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Although increasing evidence has suggested the direct role of fentanyl on cancer, little is known on

Chemerin is produced by the liver and secreted into the circulation as a precursor, but it is also expressed

Using purified Fzd proteins reconstituted in lipid nanodiscs, we investigated the factors that promote We found that the affinity of Fzd for Dvl was not affected by Wnt ligands, in contrast to other members of the GPCR superfamily for which the binding of extracellular ligands affects the affinity for downstream Instead, Fzd-Dvl binding was enhanced by increased concentration of the lipid PI(4,5)P2, which is generated by Dvl-associated lipid kinases in response to Wnt and which is required for LRP5/6 phosphorylation.

CC chemokine receptor 9 (CCR9), an organ-specific chemokine receptor, interacts with its exclusive ligand

However, little is known about the mechanism for GP coupling and activation for class C GPCRs.

We identified a novel GRK3 inhibitor, LD2, through a chemical-library screen.

Significantly, many ligands acting on neurotransmitter receptors have shown great potential for inhibiting

We also adopted live cell imaging to monitor the whole intracellular trafficking process of F-Hst1.

In light of the current COVID-19 pandemic, the topic of immunothrombosis has become more relevant than

domain and providing the means for direct regulation of catalytic activity in response to extracellular ligands

During Drosophila embryonic salivary gland (SG) invagination, the GPCR ligand Folded gastrulation (Fog Our data support a model wherein Smog regulates distinct myosin pools and actin cytoskeleton in a ligand-dependent

nucleus accumbens shell and structures in the prefrontal cortex and amygdala, which were previously linked

Smad2L "In addition to the carboxy region, Smad2 transcription factor can be phosphorylated in the linker Phosphorylation of Smad2 linker region (Smad2L) promotes the expression of plasminogen activator inhibitor were investigated<br />by western blotting using protein-specific antibodies against phospho-Smad2 linker

KISS1R signalling and physiological output in the hormone receptor-negative MDA-MB-231 and BT-20 cell lines MDA-MB-231 cells are metastatic when implanted in mice while BT-20 are not and remain epithelial-like We show that both cell lines express KISS1R mRNA and respond to KP-10 by elevating calcium mobilisation Interestingly, both cell lines displayed different complements of β-arrestin 1 and 2 expression. stimulate migration or pro-metastatic behaviour, as divergent responses were observed in the two TNBC lines

receptor-mediated Gα protein signalling using a G protein activation assay and second messenger assay conducted on living

Using shRNA knockdown and CRISPR/Cas9 knockout cell lines, as well as mouse models, we confirmed the These findings shed light on a sophisticated signaling network directed by intestinal microbial metabolites that orchestrate P-gp expression and highlight unappreciated connections between multiple pathways linked

Thus, we investigated the regulatory functions of its β-adrenergic-like octopamine receptor (PxOctβ3)

Mechanistically, GASP1 inhibited proteasomal degradation of insulin-like growth factor 1 receptor (IGF1R ) by competitively binding to IGF1R with ubiquitin E3 ligase MDM2, thereby activating its downstream

While the receptor with the crystal ligand (i.e. antagonist naltrindole) maintained the inactive conformation the conventional molecular switch analysis and a pairwise distance analysis, which provides a short list

The structure demonstrates a unique ligand-binding mode, involving an allosteric sub-pocket, which clarifies structures in complex with antagonists and agonists, our structure with S1P5-inverse agonist sheds light

Additionally, we employed optical assays in living cells to thoroughly profile both GPR35 isoforms for constitutive and ligand-induced activation and signaling of 10 different heterotrimeric G proteins, ligand-induced arrestin recruitment, and receptor internalization. Our results reveal that the extended N-terminus of the long isoform limits G protein activation yet elevates and mechanistic insights of our study provide clues for the future design of isoform-specific GPR35 ligands

Venus flytrap (VFT) unit that activates G protein-dependent signaling via twin Cysteine-rich domains linked

modulator of PTH1R, shifting PTH1R to a unique preactivated state that permits faster activation in a ligand-specific

that GPR84 expression in leukocytes is remarkably increased under acute inflammatory stimuli such as lipopolysaccharide

conformational ensemble of CX3C chemokine receptor 1 (CX3CR1) and its interactions with antagonist and agonist ligands receptor 1 (CX3CR1), a member of the class A of G Protein-Coupled Receptors (GPCR) superfamily, and its ligand characterize the conformational ensemble of the receptor in the presence of its antagonist and agonist ligands the receptor conformational changes and described interactions within its key regions and the bounded ligands

Here, we used a proximity ligation assay (PLA)–based approach for the in situ visualization and quantification