1168136-35-3Relevant academic research and scientific papers
Selective chemical rescue of a thyroid-hormone-receptor mutant, TRβ(H435Y), identified in pituitary carcinoma and resistance to thyroid hormone
Hassan, A. Quamrul,Koh, John T.
supporting information; experimental part, p. 7280 - 7283 (2009/04/20)
(Figure Presented) Ligand to the rescue! Thyroid hormone receptor (TR) plays a critical role in development and homeostasis. The mutant TRβ(H435Y) was identified in both cancer and resistance to thyroid hormone. A designed synthetic ligand recovered the cellular reporter-gene activity of TRβ(H435Y) with a 5850-fold improvement in selectivity for the mutant relative to that of the natural hormone T3 (shown in a modeled structure with TRβ-(H435Y)).
