2022 Luciferase-based GloSensor™ cAMP assay: Temperature optimization and application to cell-based kinetic this regard, luminescence-based biosensors have revolutionized our ability to monitor GPCR signaling kinetics

September 2022 Roles of Focal Adhesion Kinase PTK2 and Integrin αIIbβ3 Signaling in Collagen- and GPVI-Dependent Here, we focused on disclosing the integrin-dependent roles of focal adhesion kinase (protein tyrosine kinase 2, PTK2), the shear-dependent collagen receptor GPR56 (ADGRG1 gene), and calcium and integrin-binding

December 2021 Neurocrine Biosciences Announces Positive Phase 3 Data for KINECT-HD Study Evaluating Valbenazine PRNewswire/ -- Neurocrine Biosciences (Nasdaq: NBIX) today announced positive top-line data from its Phase 3 KINECT-HD

To overcome this potential uncertainty, we used a homologous recombination-based knockin (KI) approach The resulting homozygous hPTH1R-KI (humanized) mice were healthy over at least 10 generations and showed injected PTH analog peptides that are consistent with a fully functional human PTH1R in target bone and kidney

Extracellular signal-regulated kinases (ERK), a subset of the mitogen-activated protein kinase (MAPK) Initially, the activation of small GTPases like RAS leads to the activation of the MAP kinase kinase kinases (MAPKKKs), such as RAF. RAF then phosphorylates and activates the MAP kinase kinases (MAPKKs), MEK1 and MEK2, which in turn phosphorylate Extracellular Signal-Regulated Kinase: A Regulator of Cell Growth, Inflammation, Chondrocyte and Bone

We synthesized and characterized a novel A2AAR antagonist, 2 (LJ-4517), with Ki = 18.3 nM.

displacement of the radioligand at 10 µM concentration with compound 6c resulting in 100% displacement and a Ki

October 2022 Use of CRISPR/Cas9-edited HEK293 cells reveals that both conventional and novel protein kinase In this study, we generated and characterized human embryonic kidney 293A (HEK293A) cell lines devoid Additionally, using the Gαq/11 inhibitor YM-254890, GPCR kinase 2 and 3 (GRK2 and GRK3) KO cells, and

October 2022 Bell-Evans model and steered molecular dynamics in uncovering the dissociation kinetics targeting G-protein-coupled receptors "Recently, academic and industrial scientific communities involved in kinetics-based Our results build a strong foundation for further improvement of our approach by rationalizing the kinetics

August 2022 G protein-coupled receptor kinase type 2 and β-arrestin2: Key players in immune cell functions and inflammation "G protein-coupled receptor kinase type 2 (GRK2) and β-arrestin2 are representative The kinase GRK2 and the multifunctional scaffolding protein β-arrestin2 are key integrated signaling

August 2022 "Emerging evidence suggests that G protein-coupled receptor (GPCR) kinases (GRKs) are associated

September 2022 Lack of Oestrogen Receptor Expression in Breast Cancer Cells Does Not Correlate with Kisspeptin Signalling and Migration "Kisspeptin is an anti-metastatic mediator in many cancer types, acting through its receptor, KISS1R. In KISS1R overexpressing triple-negative breast cancer (TNBC) cells, stimulation has been associated Overall, our data shows that, in TNBC, it is not universally true that kisspeptin/KISS1R stimulate migration

September 2022 "G protein-coupled receptor (GPCR) kinases (GRKs) and arrestins mediate GPCR desensitization recruitment of the adaptor protein STAM1 (signal-transducing adaptor molecule) to βarr1 and focal adhesion kinase phosphorylation but not extracellular signal-regulated kinase 1/2 phosphorylation.

September 2022 Opposite Effects of Src Family Kinases on YAP and ERK Activation in Pancreatic Cancer combination of insulin and the GPCR agonist neurotensin induced rapid activation of Src family of tyrosine kinases

Among the known effectors recruited by GPCR-bound arrestins are Src family kinases, which regulate cellular Here, we focus on arrestin-3 interactions with Fgr kinase, a member of the Src family.

Lysophosphatidic Acid and Several Neurotransmitters Converge on Rho-Kinase 2 Signaling to Manage Motoneuron We hypothesized that isoform 2 of rho-kinase (ROCK2), acting as downstream GPCRs, mediates adjustment

G protein-coupled receptor kinase 2 is essential to enable vasoconstrictor-mediated arterial smooth muscle GPCR signalling through phosphoinositide 3-kinase (PI3K)/protein kinase B (Akt) promotes VSMC proliferation In VSMC, G protein-coupled receptor kinase 2 (GRK2) is known to regulate numerous vasoconstrictor GPCRs

Sandra Berndt talk about new structural perspectives in GPCR-mediated Src family kinase activation.

September 2022 "Yeast use the G-protein–coupled receptor signaling pathway to detect and track the mating pheromone. The G-protein–coupled receptor pathway is inhibited by the regulator of G-protein signaling (RGS) Sst2 which induces Gα GTPase activity and inactivation of downstream signaling. G-protein signaling activates the MAPK Fus3, which phosphorylates the RGS; however, the role of this modification is unknown. We found that pheromone-induced RGS phosphorylation peaks early; the phospho-state of RGS controls its localization and influences MAPK spatial distribution. Surprisingly, phosphorylation of the RGS promotes completion of cytokinesis before pheromone-induced growth. Completion of cytokinesis in the presence of pheromone is promoted by the kelch-repeat protein, Kel1 and antagonized by the formin Bni1. We found that RGS complexes with Kel1 and prefers the unphosphorylatable RGS mutant. We also found overexpression of unphosphorylatable RGS exacerbates cytokinetic defects, whereas they are rescued by overexpression of Kel1. These data lead us to a model where Kel1 promotes completion of cytokinesis before pheromone-induced polarity but is inhibited by unphosphorylated RGS binding." Read more at the source #DrGPCR #GPCR #IndustryNews

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ATG5: autophagy related 5; ATG7: autophagy related 7; Baf A1: bafilomycin A1; CDK2: cyclin dependent kinase 2; CDKN1B/p27Kip1: cyclin dependent kinase inhibitor 1B; CQ: chloroquine; E2F1: E2F transcription factor ; MAP1LC3B/LC3: microtubule associated protein 1 light chain 3 beta; MKI67: marker of proliferation Ki -67; MTOR: mechanistic target of rapamycin kinase; MAPK: mitogen-activated protein kinase; 3-MA: 3-methyladenine ; NFKB/NF-κB: nuclear factor kappa B; PIK3CA: phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic

The distinct molecular actions are ascribed to the differences in ligand recognition and dissociation kinetics

October 2022 "The cAMP-dependent protein kinase (PKA) system represents a primary cell-signaling pathway

August 2022 "Three classes of G-protein-coupled receptor (GPCR) partners - G proteins, GPCR kinases,

signaling pathways mediating in sea bass GnIH actions and the potential interactions with sea bass kisspeptin (Kiss) signaling. Notably, GnIH2 antagonized Kiss2-evoked CRE-luc activity in COS-7 cells expressing GnIHR and Kiss2 receptor (Kiss2R). bass GnIHR signals can be transduced through the PKA and PKC pathways, and GnIH can interfere with kisspeptin

The distinct molecular actions are ascribed to the differences in ligand recognition and dissociation kinetics

September 2022 "Serotonin receptor 5-HT2A and tropomyosin receptor kinase B (TrkB) strongly contribute

compared to wild type CXCR4 including agonist-promoted calcium flux and extracellular signal-regulated kinase