Emerging paradigms in GPCR allostery: implications for drug discovery
Allosteric ligands bind to G protein-coupled receptors (GPCRs; also known as seven-
transmembrane receptors) at sites that are distinct from the sites to which endogenous …
transmembrane receptors) at sites that are distinct from the sites to which endogenous …
New insights into the structure and function of class B1 GPCRs
G protein–coupled receptors (GPCRs) are the largest family of cell surface receptors. Class
B1 GPCRs constitute a subfamily of 15 receptors that characteristically contain large …
B1 GPCRs constitute a subfamily of 15 receptors that characteristically contain large …
Structural perspective of class B1 GPCR signaling
Class B1 G protein-coupled receptors (GPCRs) play important roles in human physiology
and disease pathology. Using cryo-electron microscopy (cryo-EM) and X-ray …
and disease pathology. Using cryo-electron microscopy (cryo-EM) and X-ray …
The structure and function of the glucagon‐like peptide‐1 receptor and its ligands
D Donnelly - British journal of pharmacology, 2012 - Wiley Online Library
Glucagon‐like peptide‐1 (7‐36) amide (GLP‐1) is a 30‐residue peptide hormone released
from intestinal L cells following nutrient consumption. It potentiates the glucose‐induced …
from intestinal L cells following nutrient consumption. It potentiates the glucose‐induced …
Structures of the human cholecystokinin 1 (CCK1) receptor bound to Gs and Gq mimetic proteins provide insight into mechanisms of G protein selectivity
G protein–coupled receptors (GPCRs) are critical regulators of cellular function acting via
heterotrimeric G proteins as their primary transducers with individual GPCRs capable of …
heterotrimeric G proteins as their primary transducers with individual GPCRs capable of …
Dopamine D2 receptors form higher order oligomers at physiological expression levels
W Guo, E Urizar, M Kralikova, JC Mobarec, L Shi… - The EMBO …, 2008 - embopress.org
G‐protein‐coupled receptors are generally thought to be organized as dimers; whether they
form higher order oligomers is a topic of much controversy. We combined bioluminescence …
form higher order oligomers is a topic of much controversy. We combined bioluminescence …
G protein‐coupled receptor hetero‐dimerization: contribution to pharmacology and function
G Milligan - British journal of pharmacology, 2009 - Wiley Online Library
The concept that G protein‐coupled receptors (GPCRs) can form hetero‐dimers or hetero‐
oligomers continues to gain experimental support. However, with the exception of the …
oligomers continues to gain experimental support. However, with the exception of the …
Structure and dynamics of the active Gs-coupled human secretin receptor
The class B secretin GPCR (SecR) has broad physiological effects, with target potential for
treatment of metabolic and cardiovascular disease. Molecular understanding of SecR …
treatment of metabolic and cardiovascular disease. Molecular understanding of SecR …
The BRET technology and its application to screening assays
The bioluminescence resonance energy transfer (BRET) method is based on resonance
energy transfer between a light‐emitting enzyme and a fluorescent acceptor. Since its first …
energy transfer between a light‐emitting enzyme and a fluorescent acceptor. Since its first …
Allostery and biased agonism at class BG protein-coupled receptors
Class BG protein-coupled receptors (GPCRs) respond to paracrine or endocrine peptide
hormones involved in control of bone homeostasis, glucose regulation, satiety, and gastro …
hormones involved in control of bone homeostasis, glucose regulation, satiety, and gastro …