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 …

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 …

[HTML][HTML] Biased β-agonists favoring Gs over β-arrestin for individualized treatment of obstructive lung disease

A Tokmakova, D Kim, WA Goddard III… - Journal of Personalized …, 2022 - mdpi.com
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 …

Mechanical GPCR Activation by Traction Forces Exerted on Receptor N-Glycans

S Marullo, S Doly, K Saha, H Enslen… - ACS Pharmacology & …, 2020 - ACS Publications
Cells are sensitive to chemical stimulation which is converted into intracellular biochemical
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 …

[HTML][HTML] Selective Signal Capture from Multidimensional GPCR Outputs with Biased Agonists: Progress Towards Novel Drug Development

D Kim, A Tokmakova, JAA Woo, SS An… - Molecular Diagnosis & …, 2022 - Springer
G protein coupled receptors (GPCRs) are a superfamily of transmembrane-spanning
receptors that are activated by multiple endogenous ligands and are the most common …

PRECOG: PREdicting COupling probabilities of G-protein coupled receptors

G Singh, A Inoue, JS Gutkind, RB Russell… - Nucleic Acids …, 2019 - academic.oup.com
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 …

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 …

[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 …

Identification of conformation-selective nanobodies against the membrane protein insertase BamA by an integrated structural biology approach

H Kaur, JB Hartmann, RP Jakob, M Zahn… - Journal of biomolecular …, 2019 - Springer
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 …