scholarly journals Nuclear Receptor Modulators — Current Approaches and Future Perspectives

10.5772/59666 ◽  
2015 ◽  
Author(s):  
Thales Kronenberger ◽  
Oliver Keminer ◽  
Carsten Wrenger ◽  
Björn Windshügel
Keyword(s):  
Nuclear Receptor ◽  
Future Perspectives ◽  
Receptor Modulators

scholarly journals The Therapeutic Potential of Nuclear Receptor Modulators for Treatment of Metabolic Disorders: PPARγ, RORs, and Rev-erbs

2014 ◽  
Vol 19 (2) ◽  
pp. 193-208 ◽  
Author(s):  
David P. Marciano ◽  
Mi Ra Chang ◽  
Cesar A. Corzo ◽  
Devrishi Goswami ◽  
Vinh Q. Lam ◽  
...  
Keyword(s):  
Nuclear Receptor ◽  
Metabolic Disorders ◽  
Therapeutic Potential ◽  
Receptor Modulators

A CNS-Targeting Prodrug Strategy for Nuclear Receptor Modulators

2020 ◽  
Vol 63 (17) ◽  
pp. 9742-9751 ◽  
Author(s):  
Skylar J. Ferrara ◽  
Thomas S. Scanlan
Keyword(s):  
Nuclear Receptor ◽  
Receptor Modulators ◽  
Cns Targeting

Orphan Nuclear Receptor Modulators

2003 ◽  
Vol 3 (14) ◽  
pp. 1637-1647 ◽  
Author(s):  
Raju Mohan ◽  
Richard Heyman
Keyword(s):  
Nuclear Receptor ◽  
Orphan Nuclear Receptor ◽  
Receptor Modulators

Design of selective nuclear receptor modulators: RAR and RXR as a case study

2007 ◽  
Vol 6 (10) ◽  
pp. 811-820 ◽  
Author(s):  
Angel R. de Lera ◽  
William Bourguet ◽  
Lucia Altucci ◽  
Hinrich Gronemeyer
Keyword(s):  
Nuclear Receptor ◽  
Receptor Modulators

scholarly journals Coregulator Function: A Key to Understanding Tissue Specificity of Selective Receptor Modulators

2004 ◽  
Vol 25 (1) ◽  
pp. 45-71 ◽  
Author(s):  
Carolyn L. Smith ◽  
Bert W. O’Malley
Keyword(s):  
Estrogen Receptor ◽  
Nuclear Receptors ◽  
Nuclear Receptor ◽  
Critical Role ◽  
Dependent Manner ◽  
Nuclear Receptor Superfamily ◽  
Binding Domains ◽  
Receptor Modulator ◽  
Cellular Environment ◽  
Receptor Modulators

Ligands for the nuclear receptor superfamily control many aspects of biology, including development, reproduction, and homeostasis, through regulation of the transcriptional activity of their cognate receptors. Selective receptor modulators (SRMs) are receptor ligands that exhibit agonistic or antagonistic biocharacter in a cell- and tissue context-dependent manner. The prototypical SRM is tamoxifen, which as a selective estrogen receptor modulator, can activate or inhibit estrogen receptor action. SRM-induced alterations in the conformation of the ligand-binding domains of nuclear receptors influence their abilities to interact with other proteins, such as coactivators and corepressors. It has been postulated, therefore, that the relative balance of coactivator and corepressor expression within a given target cell determines the relative agonist vs. antagonist activity of SRMs. However, recent evidence reveals that the cellular environment also plays a critical role in determining SRM biocharacter. Cellular signaling influences the activity and subcellular localization of coactivators and corepressors as well as nuclear receptors, and this contributes to gene-, cell-, and tissue-specific responses to SRM ligands. Increased understanding of the effect of cellular environment on nuclear receptors and their coregulators has the potential to open the field of SRM discovery and research to many members of the nuclear receptor superfamily.

Panning for SNuRMs: using cofactor profiling for the rational discovery of selective nuclear receptor modulators

2007 ◽  
Vol 12 (19-20) ◽  
pp. 860-869 ◽  
Author(s):  
Claus Kremoser ◽  
Michael Albers ◽  
Thomas P. Burris ◽  
Ulrich Deuschle ◽  
Manfred Koegl
Keyword(s):  
Nuclear Receptor ◽  
Receptor Modulators
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