vasopressin 2 receptor "Abstract Background and purpose: Venomous animals express numerous Kunitz-type peptides The mambaquaretin-1 (MQ1) peptide identified from the Dendroaspis angusticeps venom is the most selective antagonist of the arginine-vasopressin V2 receptor (V2R) and the only unique Kunitz-type peptide active We aimed to exploit other mamba venoms to enlarge the V2R-Kunitz peptide family and gain insight into MQs were produced by solid-phase peptide synthesis and characterized in vitro by binding and functional

several important neurohormonal perturbations, emanating from both the autonomic nervous system and the adrenal The adrenal gland plays an important role in the modulation of cardiac neurohormonal stress because it Synthesis and release of these hormones in the adrenals is tightly regulated by adrenal G protein-coupled In this review, we discuss important aspects of adrenal GPCR signaling and regulation, as they pertain to modulation of cardiac function in the context of chronic HF, by focusing on the 2 best studied adrenal

that removes the inhibitory GAIN domain on the extracellular side of receptor and releases a stalk peptide We further provide physiological evidence of GPR110 activation via stalk peptide.

September 2022 "The glucagon-like peptide-1 receptor (GLP-1R) plays a key role in metabolism and is an

September 2022 Signaling pathways activated by sea bass gonadotropin-inhibitory hormone peptides in COS increase in SRE-luc activity was noticed when COS-7 cells expressing GnIHR were challenged with both GnIH peptides However, GnIH peptides did not alter NFAT-RE-luc activity and ERK phosphorylation levels. Our results provide additional evidence for the understanding of signaling pathways activated by GnIH peptides

August 2022 "Host response to infection involves the activation of the complement system leading to the production of anaphylatoxins C3a and C5a. Complement factor C5a exerts its effect through the activation of C5aR1, chemotactic receptor 1, and triggers the G protein-coupled signaling cascade. Orthosteric and allosteric antagonists of C5aR1 are a novel strategy for anti-inflammatory therapies. Here, we discuss recent crystal structures of inactive C5aR1 in terms of an inverted orientation of helix H8, unobserved in other GPCR structures. An analysis of mutual interactions of subunits in the C5aR1-G protein complex has provided new insights into the activation mechanism of this distinct receptor. By comparing two C5aR receptors C5aR1 and C5aR2 we explained differences between their signaling pathways on the molecular level. By means of molecular dynamics we explained why C5aR2 cannot transduce signal through the G protein pathway but instead recruits beta-arrestin. A comparison of microsecond MD trajectories started from active and inactive C5aR1 receptor conformations has provided insights into details of local and global changes in the transmembrane domain induced by interactions with the Gα subunit and explained the impact of inverted H8 on the C5aR1 activation." Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Several G-protein coupled receptors (GPCR) are upregulated in Alzheimer's Disease (AD), which ought to facilitate neurotransmission, and improve cognition. Yet, despite this upregulation, associated physiological effects are not observed in AD patients. This paradox solicits urgent attention to find a suitable justification for disturbed neurotransmission in AD. This article focuses on the role of Aβ granules and their possible interaction with GPCRs that modulate neurotransmission and AD progression." Read more at the source #DrGPCR #GPCR #IndustryNews

November 2021 Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 GPCR/endocytosis/ERK signaling/S2R is involved in the regulation of the internalization, mitochondria-targeting and -activating properties of human salivary histatin 1 "Human salivary histatin 1 (Hst1) exhibits a series of cell-activating properties, such as promoting cell spreading, migration, and metabolic activity. We recently have shown that fluorescently labeled Hst1 (F-Hst1) targets and activates mitochondria, presenting an important molecular mechanism. However, its regulating signaling pathways remain to be elucidated. We investigated the influence of specific inhibitors of G protein-coupled receptors (GPCR), endocytosis pathways, extracellular signal-regulated kinases 1/2 (ERK1/2) signaling, p38 signaling, mitochondrial respiration and Na+/K+-ATPase activity on the uptake, mitochondria-targeting and -activating properties of F-Hst1. We performed a siRNA knockdown (KD) to assess the effect of Sigma-2 receptor (S2R) /Transmembrane Protein 97 (TMEM97)—a recently identified target protein of Hst1. We also adopted live cell imaging to monitor the whole intracellular trafficking process of F-Hst1. Our results showed that the inhibition of cellular respiration hindered the internalization of F-Hst1. The inhibitors of GPCR, ERK1/2, phagocytosis, and clathrin-mediated endocytosis (CME) as well as siRNA KD of S2R/TMEM97 significantly reduced the uptake, which was accompanied by the nullification of the promoting effect of F-Hst1 on cell metabolic activity. Only the inhibitor of CME and KD of S2R/TMEM97 significantly compromised the mitochondria-targeting of Hst1. We further showed the intracellular trafficking and targeting process of F-Hst1, in which early endosome plays an important role. Overall, phagocytosis, CME, GPCR, ERK signaling, and S2R/TMEM97 are involved in the internalization of Hst1, while only CME and S2R/TMEM97 are critical for its subcellular targeting. The inhibition of either internalization or mitochondria-targeting of Hst1 could significantly compromise its mitochondria-activating property." Read more at the source #DrGPCR #GPCR #IndustryNews

