A designed antagonist of the thyroid hormone receptor

A designed antagonist of the thyroid hormone receptor

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 transacti...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2001-11, Vol.11 (21), p.2821-2825
Hauptverfasser: Yoshihara, Hikari A.I., Apriletti, James W., Baxter, John D., Scanlan, Thomas S.
Format: Artikel
Sprache:eng
Schlagworte:
Acetates
Binding, Competitive
Biological and medical sciences
Biphenyl Compounds - chemistry
Biphenyl Compounds - pharmacology
Carboxylic Acids - chemistry
Carboxylic Acids - pharmacology
Crystallography, X-Ray
Hormones. Endocrine system
Medical sciences
Molecular Structure
Pharmacology. Drug treatments
Phenols
Receptors, Thyroid Hormone - antagonists & inhibitors
Receptors, Thyroid Hormone - metabolism
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Zusammenfassung: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. Graphic
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00521-2