A designed antagonist of the thyroid hormone receptor.

H. A. Yoshihara, J. W. Apriletti, J. D. Baxter, Thomas (Tom) Scanlan

Research output: Contribution to journalArticle

30 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)2821-2825
Number of pages5
JournalBioorganic & medicinal chemistry letters
Volume11
Issue number21
StatePublished - Nov 5 2001
Externally publishedYes

Fingerprint

Thyroid Hormone Receptors
Bearings (structural)
Transcriptional Activation
Assays
GC 1 compound
Estrogen Receptor Antagonists
ICI 164384

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Yoshihara, H. A., Apriletti, J. W., Baxter, J. D., & Scanlan, T. T. (2001). A designed antagonist of the thyroid hormone receptor. Bioorganic & medicinal chemistry letters, 11(21), 2821-2825.

A designed antagonist of the thyroid hormone receptor. / Yoshihara, H. A.; Apriletti, J. W.; Baxter, J. D.; Scanlan, Thomas (Tom).

In: Bioorganic & medicinal chemistry letters, Vol. 11, No. 21, 05.11.2001, p. 2821-2825.

Research output: Contribution to journalArticle

Yoshihara, HA, Apriletti, JW, Baxter, JD & Scanlan, TT 2001, 'A designed antagonist of the thyroid hormone receptor.', Bioorganic & medicinal chemistry letters, vol. 11, no. 21, pp. 2821-2825.
Yoshihara, H. A. ; Apriletti, J. W. ; Baxter, J. D. ; Scanlan, Thomas (Tom). / A designed antagonist of the thyroid hormone receptor. In: Bioorganic & medicinal chemistry letters. 2001 ; Vol. 11, No. 21. pp. 2821-2825.
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