Allosteric effect of nanobody binding on ligand-specific active states of the β2 adrenergic receptor
Y Chen, O Fleetwood, S Pérez-Conesa… - Journal of Chemical …, 2021 - ACS Publications
Nanobody binding stabilizes G-protein-coupled receptors (GPCR) in a fully active state and
modulates their affinity for bound ligands. However, the atomic-level basis for this allosteric …
modulates their affinity for bound ligands. However, the atomic-level basis for this allosteric …
Luciferase complementation approaches to measure GPCR signaling kinetics and bias
NC Dijon, DN Nesheva, ND Holliday - G Protein-Coupled Receptor …, 2021 - Springer
An understanding of the kinetic contributions to G protein-coupled receptor pharmacology
and signaling is increasingly important in compound profiling. Nonequilibrium conditions are …
and signaling is increasingly important in compound profiling. Nonequilibrium conditions are …
[HTML][HTML] Biased β-agonists favoring Gs over β-arrestin for individualized treatment of obstructive lung disease
Signals from G-protein-coupled receptors (GPCRs) are the most frequently targeted
pathways of currently prescribed therapeutics. Rather than being a simple switch, it is now …
pathways of currently prescribed therapeutics. Rather than being a simple switch, it is now …
Mechanical GPCR Activation by Traction Forces Exerted on Receptor N-Glycans
Cells are sensitive to chemical stimulation which is converted into intracellular biochemical
signals by the activation of specific receptors. Mechanical stimulations can also induce …
signals by the activation of specific receptors. Mechanical stimulations can also induce …
[HTML][HTML] Pharmacology of Antagonism of GPCR
H Kurose, SG Kim - Biological and Pharmaceutical Bulletin, 2022 - jstage.jst.go.jp
Agonists are defined as the ligands that activate intracellular signaling and evoke cellular
responses. Synthetic and endogenous agonists should bind specific amino acids to activate …
responses. Synthetic and endogenous agonists should bind specific amino acids to activate …
[HTML][HTML] Selective Signal Capture from Multidimensional GPCR Outputs with Biased Agonists: Progress Towards Novel Drug Development
G protein coupled receptors (GPCRs) are a superfamily of transmembrane-spanning
receptors that are activated by multiple endogenous ligands and are the most common …
receptors that are activated by multiple endogenous ligands and are the most common …
PRECOG: PREdicting COupling probabilities of G-protein coupled receptors
G-protein coupled receptors (GPCRs) control multiple physiological states by transducing a
multitude of extracellular stimuli into the cell via coupling to intra-cellular heterotrimeric G …
multitude of extracellular stimuli into the cell via coupling to intra-cellular heterotrimeric G …
Kinetic analysis of endogenous β2‐adrenoceptor‐mediated cAMP GloSensor™ responses in HEK293 cells
SA Cullum, DB Veprintsev… - British Journal of …, 2023 - Wiley Online Library
Abstract Background and Aim Standard pharmacological analysis of agonist activity utilises
measurements of receptor‐mediated responses at a set time‐point, or at the peak response …
measurements of receptor‐mediated responses at a set time‐point, or at the peak response …
[HTML][HTML] Intracellular VHHs to monitor and modulate GPCR signaling
P Raynaud, C Gauthier, V Jugnarain… - Frontiers in …, 2022 - frontiersin.org
Single-domain antibody fragments, also known as VHHs or nanobodies, have opened
promising avenues in therapeutics and in exploration of intracellular processes. Because of …
promising avenues in therapeutics and in exploration of intracellular processes. Because of …
Identification of conformation-selective nanobodies against the membrane protein insertase BamA by an integrated structural biology approach
The insertase BamA is an essential protein of the bacterial outer membrane. Its 16-stranded
transmembrane β-barrel contains a lateral gate as a key functional element. This gate is …
transmembrane β-barrel contains a lateral gate as a key functional element. This gate is …