and kidney fibrosis and pathological angiogenesis, including occurrence of endothelial-to-mesenchymal transition

deficient mouse models resulted in alterations in the MAM architecture and in the dysregulation of the Ca2+ transient

October 2022 "Protease activated receptors (PARs) are among the first receptors shown to transactivate

to be discussed and to be put in context as soon as possible to be up-to-date and to accelerate the translation

have participated in various cellular processes such as cell proliferation, migration, apoptosis, and transcription

However, in epithelial cells, OGR1 promotes epithelial to mesenchymal transition (EMT) and inflammation

results in the generation of diacylglycerol and inositol trisphosphate, which are downstream signal transducers In this article, we describe the signal transduction elements that regulate PLC gene expression.

We performed a siRNA knockdown (KD) to assess the effect of Sigma-2 receptor (S2R) /Transmembrane Protein

A role for BET proteins in regulating basal, dopamine-induced and cAMP/PKA-dependent transcription in signalling cascade that increases excitability and facilitates plasticity, partly through the regulation of transcription Upon activation via D1R, PKA can translocate to the nucleus to regulate transcription through the phosphorylation One candidate effector of PKA-dependent transcriptional regulation is the BET protein Brd4. However, it is unknown whether BET proteins, or Brd4 specifically, are involved in transcriptional activation

October 2022 Recurrent hypoglycemia increases hepatic gluconeogenesis without affecting glycogen metabolism or systemic lipolysis in rat "Introduction: Recurrent hypoglycemia (RH) impairs secretion of counterregulatory hormones. Whether and how RH affects responses within metabolically important peripheral organs to counterregulatory hormones are poorly understood. Objective: To study the effects of RH on metabolic pathways associated with glucose counterregulation within liver, white adipose tissue and skeletal muscle. Methods: Using a widely adopted rodent model of 3-day recurrent hypoglycemia, we first checked expression of counterregulatory hormone G-protein coupled receptors (GPCRs), their inhibitory regulators and downstream enzymes catalyzing glycogen metabolism, gluconeogenesis and lipolysis by qPCR and western blot. Then, we examined epinephrine-induced phosphorylation of PKA substrates to validate adrenergic sensitivity in each organ. Next, we measured hepatic and skeletal glycogen content, degree of breakdown by epinephrine and abundance of phosphorylated glycogen phosphorylase under hypoglycemia and that of phosphorylated glycogen synthase during recovery to evaluate glycogen turnover. Further, we performed pyruvate and lactate tolerance tests to assess gluconeogenesis. Additionally, we measured circulating FFA and glycerol to check lipolysis. The abovementioned studies were repeated in streptozotocin-induced diabetic rat model. Finally, we conducted epinephrine tolerance test to investigate systemic glycemic excursions to counterregulatory hormones. Saline-injected rats served as controls." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "GPCR signaling and function depend on their associated proteins and subcellular locations. Besides G-proteins and β-arrestins, 14-3-3 proteins participate in GPCR trafficking and signaling, and they connect a large number of diverse proteins to form signaling networks. Multiple 14-3-3 isoforms exist, and a GPCR can differentially interact with different 14-3-3 isoforms in response to agonist treatment. We found that some agonist-induced GPCR/14-3-3 signal intensities can rapidly decrease. We confirmed that this phenomenon of rapidly decreasing agonist-induced GPCR/14-3-3 signal intensity could also be paralleled with GPCR/β-arrestin-2 signals, indicating diminished levels of GPCR/signal adaptor complexes during endocytosis. The temporal signals could implicate either GPCR/14-3-3 complex dissociation or the complex undergoing a degradation process. Furthermore, we found that certain GPCR ligands can regulate GPCR/14-3-3 signals temporally, suggesting a new approach for GPCR drug development by modulating GPCR/14-3-3 signals temporally." Read more at the source #DrGPCR #GPCR #IndustryNews

Its groundbreaking ability to accurately predict protein structures is transformative for identifying Despite its transformative potential, AI in drug development faces several challenges. advanced AI models like AlphaFold3, which can predict complex protein-molecule interactions and post-translational The lack of transparency surrounding its operations and usage constraints restricts extensive academic Additionally, transparency in AI models and their operations is crucial for building trust and allowing

GPCR Activation and Signaling Trans-palmitoleic acid, a dairy fat biomarker, stimulates insulin secretion Esophageal and gastric cancer incidence trends in Golestan, Iran: An age-period-cohort analysis 2004 G protein-coupled receptors as targets for transformative neuropsychiatric therapeutics. Structure, Mechanism, and Drug Interactions of GPCRs, Ion Channels, and Transport Proteins (March 24

