G protein–coupled receptor signaling: new insights define cellular nanodomains

MJ Lohse, A Bock, M Zaccolo - Annual Review of Pharmacology …, 2024 - annualreviews.org
G protein–coupled receptors are the largest and pharmacologically most important receptor
family and are involved in the regulation of most cell functions. Most of them reside …

Determination of G-protein–coupled receptor oligomerization by molecular brightness analyses in single cells

A Işbilir, R Serfling, J Möller, R Thomas, C De Faveri… - Nature …, 2021 - nature.com
Oligomerization of membrane proteins has received intense research interest because of
their importance in cellular signaling and the large pharmacological and clinical potential …

Biased signaling due to oligomerization of the G protein-coupled platelet-activating factor receptor

J Liu, H Tang, C Xu, S Zhou, X Zhu, Y Li… - Nature …, 2022 - nature.com
G protein-coupled receptors (GPCRs) are important drug targets that mediate various
signaling pathways by activating G proteins and engaging β-arrestin proteins. Despite its …

Structural insight into apelin receptor-G protein stoichiometry

Y Yue, L Liu, LJ Wu, Y Wu, L Wang, F Li, J Liu… - Nature Structural & …, 2022 - nature.com
The technique of cryogenic-electron microscopy (cryo-EM) has revolutionized the field of
membrane protein structure and function with a focus on the dominantly observed molecular …

Structural basis of dimerization of chemokine receptors CCR5 and CXCR4

D Di Marino, P Conflitti, S Motta, V Limongelli - Nature communications, 2023 - nature.com
G protein-coupled receptors (GPCRs) are prominent drug targets responsible for
extracellular-to-intracellular signal transduction. GPCRs can form functional dimers that …

CXCL17 is an allosteric inhibitor of CXCR4 through a mechanism of action involving glycosaminoglycans

CW White, S Platt, LE Kilpatrick, N Dale… - Science …, 2024 - science.org
CXCL17 is a chemokine principally expressed by mucosal tissues, where it facilitates
chemotaxis of monocytes, dendritic cells, and macrophages and has antimicrobial …

The β2-adrenergic receptor associates with CXCR4 multimers in human cancer cells

J Liang, M Seghiri, PK Singh, HG Seo… - Proceedings of the …, 2024 - National Acad Sciences
While the existence and functional role of class C G-protein-coupled receptors (GPCR)
dimers is well established, there is still a lack of consensus regarding class A and B GPCR …

Visualization of β-adrenergic receptor dynamics and differential localization in cardiomyocytes

M Bathe-Peters, P Gmach, HH Boltz… - Proceedings of the …, 2021 - National Acad Sciences
A key question in receptor signaling is how specificity is realized, particularly when different
receptors trigger the same biochemical pathway (s). A notable case is the two β‐adrenergic …

A Versatile Sub-Nanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine H3 Receptor

N Rosier, L Grätz, H Schihada, J Möller… - Journal of Medicinal …, 2021 - ACS Publications
The histamine H3 receptor (H3R) is considered an attractive drug target for various
neurological diseases. We here report the synthesis of UR-NR266, a novel fluorescent H3R …

Nonblinking carbon dots for imaging and tracking receptors on a live cell membrane

Q Wang, Z Feng, H He, X Hu, J Mao, X Chen… - Chemical …, 2021 - pubs.rsc.org
Blinking occurs with nearly all fluorophores including organic dyes, fluorescent proteins,
semiconductor quantum dots and carbon dots (CDs). We developed non-blinking and …