The context-dependent mechanisms by which GPCRs translate extracellular cues into intracellular signals through ligand recognition, ligand-induced conformational changes, engagement with different adaptors and interactions with various molecular pathways, as well as how these processes are modulated during disease, are highlighted and the new therapeutic opportunities they present.
The rapid increase in experimentally resolved G protein-coupled receptor (GPCR)–biologic complexes has substantially improved our understanding of the molecular basis of receptor recognition and modulation. However, despite the growing number of available structures, a comparative framework integrating the major GPCR c...
G-protein-coupled receptors (GPCRs) constitute the largest family of membrane proteins involved in cellular signaling. Although X-ray crystallography and cryo-Electron Microscopy (cryo-EM) have provided valuable structural insights into GPCRs, these experimental techniques primarily capture static conformations and can...
Keya Joshi, V. Adediwura, Ying-Long Miao· Frontiers in Chemical Biolog...· 0 citations
Structural and functional studies of arrestins have revealed their essential role as multifunctional regulators of G protein-coupled receptor (GPCR) signaling, desensitization, and trafficking. Despite significant challenges in capturing the dynamic nature of GPCR-arrestin interactions, great progress has been made in...
V. Gupta, A. Beck-Sickinger· The FEBS Journal· 0 citations
G-protein-coupled receptors (GPCRs) represent the largest superfamily of membrane-bound receptors in the human organism and are involved in the regulation of numerous physiological processes in almost all organ systems. Characterized by seven transmembrane domains and coupling to heterotrimeric G-proteins, they mediate...
Ronja Zwerenz, P. Lakatos, Merle Flecks et al.· International Journal of Mol...· 0 citations
A novel strategy for functional GPCR antagonism via bispecific antibody-mediated endocytosis and lysosomal degradation is reported via bispecific antibody-mediated endocytosis and lysosomal degradation, establishing induced endocytosis and rewiring protein trafficking as a new paradigm for therapeutic GPCR modulation.
Kaitlin Rhee, L. Shue, Akimasa Adachi et al.· Nature· 2 citations
G protein-coupled receptors (GPCRs) govern diverse cellular responses and are crucial drug targets. However, the sequence of structural events from G protein recognition to GDP release has remained elusive. Here, we leveraged the viral chemokine GPCR US28 to capture multiple activation states of the US28-Gq complex. Us...
K. Jude, Carl-Mikael Suomivuori, Deepa Waghray et al.· Nature Communications· 0 citations
We use cookies to run the site and, with your consent, for analytics and to show ads.
See our Cookie Policy.