In cellular-adhesion assays, LK30 specifically broke the trans-cellular interaction of ADGRL3 with teneurin

., for their work on The N terminus-only (trans) function of the Adhesion GPCR Latrophilin-1 controls Special Issue of Molecular Pharmacology GPCR Events, Meetings, and Webinars September 5 - 6, 2024 | 4th Transatlantic mechanosensing   Postdoctoral Position Postdoctoral research position Adhesion GPCRs The N terminus-only (trans interaction Early Events in β2AR Dimer Dynamics Mediated by Activation-Related Microswitches Nuclear translocation

Retrograde trans-synaptic rabies virus tracing revealed that postsynaptic cAMP signaling is required

Machine learning (ML) and deep learning (DL) are subfields of artificial intelligence (AI) that involve training However, DL algorithms typically require large amounts of labelled training data comprising millions reason, DL models generally require more computational resources (such as powerful GPUs) and longer training models, such as deep learning neural networks, are often referred to as "black boxes" because they lack transparency Efforts will likely be made to develop AI models that can provide transparent explanations for their

CCR2 was also shown to be resistant to degradation and most likely recycling through the trans-Golgi with CCR2, indicating that β-arrestin regulates scavenging and signaling of CCR1 to a greater extent than

GPCR Activation and Signaling Signal Transduction and Gene Regulation in the Endothelium. STALICLA signs agreement with Novartis on neurodevelopmental disorders Call for GPCR Papers GPCRs: Signal Transduction Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit | February 21-23, Boston. 2nd ERNEST Training GPCR Jobs Biotechnology and Biological Sciences Doctoral Training Programme Senior QM Manager Director Molecular Pharmacology, Discovery Biology Staff Scientist/Senior Staff Scientist, Disease Biology and Translational

A much smaller conformational change of helix VI upon activation than previously solved class A GPCR-Gi with three cholesterol molecules that play essential roles in conformation stabilization and signaling transduction

GPCR Activation and Signaling New simulation insights on the structural transition mechanism of Bovine Announces Launch of US Phase 2 Trial of GPC-100 in Multiple Myeloma Call for GPCR Papers GPCRs: Signal Transduction (May 22 - 26, 2023) 2nd ERNEST Training School. (February 20 - March 3, 2023). GEM2023. GPCR Jobs Biotechnology and Biological Sciences Doctoral Training Programme Senior QM Manager Director Molecular Pharmacology, Discovery Biology Staff Scientist/Senior Staff Scientist, Disease Biology and Translational

is one of the 13 biotech companies to discover in western in 2023 Call for GPCR Papers GPCRs: Signal Transduction SLAS2023 International Conference and Exhibition (February 25 - March 1, 2023). 2nd ERNEST Training School Team Lead (depending on experience) with Structural Bioinformatics Expertise Fully Funded Doctoral Training

22 to 28, 2024 GPCR Activation and Signaling Activating an invertebrate bistable opsin with the all-trans Regulation of C-C Chemokine Receptor 3 Oligomerization by Downstream Proteins Indicates Biased Signal Transduction Receptors that Regulate the Release of Superoxide Anions GPR176 promotes fibroblast-to-myofibroblast transition

2022 "G-protein-coupled receptors (GPCRs) receive signals from ligands with different efficacies, and transduce intermediate state complex comprising β1-AR and nucleotide-free Gs is more stable when binding a full agonist than

August 2022 "Abstract Sigma receptor is a transmembrane non-GPCR protein expressed mainly in the endoplasmic Six compounds showed more than 50% displacement of the radioligand at 10 µM concentration with compound

C5a is established to interact with a set of genomically related transmembrane receptors, like C5aR1 C5aR2 is a nonclassical GPCR that tailors immune cell activity potentially through β-arrestins rather than

Train-dependent presynaptic Ca2+ accumulation forces frequency-dependent recovery of neurotransmission Thus, stimulus trains in 5-HT1B receptor agonist unveil dynamic synaptic modulation and a sophisticated leaving synaptic properties unchanged, while 5-HT1B receptors fundamentally change properties of synaptic transmission

their biological context due to the low solubility that the hydrophobic nature imprinted by their seven transmembrane density obtained by quantitative Western blot were of the same order of magnitude but slightly higher than