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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 

Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TR beta subtype-selective thyromimetics.

In this communication, we wish to describe the discovery of a novel series of 6-azauracil-based thyromimetics that possess up to 100-fold selectivities for binding and functional activation of the beta(1)-isoform of the thyroid receptor family. Structure-activity relationship studies on the 3,5- and 3'-positions provided compounds with enhanced TR beta affinity and selectivity. Key binding interactions between the 6-azauracil moiety and the receptor have been determined through of X-ray crystallographic analysis.[1]

References

  1. Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TR beta subtype-selective thyromimetics. Dow, R.L., Schneider, S.R., Paight, E.S., Hank, R.F., Chiang, P., Cornelius, P., Lee, E., Newsome, W.P., Swick, A.G., Spitzer, J., Hargrove, D.M., Patterson, T.A., Pandit, J., Chrunyk, B.A., LeMotte, P.K., Danley, D.E., Rosner, M.H., Ammirati, M.J., Simons, S.P., Schulte, G.K., Tate, B.F., DaSilva-Jardine, P. Bioorg. Med. Chem. Lett. (2003) [Pubmed]
 
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