GPCR Summit 2022 is less than a month away!

neuron morphogenesis and shapes chemo- and mechanosensation-dependent behavior in C. elegans via a trans Latrophilins in the nematode Caenorhabditis elegans can also function independently of their seven-transmembrane domain and C terminus (trans function). Here, we show that Latrophilin-1 acts in trans to mediate morphogenesis of sensory structures in the This trans function is physiologically relevant in copulation behavior.

August 2022 "Opioid receptors (ORs) represent one of the most significant groups of G-protein coupled receptor (GPCR) drug targets and also act as prototypical models for GPCR function. In a constant effort to develop drugs with less side effects, and tools to explore the ORs nature and function, various (poly)pharmacological ligand design approaches have been performed. That is, besides classical ligands, a great number of bivalent ligands (i. e. aiming on two distinct OR subtypes), univalent heteromer-selective ligands and bitopic and allosteric ligands have been synthesized for the ORs. The scope of our review is to present the most important of the aforementioned ligands, highlight their properties and exhibit the current state-of-the-art pallet of promising drug candidates or useful molecular tools for the ORs." Read more at the source #DrGPCR #GPCR #IndustryNews

flytrap (VFT) unit that activates G protein-dependent signaling via twin Cysteine-rich domains linked to transmembrane Transfected HEK-293 cells were assessed for Ca2+o -stimulated Ca2+i mobilization using mutations in either Finally, we observed that the Ca2+o -stimulated CaSR operated exclusively via signaling in-trans and not via combined in-trans and in-cis signaling.

In particular, platelets can activate neutrophils to form neutrophil extracellular traps (NETs). decorated with histones and antimicrobial proteins into the extracellular space where they serve to trap In light of the current COVID-19 pandemic, the topic of immunothrombosis has become more relevant than

September 2022 Ginsenoside Rg5 allosterically interacts with P2RY12 and ameliorates deep venous thrombosis by counteracting neutrophil NETosis and inflammatory response "Deep venous thrombosis (DVT) highly occurs in patients with severe COVID-19 and probably accounted for their high mortality. DVT formation is a time-dependent inflammatory process in which NETosis plays an important role. However, whether ginsenoside Rg5 from species of Panax genus could alleviate DVT and its underlying mechanism has not been elucidated." Read more at the source #DrGPCR #GPCR #IndustryNews

recent research has benefited from advances in high-resolution techniques to investigate peptidergic transmission Neuropeptides exhibit distinct characteristics which includes their post-translational processing, release Current research has focused on isolating when and how neuropeptide transmission occurs, as well as the

September 2022 Endothelin-1 Stimulates PAI-1 Protein Expression via Dual Transactivation Pathway Dependent ROCK and Phosphorylation of Smad2L "In addition to the carboxy region, Smad2 transcription factor can The purpose of this study was to evaluate the role of dual transactivation of EGF and TGF-β receptors protein-coupled receptor (GPCR) signaling, the functions of ROCK and PLC were investigated in dual transactivation that ET-1 increases the phosphorylation of Smad2L and protein expression of PAI-1<br />via induced the transactivation

Coordinated transcriptomics and peptidomics of central nervous system identify neuropeptides and their Here, we generated a transcriptome of the central nervous system (CNS) of G. molesta.

Recent advancements in transcriptomic profiling have provided new insights into the expression patterns semi-quantitative multiplex PCR method, which allowed for the detection of both abundant and rare GPCR transcripts

AlphaProteo generates novel proteins for biology and health research Innovate UK announced the winners of its Transforming Special Issue of Molecular Pharmacology GPCR Events, Meetings, and Webinars September 5 - 6, 2024 | 4th Transatlantic

orientation of individual residues and/or their interactions not easily detectable in the receptor-transducer determine partner preference; or (iii) the dynamics of GPCR binding to different types of partners rather than the structures of the final complexes might underlie transducer bias."

