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

Research output: Contribution to journal › Article › peer-review

33 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
Externally published	Yes

ASJC Scopus subject areas

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

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title = "A designed antagonist of the thyroid hormone receptor",

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.",

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AU - Yoshihara, Hikari A.I.

AU - Apriletti, James W.

AU - Baxter, John D.

AU - Scanlan, Thomas S.

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Y1 - 2001/11/5

N2 - 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.

AB - 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.

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JO - Bioorganic and Medicinal Chemistry Letters

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A designed antagonist of the thyroid hormone receptor

Abstract

ASJC Scopus subject areas

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