A growing number of GPCRs have been shown to be localized in the nucleus and contribute toward transcriptional In the presence of its ligand, we show significant upregulation of H2R nuclear translocation kinetics tagged histamine, we explored H2R-histamine binding interaction, which exhibits a critical role in this translocation , such as the functional relevance of this localization, and whether H2R can contribute directly to transcriptional

By means of molecular dynamics we explained why C5aR2 cannot transduce signal through the G protein pathway C5aR1 receptor conformations has provided insights into details of local and global changes in the transmembrane

ligand-free forms of CCR5 at the cell surface constituted of various oligomeric states and exhibiting transient

In GPCR crystallography, inserting a fusion protein between transmembrane helices 5 and 6 is a highly

and 125I NF-α1/CPE-binding studies demonstrated saturable, high-affinity binding to 5-HTR1E in stably transfected

The SG receptor that transduces the Fog signal into Rho1-dependent myosin activation has not been identified Here, we reveal that the Smog GPCR transduces Fog signal to regulate Rho kinase accumulation and myosin

domain (WAP) is necessary for this modulatory activity, although data from GST pull-down (glutathione-S-transferase

Studies have indicated that transmembrane helix 7 (TMH7) and the highly conserved NPXXY motif can be

We discuss the importance of understanding the translatability of cell and animal models to have more

Listen to her talk about her work and her transition to PI in Belfast.

2022 Signaling pathways activated by sea bass gonadotropin-inhibitory hormone peptides in COS-7 cells transfected basal CRE-luc activity, they significantly decreased forskolin-elicited CRE-luc activity in COS-7 cells transfected These data indicate that sea bass GnIHR signals can be transduced through the PKA and PKC pathways, and

Wnt binding to Frizzled (Fzd) and LRP5 or LRP6 (LRP5/6) co-receptors inhibits the degradation of the transcriptional GPCR superfamily for which the binding of extracellular ligands affects the affinity for downstream transducers

Counting Kit-8 and colon formation, and cell migration and invasion were detected by wound healing and transwell

computations to predict the mechanism by which the inactive GP induces conformational changes in the GABABR transmembrane

between the activated GALR2 and inactive hβ2AR was used to relate galanin binding to the movements of transmembrane

Although the vital role of ACs in cellular signalling is well established, the function of their transmembrane

The SG receptor that transduces the Fog signal into Rho1-dependent myosin activation has not been identified Here, we reveal that the Smog GPCR transduces Fog signal to regulate Rho kinase accumulation and myosin

epithelial cells responding to butyrate and secondary bile acids in combination discovered a unique transcriptional

These structures show that ZCZ011 binds to an extrahelical site in the transmembrane 2 (TM2)-TM3-TM4

Major conformational differences were located on transmembrane (TM) 5 and 6, as well as intracellular Compared to naltrindole, ADL5859 exhibited high conformational flexibility and strong interaction with the transmission

September 2022 Isoforms of GPR35 have distinct extracellular N-termini that allosterically modify receptor-transducer provide clues for the future design of isoform-specific GPR35 ligands that selectively modulate GPR35-transducer

Receptor Enhances Chemoresistance of Glioblastoma Stem-Like Cells under Hypoxia: New Insights into MRP3 Transporter The chemoresistance of GSCs is mediated in part by adenosine signaling and ABC transporters, which extrude Transcript and protein levels were determined by RT-qPCR and Western blot, respectively.

Based on our transcriptomic analysis, expression of GPER was correlated with clinicopathological variables Transcriptome-based bioinformatics analysis revealed that GPER was linked to pro-metastatic pathways

Promising nuclear receptors as key regulators of transcriptional programmes will be introduced as well stem cell maintenance such as by employing hedgehog and WNT, which promote fibroblast-to-myofibroblast transition

Structurally, the extensive extracellular domain, which contains the hormone-binding site and is linked to the transmembrane How this HR is involved in hormone binding and signal transduction is still an open question. The models are expected to allow for testable hypotheses about signal transduction and drug development

September 2022 "RNA editing is a process by which post-transcriptional changes of mRNA nucleotides alter molecular mechanisms responsible for these effects of RNA editing, we present four active-state 5HT2C-transducer-coupled

September 2022 "The Smoothened receptor (SMO, a 7 pass transmembrane domain, Class F GPCR family protein In the absence of HH signaling, SMO is inhibited by Patched 1 (PTC1; a 12 pass transmembrane domain protein We show that cholesterol interactions with the transmembrane domain TMD, unlike those with the cysteine-rich also reported the interaction of phosphatidylinositol 4-phosphate with the intracellular region of transmembrane

September 2022 "Heterotrimeric G-protein transducin, Gt, is a key signal transducer and amplifier in Immunohistochemistry and Western blotting demonstrated the robust expression of each transgenic Gγ in Bright illumination triggered Gαt1 translocation from the rod outer to inner segments in all three transgenic However, Gαt1 translocation in Gγ11 transgenic mice occurred at significantly dimmer background light illumination in Gγ11 transgenic mice but not in Gγ1 controls.