scholarly journals Structural Dynamics of Agonist and Antagonist Binding to the Androgen Receptor

2019 ◽  
Vol 123 (36) ◽  
pp. 7657-7666 ◽  
Author(s):  
Ettayapuram Ramaprasad Azhagiya Singam ◽  
Phum Tachachartvanich ◽  
Michele A. La Merrill ◽  
Martyn T. Smith ◽  
Kathleen A. Durkin
Keyword(s):  
Androgen Receptor ◽  
Structural Dynamics ◽  
Agonist And Antagonist ◽  
Antagonist Binding

scholarly journals A Paradigm for Peptide Hormone-GPCR Analyses

Molecules ◽  
2020 ◽  
Vol 25 (18) ◽  
pp. 4272
Author(s):  
Fred Naider ◽  
Jeffrey M. Becker
Keyword(s):  
Conformational Dynamics ◽  
Peptide Hormone ◽  
Yeast Saccharomyces Cerevisiae ◽  
Peptide Analogs ◽  
C Terminus ◽  
Peptide Interactions ◽  
Agonist And Antagonist ◽  
Antagonist Binding ◽  
And Function ◽  
G Protein Coupled

Work from our laboratories over the last 35 years that has focused on Ste2p, a G protein-coupled receptor (GPCR), and its tridecapeptide ligand α-factor is reviewed. Our work utilized the yeast Saccharomyces cerevisiae as a model system for understanding peptide-GPCR interactions. It explored the structure and function of synthetic α-factor analogs and biosynthetic receptor domains, as well as designed mutations of Ste2p. The results and conclusions are described using the nuclear magnetic resonance interrogation of synthetic Ste2p transmembrane domains (TMs), the fluorescence interrogation of agonist and antagonist binding, the biochemical crosslinking of peptide analogs to Ste2p, and the phenotypes of receptor mutants. We identified the ligand-binding domain in Ste2p, the functional assemblies of TMs, unexpected and interesting ligand analogs; gained insights into the bound α-factor structure; and unraveled the function and structures of various Ste2p domains, including the N-terminus, TMs, loops connecting the TMs, and the C-terminus. Our studies showed interactions between specific residues of Ste2p in an active state, but not resting state, and the effect of ligand activation on the dimerization of Ste2p. We show that, using a battery of different biochemical and genetic approaches, deep insight can be gained into the structure and conformational dynamics of GPCR-peptide interactions in the absence of a crystal structure.

scholarly journals Comparative study of agonist and antagonist binding to GABAA receptors in rat brain

1991 ◽  
Vol 55 ◽  
pp. 165
Author(s):  
Yoshihisa Ito ◽  
Kumiko Ishige ◽  
Mizue Makimura ◽  
Hideomi Fukuda ◽  
Yoshie Murakoshi
Keyword(s):  
Comparative Study ◽  
Rat Brain ◽  
Gabaa Receptors ◽  
Agonist And Antagonist ◽  
Antagonist Binding

scholarly journals Distinct Conformations of the Corticotropin Releasing Factor Type 1 Receptor Adopted following Agonist and Antagonist Binding Are Differentially Regulated

2005 ◽  
Vol 280 (12) ◽  
pp. 11560-11568 ◽  
Author(s):  
Stephen J. Perry ◽  
Sachiko Junger ◽  
Trudy A. Kohout ◽  
Sam R.J. Hoare ◽  
R. Scott Struthers ◽  
...  
Keyword(s):  
Corticotropin Releasing Factor ◽  
Agonist And Antagonist ◽  
Antagonist Binding ◽  
Factor Type
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