A designed antagonist of the thyroid hormone receptor

Bioorg Med Chem Lett. 2001 Nov 5;11(21):2821-5. doi: 10.1016/s0960-894x(01)00521-2.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Acetates*
  • Binding, Competitive
  • Biphenyl Compounds / chemistry*
  • Biphenyl Compounds / pharmacology
  • Carboxylic Acids / chemistry*
  • Carboxylic Acids / pharmacology
  • Crystallography, X-Ray
  • Molecular Structure
  • Phenols*
  • Receptors, Thyroid Hormone / antagonists & inhibitors*
  • Receptors, Thyroid Hormone / metabolism

Substances

  • Acetates
  • Biphenyl Compounds
  • Carboxylic Acids
  • GC 1 compound
  • Phenols
  • Receptors, Thyroid Hormone