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A designed antagonist of the thyroid hormone receptor
H A Yoshihara1, J W Apriletti, J D Baxter
1Department of Pharmaceutical Chemistry, University of California, San Francisco, 94143-0446, USA.
Bioorganic & Medicinal Chemistry Letters
|October 13, 2001
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.