Allosteric modulators of rhodopsin-like G protein-coupled receptors: Opportunities in drug development

2012 ◽  
Vol 135 (3) ◽  
pp. 292-315 ◽  
Author(s):  
Christa E. Müller ◽  
Anke C. Schiedel ◽  
Younis Baqi
Keyword(s):  
Drug Development ◽  
G Protein ◽  
G Protein Coupled Receptors ◽  
Allosteric Modulators ◽  
G Protein Coupled

Virally Encoded G Protein-Coupled Receptors: Targets for Potentially Innovative Anti-Viral Drug Development

2003 ◽  
Vol 4 (5) ◽  
pp. 431-441 ◽  
Author(s):  
J. Smit ◽  
C. Vink ◽  
D. Verzijl ◽  
P. Casarosa ◽  
A. Bruggeman ◽  
...  
Keyword(s):  
Drug Development ◽  
G Protein ◽  
G Protein Coupled Receptors ◽  
Virally Encoded ◽  
G Protein Coupled

Structural insights into RAMP modification of secretin family G protein-coupled receptors: implications for drug development

2011 ◽  
Vol 32 (10) ◽  
pp. 591-600 ◽  
Author(s):  
Julia K. Archbold ◽  
Jack U. Flanagan ◽  
Harriet A. Watkins ◽  
Joseph J. Gingell ◽  
Debbie L. Hay
Keyword(s):  
Drug Development ◽  
G Protein ◽  
G Protein Coupled Receptors ◽  
G Protein Coupled ◽  
Structural Insights

G-protein-coupled receptor allosterism: the promise and the problem(s)

2004 ◽  
Vol 32 (5) ◽  
pp. 873-877 ◽  
Author(s):  
A. Christopoulos ◽  
L.T. May ◽  
V.A. Avlani ◽  
P.M. Sexton
Keyword(s):  
G Protein ◽  
Binding Sites ◽  
G Protein Coupled Receptors ◽  
Receptor Activity ◽  
Screening Methods ◽  
Receptor Subtype ◽  
Allosteric Modulators ◽  
Physiological Regulation ◽  
Subtype Selectivity ◽  
G Protein Coupled

Allosteric modulators of G-protein-coupled receptors interact with binding sites that are topographically distinct from the orthosteric site recognized by the receptor's endogenous agonist. Allosteric ligands offer a number of advantages over orthosteric drugs, including the potential for greater receptor subtype selectivity and a more ‘physiological’ regulation of receptor activity. However, the manifestations of allosterism at G-protein-coupled receptors are quite varied, and significant challenges remain for the optimization of screening methods to ensure the routine detection and validation of allosteric ligands.

Endogenous Allosteric Modulators of G Protein–Coupled Receptors

2015 ◽  
Vol 353 (2) ◽  
pp. 246-260 ◽  
Author(s):  
Emma T. van der Westhuizen ◽  
Celine Valant ◽  
Patrick M. Sexton ◽  
Arthur Christopoulos
Keyword(s):  
G Protein ◽  
G Protein Coupled Receptors ◽  
Allosteric Modulators ◽  
G Protein Coupled
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