Small Molecule Agonists of the Orphan Nuclear Receptors Steroidogenic Factor-1 (SF-1, NR5A1) and Liver Receptor Homologue-1 (LRH-1, NR5A2)

The crystal structure of LRH-1 ligand binding domain bound to our previously reported agonist 3-(E-oct-4-en-4-yl)-1-phenylamino-2-phenyl-cis-bicyclo[3.3.0]oct-2-ene 5 is described. Two new classes of agonists in which the bridgehead anilino group from our first series was replaced with an alkoxy or...

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Veröffentlicht in:	Journal of medicinal chemistry 2011-04, Vol.54 (7), p.2266-2281
Hauptverfasser:	Whitby, Richard J, Stec, Jozef, Blind, Raymond D, Dixon, Sally, Leesnitzer, Lisa M, Orband-Miller, Lisa A, Williams, Shawn P, Willson, Timothy M, Xu, Robert, Zuercher, William J, Cai, Fang, Ingraham, Holly A
Format:	Artikel
Sprache:	eng
Schlagworte:	60 APPLIED LIFE SCIENCES Amino Acid Sequence ANIMAL CELLS Animals BASIC BIOLOGICAL SCIENCES CRYSTAL STRUCTURE Crystallography, X-Ray GENES HEK293 Cells Humans Ligands LIVER Mice Models, Molecular Molecular Sequence Data PEPTIDES Protein Conformation Receptors, Cytoplasmic and Nuclear - agonists Receptors, Cytoplasmic and Nuclear - chemistry Receptors, Cytoplasmic and Nuclear - metabolism REGULATIONS Sequence Homology, Amino Acid Small Molecule Libraries - chemical synthesis Small Molecule Libraries - chemistry Small Molecule Libraries - pharmacology Steroidogenic Factor 1 - agonists Steroidogenic Factor 1 - chemistry Steroidogenic Factor 1 - metabolism TARGETS Transcriptional Activation - drug effects
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