A designed antagonist of the thyroid hormone receptor

Hikari A.I. Yoshihara; James W. Apriletti; John D. Baxter; Thomas S. Scanlan

doi:10.1016/S0960-894X(01)00521-2

A designed antagonist of the thyroid hormone receptor

Hikari A.I. Yoshihara, James W. Apriletti, John D. Baxter, Thomas S. Scanlan

Physiology & Pharmacology

Research output: Contribution to journal › Article

31 Scopus citations

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 language	English (US)
Pages (from-to)	2821-2825
Number of pages	5
Journal	Bioorganic & medicinal chemistry letters
Volume	11
Issue number	21
DOIs	https://doi.org/10.1016/S0960-894X(01)00521-2
State	Published - Nov 5 2001

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ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Cite this

Yoshihara, H. A. I., Apriletti, J. W., Baxter, J. D., & Scanlan, T. S. (2001). A designed antagonist of the thyroid hormone receptor. Bioorganic & medicinal chemistry letters, 11(21), 2821-2825. https://doi.org/10.1016/S0960-894X(01)00521-2

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Access to Document

10.1016/S0960-894X(01)00521-2