1n46
From Proteopedia
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CRYSTAL STRUCTURE OF HUMAN TR BETA LIGAND-BINDING DOMAIN COMPLEXED WITH A POTENT SUBTYPE-SELECTIVE THYROMIMETIC
Contents |
Overview
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.
Disease
Known diseases associated with this structure: Thyroid hormone resistance OMIM:[190160], Thyroid hormone resistance, autosomal recessive OMIM:[190160]
About this Structure
1N46 is a Single protein structure of sequence from Homo sapiens with as ligand. Full crystallographic information is available from OCA.
Reference
Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TR beta subtype-selective thyromimetics., Dow RL, Schneider SR, Paight ES, Hank RF, Chiang P, Cornelius P, Lee E, Newsome WP, Swick AG, Spitzer J, Hargrove DM, Patterson TA, Pandit J, Chrunyk BA, LeMotte PK, Danley DE, Rosner MH, Ammirati MJ, Simons SP, Schulte GK, Tate BF, DaSilva-Jardine P, Bioorg Med Chem Lett. 2003 Feb 10;13(3):379-82. PMID:12565933
Page seeded by OCA on Thu Feb 21 14:02:07 2008
Categories: Homo sapiens | Single protein | Ammirati, M J. | Chiang, P. | Chrunyk, B A. | Cornelius, P. | DaSilva-Jardine, P. | Danley, D E. | Dow, R L. | Hank, R F. | Hargrove, D M. | LeMotte, P K. | Lee, E. | Newsome, W P. | Paight, E S. | Pandit, J. | Patterson, T A. | Rosner, M H. | Schneider, S R. | Schulte, G K. | Simons, S P. | Spitzer, J. | Swick, A G. | Tate, B F. | PFA | Transcription
