Author/Authors :
Ana Maria Garcia Collazo، نويسنده , , Konrad F. Koehler، نويسنده , , Neeraj Garg، نويسنده , , Mathias F?rneg?rdh، نويسنده , , Bolette Husman، نويسنده , , Liu Ye، نويسنده , , Jan Ljunggren، نويسنده , , Karin Mellstr?m، نويسنده , , Johnny Sandberg، نويسنده , , Marlena Grynfarb، نويسنده , , Harri Ahola، نويسنده , , Johan Malm، نويسنده ,
Abstract :
Based on the examination of the crystal structure of rat TRβ complexed with 3,5,3′-triiodo-l-thyronine (2) a novel TRβ-selective indole derivative 6b was prepared and tested in vitro. This compound was found to be 14 times selective for TRβ over TRα in binding and its β-selectivity could be rationalized through the comparison of the X-ray crystallographic structures of 6b complexed with TRα and TRβ.
Keywords :
TR?-selectivity , Thyroid hormone receptor agonist , Quinoline , x-ray , Indole , Indane
