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 transactivation assay.
Yoshihara
H A
HA
Department of Pharmaceutical Chemistry, University of California, San Francisco, 94143-0446, USA.
Apriletti
J W
JW
Baxter
J D
JD
Scanlan
T S
TS
D000085:Acetates; D001667:Binding, Competitive; D001713:Biphenyl Compounds / Q000737:chemistry* / Q000494:pharmacology; D002264:Carboxylic Acids / Q000737:chemistry* / Q000494:pharmacology; D018360:Crystallography, X-Ray; D015394:Molecular Structure; D010636:Phenols; D011988:Receptors, Thyroid Hormone / Q000037:antagonists & inhibitors* / Q000378:metabolism
D000085:Acetates; D001713:Biphenyl Compounds; D002264:Carboxylic Acids; C413355:GC 1 compound; D010636:Phenols; D011988:Receptors, Thyroid Hormone