A designed antagonist of the thyroid hormone receptor

Citation
Hai. Yoshihara et al., A designed antagonist of the thyroid hormone receptor, BIOORG MED, 11(21), 2001, pp. 2821-2825
Citations number
25
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
21
Year of publication
2001
Pages
2821 - 2825
Database
ISI
SICI code
0960-894X(20011105)11:21<2821:ADAOTT>2.0.ZU;2-L
Abstract
We synthesized an analogue of the thyromimetic GC-1 bearing the same hydrop hobic appendage as the estrogen receptor antagonist ICI-164,384. While havi ng reduced affinity for the thyroid hormone receptors compared to GC-1, it behaves in a manner consistent with a competitive antagonist in a transacti vation assay. (C) 2001 Elsevier Science Ltd. All rights reserved.