GPCR biosensors to study conformational dynamics and signaling in drug discovery

VR Saca, C Burdette, TP Sakmar - Annual Review of …, 2024 - annualreviews.org
G protein–coupled receptors (GPCRs) are a superfamily of transmembrane signal
transducers that facilitate the flow of chemical signals across membranes. GPCRs are a …

G protein-coupled receptor (GPCR) pharmacogenomics

MD Thompson, D Reiner-Link, A Berghella… - Critical Reviews in …, 2024 - Taylor & Francis
The field of pharmacogenetics, the investigation of the influence of one or more sequence
variants on drug response phenotypes, is a special case of pharmacogenomics, a discipline …

Get ready to sharpen your tools: A short guide to heterotrimeric G protein activity biosensors

R Janicot, M Garcia-Marcos - Molecular Pharmacology, 2024 - Elsevier
ABSTRACT G protein-coupled receptors (GPCRs) are the largest class of transmembrane
receptors encoded in the human genome, and they initiate cellular responses triggered by a …

[HTML][HTML] Genome-wide pan-GPCR cell libraries accelerate drug discovery

H Yang, Y Wang, W Liu, T He, J Liao, Z Qian… - … Pharmaceutica Sinica B, 2024 - Elsevier
G protein-coupled receptors (GPCRs) are pivotal in mediating diverse physiological and
pathological processes, rendering them promising targets for drug discovery. GPCRs …

Emerging modes of regulation of neuromodulatory G protein-coupled receptors

AJ Gonzalez-Hernandez, H Munguba, J Levitz - Trends in Neurosciences, 2024 - cell.com
In the nervous system, G protein-coupled receptors (GPCRs) control neuronal excitability,
synaptic transmission, synaptic plasticity, and, ultimately, behavior through spatiotemporally …

[PDF][PDF] Advances in GPCRs: structure, mechanisms, disease, and pharmacology

Z Cai, W Kong - American Journal of Physiology-Cell …, 2024 - journals.physiology.org
G protein-coupled receptors (GPCRs) represent the largest family of cell membrane 10
receptors, encompassing over 800 members in humans. These receptors play a pivotal role …

Quantitative approaches for studying G protein-coupled receptor signalling and pharmacology

A Pearce, T Redfern-Nichols, E Wills… - Journal of Cell …, 2025 - journals.biologists.com
ABSTRACT G protein-coupled receptor (GPCR) signalling pathways underlie numerous
physiological processes, are implicated in many diseases and are major targets for …

ONE-GO: Direct detection of context-dependent GPCR activity

A Raskovalov, D Kim, V Cherezov - Cell Research, 2024 - nature.com
G protein-coupled receptors (GPCRs) represent some of the most important drug targets in
the human genome, however, our understanding of these receptors has primarily been …

Phenotypic drug discovery: a case for thymosin alpha-1

E Garaci, M Paci, C Matteucci, C Costantini… - Frontiers in …, 2024 - frontiersin.org
Phenotypic drug discovery (PDD) involves screening compounds for their effects on cells,
tissues, or whole organisms without necessarily understanding the underlying molecular …

[HTML][HTML] Application of FRET-and BRET-based live-cell biosensors in deorphanization and ligand discovery studies on orphan G protein-coupled receptors

JJ Sajkowska, CH Tsang, P Kozielewicz - SLAS Discovery, 2024 - Elsevier
Bioluminescence-and fluorescence-based resonance energy transfer assays have gained
considerable attention in pharmacological research as high-throughput scalable tools …