Ligands for orphan nuclear hormone receptor steroidogenic factor-1 (SF-1)
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United States of America Patent
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Issued Date -
Feb 1, 2007
app pub date -
Feb 6, 2006
filing date -
Feb 4, 2005
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Abstract
The 1.5 .ANG. crystal structure of the orphan nuclear receptor steroidogenic factor 1 (SF-1) ligand binding domain in complex with an LxxLL motif from a co-regulator protein is disclosed. The structure reveals the presence of a phospholipid ligand in a surprisingly large pocket (.about.1600 .ANG..sup.3), with the receptor adopting the canonical active conformation. The bound phospholipid is readily exchanged and modulates SF-1 interactions with co-activators. Directed mutations that alter the ligand binding pocket disrupt SF-1/co-activator interactions and reduce SF-1 transcriptional activity. Also disclosed is a method to screen chemical libraries for compounds with high specificity or binding affinity for SF-1, thereby permitting the discovery of agonist or antagonist drugs useful in treating dyslipidemias and/or in promoting cholesterol homeostasis.
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