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A structural role for hormone in the thyroid hormone receptor

Nature volume 378, pages 690–697 (1995)Cite this article

Abstract

The crystal structure of the rat aα thyroid hormone receptor ligand-binding domain bound with a thyroid hormone agonist reveals that ligand is completely buried within the domain as part of the hydrophobic core. In addition, the carboxy-terminal activation domain forms an amphi-pathic helix, with its hydrophobic face constituting part of the hormone binding cavity. These observations suggest a structural role for ligand, in establishing the active conformation of the receptor, that is likely to underlie hormonal regulation of gene expression for the nuclear receptors.

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Author information

Authors and Affiliations

  1. Graduate Group in Biophysics, University of California at San Francisco, San Francisco, California, 94143-0448, USA

    Richard L. Wagner

  2. Metabolic Research Unit, University of California at San Francisco, San Francisco, California, 94143-0448, USA

    James W. Apriletti, Brian L. West & John D. Baxter

  3. Department of Medicine, University of California at San Francisco, San Francisco, California, 94143-0448, USA

    John D. Baxter

  4. Department of Biochemistry and Biophysics, University of California at San Francisco, San Francisco, California, 94143-0448, USA

    Robert J. Fletterick

  5. Khepri Pharmaceutical, Inc., 260 Little Field Avenue, South San Francisco, California, 94080, USA

    Mary E. McGrath

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  1. Richard L. Wagner
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  2. James W. Apriletti
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  4. Brian L. West
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  5. John D. Baxter
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Wagner, R., Apriletti, J., McGrath, M. et al. A structural role for hormone in the thyroid hormone receptor. Nature 378, 690–697 (1995). https://doi.org/10.1038/378690a0

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