Profiling of basal and ligand-dependent GPCR activities by means of a polyvalent cell-based high-throughput platform

M Zeghal, G Laroche, JD Freitas, R Wang… - Nature …, 2023 - nature.com
Representing the most attractive and successful druggable receptors of the proteome,
GPCRs regulate a myriad of physiological and pathophysiological functions. Although over …

PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome

WK Kroeze, MF Sassano, XP Huang, K Lansu… - Nature structural & …, 2015 - nature.com
G protein–coupled receptors (GPCRs) are essential mediators of cellular signaling and are
important targets of drug action. Of the approximately 350 nonolfactory human GPCRs, more …

Recent progress in assays for GPCR drug discovery

S Guo, T Zhao, Y Yun, X Xie - American Journal of …, 2022 - journals.physiology.org
G-protein-coupled receptors (GPCRs), also known as seven transmembrane receptors, are
the largest family of cell surface receptors in eukaryotes. There are∼ 800 GPCRs in human …

Tools for GPCR drug discovery

R Zhang, X Xie - Acta Pharmacologica Sinica, 2012 - nature.com
G-protein-coupled receptors (GPCRs) mediate many important physiological functions and
are considered as one of the most successful therapeutic targets for a broad spectrum of …

Direct interrogation of context-dependent GPCR activity with a universal biosensor platform

R Janicot, M Maziarz, JC Park, J Zhao, A Luebbers… - Cell, 2024 - cell.com
G protein-coupled receptors (GPCRs) are the largest family of druggable proteins encoded
in the human genome, but progress in understanding and targeting them is hindered by the …

Selectivity landscape of 100 therapeutically relevant GPCR profiled by an effector translocation-based BRET platform

C Avet, A Mancini, B Breton, C Le Gouill, A Hauser… - 2020 - papers.ssrn.com
The ability of individual G protein-coupled receptors (GPCR) to engage multiple signaling
pathways opens opportunities for the development of better drugs. This requires new …

Pharmacologically targeting intracellular allosteric sites of GPCRs for drug discovery

M Zhang, X Lan, X Li, S Lu - Drug Discovery Today, 2023 - Elsevier
G-protein-coupled receptors (GPCRs) are a family of cell surface proteins that can sense a
variety of extracellular stimuli and mediate multiple signaling transduction pathways …

Receptor-associated independent cAMP nanodomains mediate spatiotemporal specificity of GPCR signaling

SE Anton, C Kayser, I Maiellaro, K Nemec, J Möller… - Cell, 2022 - cell.com
G protein-coupled receptors (GPCRs) relay extracellular stimuli into specific cellular
functions. Cells express many different GPCRs, but all these GPCRs signal to only a few …

Effector membrane translocation biosensors reveal G protein and βarrestin coupling profiles of 100 therapeutically relevant GPCRs

C Avet, A Mancini, B Breton, C Le Gouill, AS Hauser… - Elife, 2022 - elifesciences.org
The recognition that individual GPCRs can activate multiple signaling pathways has raised
the possibility of developing drugs selectively targeting therapeutically relevant ones. This …

Chemical biology of noncanonical G protein–coupled receptor signaling: Toward advanced therapeutics

MM Shchepinova, AC Hanyaloglu, GS Frost… - Current Opinion in …, 2020 - Elsevier
G protein–coupled receptors (GPCRs), the largest family of signaling membrane proteins,
are the target of more than 30% of the drugs on the market. Recently, it has become clear …