Autor: |
Garcia Collazo AM; Karo Bio AB, Novum, Huddinge SE-141 57, Sweden., Koehler KF, Garg N, Färnegårdh M, Husman B, Ye L, Ljunggren J, Mellström K, Sandberg J, Grynfarb M, Ahola H, Malm J |
Jazyk: |
angličtina |
Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 Mar 01; Vol. 16 (5), pp. 1240-4. Date of Electronic Publication: 2005 Dec 09. |
DOI: |
10.1016/j.bmcl.2005.11.077 |
Abstrakt: |
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. |
Databáze: |
MEDLINE |
Externí odkaz: |
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