Transmembrane domains of GPCR dimers – a novel hot spot for drug discovery G-protein-coupled receptors The interaction between two receptors in a dimer involves a conformational change in the transmembrane domain (TMD), with the most compelling studies revealing that the transmembrane helices TM4 and TM5 GPCRs dimers exist in a transient state however they are still able to be activated and interact with A more in-depth analysis of the functional specificity of transmembrane peptides will provide a better

October 2022 Glucagon receptor-mediated regulation of gluconeogenic gene transcription is endocytosis-dependent GPCRs) are now thought to use endocytosis to promote cellular cAMP signaling that drives downstream transcription dynamin-dependent endocytosis in HEK293 and Huh-7-Lunet cells after activation by glucagon within 5 min and transit

October 2022 Membrane Lipids Are an Integral Part of Transmembrane Allosteric Sites in GPCRs: A Case ORG27569, and Analogs "A growing number of G-protein-coupled receptor (GPCR) structures reveal novel transmembrane show that membrane lipids are critical in the access and binding of ORG27569 and its analogs at the transmembrane Our results demonstrate the significance of incorporating membrane lipids as an integral component of transmembrane

We will first summarize their prominent roles in GPCR pharmacology before transitioning into less well-explored

October 2022 High hedgehog signaling is transduced by a multikinase-dependent switch controlling the distribution of the GPCR smoothened "The oncogenic G-protein-coupled receptor (GPCR) Smoothened (SMO) is a key transducer

involved in the modulation of fundamental physiological functions, and dysregulation of dopaminergic transmission azodopa, a novel photoswitchable ligand that enables reversible spatiotemporal control of dopaminergic transmission

distinct signaling and physiological properties: PTH evokes prolonged Gs activation, whereas PTHrP evokes transient

opsin indicated that phospholipid headgroups traverse a dynamically revealed hydrophilic groove between transmembrane

September 2022 Lysine 101 in the CRAC Motif in Transmembrane Helix 2 Confers Cholesterol-Induced Thermal Receptor "G protein-coupled receptors (GPCRs) constitute the largest class of membrane proteins that transduce role of the K101 residue in a cholesterol recognition/interaction amino acid consensus (CRAC) motif in transmembrane

distinct signaling and physiological properties: PTH evokes prolonged Gs activation, whereas PTHrP evokes transient

April 2022 Trevena Announces Receipt of First $15 million Tranche in Connection with its $40 million (Nasdaq: TRVN), a biopharmaceutical company focused on the development and commercialization of novel patients with central nervous system (CNS) disorders, today announced receipt of the first $15 million tranche

The sixth transmembrane region of a pheromone G-protein coupled receptor, Map3, is implicated in discrimination

heterodimers with allosteric cross-talk between receptor entities, which contributes to fine-tuning of transmembrane examined the mode of action of positive allosteric modulators (PAMs) that bind at the interface of the transmembrane The data support the inference that they act at the active interface between both transmembrane domains Importantly, the agonist activity of these PAMs involves a key region in the central core of the GABAB2 transmembrane compounds able to specifically modulate the activity of GPCR homo- and heterodimers by acting at their transmembrane

March 2022 ERNEST has established an Emergency Fund for Ukrainian researchers. "General Eligibility Researchers affiliated to any legal entity in Ukraine (for example, schools and universities, research centers, governmental institutions, or private companies) Deadlines Start of the project: now End of the project: 31 October 2022 SHORT-TERM SCIENTIFIC MISSIONS (STSM) We offer short-term scientific mission grants to Ukrainian researchers who have been recently displaced by the war, or those who can travel to institutions participating in ERNEST COST Action. The purpose of the STSM is to carry out a collaborative research project on topics relevant to the network. Our scientific perspective is broad, and we are happy to consider any research proposals from those in need." Read more at the source #DrGPCR #GPCR #IndustryNews

G protein-coupled receptors (GPCRs) have been shown to play integral roles in Alzheimer's disease pathogenesis. However, it is unclear how diverse GPCRs similarly affect Aβ and tau pathogenesis. GPCRs share a common mechanism of action via the β-arrestin scaffolding signaling complexes, which not only serve to desensitize GPCRs by internalization, but also mediate multiple downstream signaling events. As signaling via the GPCRs, β2-adrenergic receptor (β2AR), and metabotropic glutamate receptor 2 (mGluR2) promotes hyperphosphorylation of tau, we hypothesized that β-arrestin1 represents a point of convergence for such pathogenic activities. Here, we report that β-arrestins are not only essential for β2AR and mGluR2-mediated increase in pathogenic tau but also show that β-arrestin1 levels are increased in brains of Frontotemporal lobar degeneration (FTLD-tau) patients. Increased β-arrestin1 in turn drives the accumulation of pathogenic tau, whereas reduced ARRB1 alleviates tauopathy and rescues impaired synaptic plasticity and cognitive impairments in PS19 mice. Biochemical and cellular studies show that β-arrestin1 drives tauopathy by destabilizing microtubules and impeding p62/SQSTM1 autophagy flux by interfering with p62 body formation, which promotes pathogenic tau accumulation. Read full article

Here, we briefly summarize a subset of this field with accelerating importance: transducer biosensors