A designed antagonist of the thyroid hormone receptor.

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Yoshihara HA, Apriletti JW, Baxter JD, Scanlan TS

A designed antagonist of the thyroid hormone receptor.

Bioorg Med Chem Lett. 2001 Nov 5;11(21):2821-5.

PubMed ID
11597408 [ View in PubMed
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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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
LiothyronineThyroid hormone receptor alphaKd (nM)0.17N/AN/ADetails
LiothyronineThyroid hormone receptor betaKd (nM)0.14N/AN/ADetails