Characterization of Calmodulin Binding to the Orphan Nuclear Receptor ERRγ

2003 ◽  
Vol 384 (3) ◽  
Author(s):  
M. Hentschke ◽  
C. Schulze ◽  
U. Süsens ◽  
U. Borgmeyer
Keyword(s):  
Nuclear Receptor ◽  
Orphan Nuclear Receptor ◽  
Calmodulin Binding

scholarly journals Molecular cloning and characterization of chicken orphan nuclear receptor cTR21

2003 ◽  
Vol 132 (3) ◽  
pp. 474-484 ◽  
Author(s):  
Sabyasachi Sanyal ◽  
Chirstoph Handschin ◽  
Michael Podvinec ◽  
Kwang-Hoon Song ◽  
Han-Jong Kim ◽  
...  
Keyword(s):  
Molecular Cloning ◽  
Nuclear Receptor ◽  
Orphan Nuclear Receptor

scholarly journals Functional characterization of an orphan nuclear receptor, Rev-ErbAα, in chondrocytes and its potential role in osteoarthritis

2006 ◽  
Vol 54 (11) ◽  
pp. 3513-3522 ◽  
Author(s):  
P. Chaturvedi ◽  
M. Pratta ◽  
K. Steplewski ◽  
J. Connor ◽  
S. Kumar
Keyword(s):  
Nuclear Receptor ◽  
Potential Role ◽  
Functional Characterization ◽  
Orphan Nuclear Receptor

scholarly journals Characterization of the Promoter of SF-1, an Orphan Nuclear Receptor Required for Adrenal and Gonadal Development

1997 ◽  
Vol 11 (2) ◽  
pp. 117-126 ◽  
Author(s):  
Karen G. Woodson ◽  
Peter A. Crawford ◽  
Yoel Sadovsky ◽  
Jeffrey Milbrandt
Keyword(s):  
Nuclear Receptor ◽  
Gonadal Development ◽  
Orphan Nuclear Receptor

scholarly journals HDX-MS reveals structural determinants for RORγ hyperactivation by synthetic agonists

2019 ◽  
Author(s):  
Timothy S. Strutzenberg ◽  
Ruben Garcia-Ordonez ◽  
Scott Novick ◽  
HaJeung Park ◽  
Mi Ra Chang ◽  
...  
Keyword(s):  
Nuclear Receptor ◽  
Receptor Activation ◽  
Site Directed Mutagenesis ◽  
Orphan Nuclear Receptor ◽  
Chemical Probes ◽  
Structural Determinants ◽  
Synthetic Ligand ◽  
Hdx Ms

ABSTRACTMembers of the nuclear receptor (NR) superfamily regulate both physiological and pathophysiological processes ranging from development and metabolism1 to inflammation2 and cancer3. As ligand-gated transcription factors, synthetic small molecules targeting NRs are often deployed as therapeutics to correct aberrant NR signaling or as chemical probes to explore the role of the receptor in physiology4. However, nearly half of NRs do not have specific cognate ligands or its unclear if they possess ligand dependent activities and these receptors are called orphans. Here we demonstrate that ligand-dependent action of the orphan nuclear receptor RORγ can be defined by selectively disrupting putative endogenous—but not synthetic—ligand binding. Furthermore, the characterization of a library of RORγ modulators reveals that structural dynamics of the receptor assessed by HDX-MS correlate with activity in biochemical and cell-based assays. These findings are corroborated with X-ray co-crystallography and site-directed mutagenesis to collectively reveal the structural determinants of RORγ ligand-dependent activation, critical for designing full agonists for application in cancer immunotherapy. Combined these observations support a model of receptor activation to more accurately describe RORγ pharmacology. Likewise, this ‘bump-and-hole’ inspired approach could be extended to other orphan NRs to explore the ligand-dependent activities that are important for defining pharmacology.

Expression, purification, and initial structural characterization of rat orphan nuclear receptor NOR-1 LBD domain

2004 ◽  
Vol 37 (2) ◽  
pp. 443-449 ◽  
Author(s):  
Guilherme Razzera ◽  
Javier Vernal ◽  
Rodrigo V. Portugal ◽  
Marcos R. Calgaro ◽  
Pablo Fernandez ◽  
...  
Keyword(s):  
Nuclear Receptor ◽  
Structural Characterization ◽  
Orphan Nuclear Receptor
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