4.5 Article

A designed antagonist of the thyroid hormone receptor

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 11, Issue 21, Pages 2821-2825

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(01)00521-2

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Funding

  1. NCI NIH HHS [T32 CA09270] Funding Source: Medline
  2. NIDDK NIH HHS [DK52798] Funding Source: Medline

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We synthesized an analogue of the thyromimetic GC-1 bearing the same hydrophobic appendage as the estrogen receptor antagonist ICI-164,384. While having reduced affinity for the thyroid hormone receptors compared to GC-1, it behaves in a manner consistent with a competitive antagonist in a transactivation assay. (C) 2001 Elsevier Science Ltd. All rights reserved.

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