Ligands and Beyond: Mechanosensitive Adhesion GPCRs
, 2022 Cells respond to diverse types of mechanical stimuli using a wide range of plasma membrane-associated mechanosensitive receptors to convert extracellular mechanical cues into intracellular signaling.
Hsi-Hsien Lin +3 more
core +1 more source
Molecular glues: Recent advances in cereblon substrate identification and mechanistic insights. [PDF]
Smart MolMolecular glues exert diverse core biological functions by inducing or stabilizing protein–protein interactions, extending far beyond the traditional scope of targeted protein degradation. Key breakthroughs include expanded cereblon substrate recognition, sustained G protein‐coupled receptor megacomplex signaling, and the first orthosteric molecular ...
Guan Q +5 more
europepmc +2 more sources
G Protein-Coupled Receptors (GPCRs) in Alzheimer’s Disease: A Focus on BACE1 Related GPCRs [PDF]
, 2016 The G protein coupled receptors (GPCRs) have been considered as one of the largest families of validated drug targets, which involve in almost overall physiological functions and pathological processes.
Yulin eDeng +7 more
core +1 more source
The Adhesion GPCRs; Gene Repertoire, Phylogeny and Evolution
, 2010 The Adhesion family is unique among the GPCR (G protein-coupled receptor) families because of several features including long N-termini with multiple domains. The gene repertoire has recently been mined in great detail in several species including mouse,
Helgi B. Schiöth +5 more
core +1 more source
Orphan GPCRs and Neuromodulation [PDF]
, 2012 Most G protein-coupled receptors (GPCRs) started as orphan GPCRs. Matching them to known neuromodulators led to the elucidation of the broad diversity of the neuroreceptor families.
Civelli, Olivier
core +1 more source
Intranuclear Signaling Cascades Triggered by Nuclear GPCRs [PDF]
, 2016 G protein-couped receptors (GPCRs) play a key role on cellular membranes, where they respond to a broad array of extracellular signals such as lipids, peptides, proteins and sensory agents.
Fabio Cattaneo +9 more
core +1 more source
Microbiome‐blood–brain barrier interactions in aging — mechanisms and therapeutic potential
FEBS Letters, EarlyView.Aging reshapes the gut microbiome (↓SCFA‐producing commensals; ↑pro‐inflammatory outputs), shifting circulating metabolites (↓SCFAs; ↑LPS, ↑TMAO, ↑PAA) that act at the BBB to increase nonspecific transcytosis, alter transport, and promote astrocyte reactivity, heightening brain vulnerability.
Daniel Cuervo‐Zanatta +3 more
wiley +1 more source
Thermodynamic architecture and conformational plasticity of GPCRs
, 2023 GPCRs are integral membrane proteins that serve as attractive drug targets. Here, authors delineate the conformational landscapes of 45 GPCRs using a statistical model, highlighting their malleable native ensembles and providing functional ...
Athi N. Naganathan +1 more
core +1 more source
An epithelial GPR35 isoform supports tumor‐associated transcriptional and metabolic phenotypes
FEBS Letters, EarlyView.GPR35 generates two functionally distinct isoforms with previously unresolved roles. GPR35‐short mediates immune‐cell chemotaxis, while GPR35‐long is enriched in colorectal cancer epithelium, where it supports increased metabolism, proliferation, and tumor‐associated transcriptional programs.
Jørgen D. Rønneberg +14 more
wiley +1 more source
Untersuchung der Struktur und Interaktion mit allosterischen Modulatoren der Familie C GPCRs mit Hilfe von Sequenz-, Struktur- und Ligand-basierten Verfahren [PDF]
, 2009 This study focuses on structural features of a particular GPCR type, the family C GPCRs. Structure- and ligand-based approaches were adopted for prediction of novel mGluR5 binding ligand and their binding modes. The objectives of this study were: 1.
Derksen, Swetlana
core