interaction between the thyroid receptor (TR) and obligate coregulators has been reported recently with the discovery of the lead compound 3-(dimethylamino)-1-(4-hexylphenyl)propan-1-one). Herein we report studies aimed at optimization of this initial hit to determine the basic parameters of the structure-activity relationships and clarify the mechanism of action. These studies provided new insights, showing that activity and TRbeta isoform selectivity is highly correlated with the structural composition of these covalent inhibitors.

    PMID:
    17918822
    [PubMed - indexed for MEDLINE]
    PMCID:
    PMC2536611
    Free PMC Article

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