甲状腺受体配体。第5部分：对甲状腺激素受体β具有选择性的新型双环激动剂配体。
Thyroid receptor ligands. Part 5: novel bicyclic agonist ligands selective for the thyroid hormone receptor beta.
作者信息
Garcia Collazo Ana-Maria, Koehler Konrad F, Garg Neeraj, Färnegårdh Mathias, Husman Bolette, Ye Liu, Ljunggren Jan, Mellström Karin, Sandberg Johnny, Grynfarb Marlena, Ahola Harri, Malm Johan
机构信息
Karo Bio AB, Novum, Huddinge SE-141 57, Sweden.
出版信息
Bioorg Med Chem Lett. 2006 Mar 1;16(5):1240-4. doi: 10.1016/j.bmcl.2005.11.077. Epub 2005 Dec 9.
Based on the examination of the crystal structure of rat TRbeta complexed with 3,5,3'-triiodo-l-thyronine (2) a novel TRbeta-selective indole derivative 6b was prepared and tested in vitro. This compound was found to be 14 times selective for TRbeta over TRalpha in binding and its beta-selectivity could be rationalized through the comparison of the X-ray crystallographic structures of 6b complexed with TRalpha and TRbeta.
基于对与3,5,3'-三碘-L-甲状腺原氨酸（2）复合的大鼠TRβ晶体结构的研究，制备了一种新型的TRβ选择性吲哚衍生物6b并进行了体外测试。发现该化合物在结合时对TRβ的选择性是TRα的14倍，并且通过比较与TRα和TRβ复合的6b的X射线晶体结构，可以合理地解释其β选择性。
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