Triblock peptide–linker–lipid molecular design improves potency of peptide ligands targeting family B G protein-coupled receptors

2015 ◽  
Vol 51 (28) ◽  
pp. 6157-6160 ◽  
Author(s):  
Yuting Liu ◽  
Yingying Cai ◽  
Wei Liu ◽  
Xiao-Han Li ◽  
Elizabeth Rhoades ◽  
...  
Keyword(s):  
G Protein ◽  
Molecular Design ◽  
G Protein Coupled Receptors ◽  
Peptide Ligands ◽  
G Protein Coupled

Design and characterization of triblock peptide–linker–lipid constructs for targeting family B G protein-couple receptors with improved bioactivity and biostability.

scholarly journals Cell‐free synthesis of isotopically labelled peptide ligands for the functional characterization of G protein‐coupled receptors

FEBS Open Bio ◽  
2015 ◽  
Vol 6 (1) ◽  
pp. 90-102 ◽  
Author(s):  
Lisa Joedicke ◽  
Raphael Trenker ◽  
Julian D. Langer ◽  
Hartmut Michel ◽  
Julia Preu
Keyword(s):  
G Protein ◽  
Functional Characterization ◽  
G Protein Coupled Receptors ◽  
Peptide Ligands ◽  
G Protein Coupled

Proteinase-Activated Receptors: New Functions for Old Enzymes

Physiology ◽  
1998 ◽  
Vol 13 (5) ◽  
pp. 231-240 ◽  
Author(s):  
Stephan K. Böhm ◽  
Karen McConalogue ◽  
Wuyi Kong ◽  
Nigel W. Bunnett
Keyword(s):  
G Protein ◽  
Signaling Molecules ◽  
G Protein Coupled Receptors ◽  
Proteinase Activated Receptors ◽  
Degradative Enzymes ◽  
G Protein Coupled

Although proteases are traditionally viewed as degradative enzymes, characterization of a family of G protein-coupled receptors that are activated by proteolysis reveals a new role. Certain proteases function as signaling molecules that specifically regulate cells by cleaving and activating a family of proteinase-activated receptors.

Structural characterization of the parathyroid hormone receptor domains determinant for ligand binding

2007 ◽  
Vol 35 (4) ◽  
pp. 721-723 ◽  
Author(s):  
D.F. Mierke ◽  
L. Mao ◽  
M. Pellegrini ◽  
A. Piserchio ◽  
J. Plati ◽  
...  
Keyword(s):  
Parathyroid Hormone ◽  
G Protein Coupled Receptors ◽  
Peptide Ligands ◽  
Receptor Complex ◽  
Receptor Model ◽  
Receptor System ◽  
Parathyroid Hormone Receptor ◽  
Contact Points ◽  
G Protein Coupled

Over the years, the association of peptide ligands to Family B GPCRs (G-protein coupled receptors) has been characterized by a number of experimental and theoretical techniques. For the PTH (parathyroid hormone) ligand–receptor system, important insight has been provided by photoaffinity labelling experiments and the elucidation of direct contact points between ligand and receptor. Our research has focused on the structural elucidation of the receptor domains shown to be involved in the binding of PTH. Employing a combination of carefully designed receptor domains, solution-state NMR carried out in the presence of membrane mimetics and extensive computer simulations, we have obtained a well-resolved model of the ligand–receptor complex for PTH. Here, we review the development of this model and highlight some inherent limitations of the methods employed and their consequences on interpretation of the ligand–receptor model.

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