November 2022 "Neuropeptides produce robust effects on behavior across species, and recent research has benefited from advances in high-resolution techniques to investigate peptidergic transmission and expression throughout the brain in model systems. Neuropeptides exhibit distinct characteristics which includes their post-translational processing, release from dense core vesicles, and ability to activate G-protein-coupled receptors (GPCRs). These complex properties have driven the need for development of specialized tools that can sense neuropeptide expression, cell activity, and release. Current research has focused on isolating when and how neuropeptide transmission occurs, as well as the conditions in which neuropeptides directly mediate physiological and adaptive behavioral states. Here we describe the current technological landscape in which the field is operating to decode key questions regarding these dynamic neuromodulators." Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE

2022 Neurocrine Biosciences Presents Data on Treatment of Adolescent Patients with Classic Congenital Adrenal Hyperplasia at ENDO 2022 "06/13/22 - Substantial Reductions in Key Hormones and Hormone Precursors Observed present new Phase 2 data on the use of crinecerfont in adolescent patients with classic congenital adrenal hyperplasia (CAH) due to 21-hydroxylase deficiency (21-OHD), which demonstrated substantial reductions in adrenal

Antoinette MaassenVanDenBrink, et al. for their work on Intracellular pathways of calcitonin gene-related peptide-induced GPCR Partnered Events April 22 - 23, 2024 | Endocrine Metabolic GPCRs Join the Endocrine Metabolic GPCRs event in Birmingham, UK, on April 22-23, 2024. 1 is discarded by exosomes after internalization Intracellular pathways of calcitonin gene-related peptide-induced dynamics using single-molecule fluorescence Droplet-based microfluidic platform for detecting agonistic peptides

GPCR University February 8 - 29: Join Dr. GPCR University's live course with Dr. Terry Kenakin. April 22 - 23, 2024 | Endocrine Metabolic GPCRs Join us at the Endocrine Metabolic GPCRs event on April 22-23, 2024 in Birmingham, UK.

Here, we discovered that the epithelial-cell-derived antimicrobial peptides defensins activated orphan

GPCRs in Oncology and Immunology Vasoactive intestinal peptide receptor 2 signaling promotes breast cancer Scientist, Drug Metabolism and Pharmacokinetics PhD Opportunity - Investigation Of The Role Of The Formyl Peptide

cell-induced inflammation "Gut intraepithelial lymphocytes (IELs) are thought to calibrate glucagon-like peptide

Hello GPCR people! Check out our GPCR roundup now, and be the first to read! This week's highlight: Congrats to our partner GPCR Therapeutics, on their expansion into fibrosis with their new research. Save the dates: November 2 - 4: We're sponsoring the GPCR Retreat and would love to meet you there! Join the waitlist by emailing gpcrretreat@uottawa.ca. Submit a logo design by Nov 1st on the Logo Contest page. No registration is needed to submit your logo design. Subscribe now to Dr. GPCR Newsletter to get more info! Check out the weekly Classified GPCR News from October 2nd to 8th, 2023. GPCR Binders, Drugs, and more In silico identification of a biarylamine acting as agonist at human β3 adrenoceptors and exerting BRL37344-like effects on mouse metabolism Development, synthesis and evaluation of novel fluorescent Endothelin-B receptor probes GPCRs in Cardiology, Endocrinology, and Taste GPRASP1 loss-of-function links to arteriovenous malformations by endothelial activating GPR4 signals GPCRs in Neuroscience Involvement of a silkworm D2-like dopamine receptor in the promotion of feeding and related behaviors Methods & Updates in GPCR Research Functional GPCR expression in eukaryotic LEXSY system Structural and Molecular Insights into GPCR Function Interplay of Cholesterol and Actin in Neurotransmitter GPCR Signaling: Insights from Chronic Cholesterol Depletion Using Statin Side-Chain Dynamics of the α1B -Adrenergic Receptor determined by NMR via Methyl Relaxation Structural determinants of sphingosine-1-phosphate receptor selectivity Industry News Sosei Heptares and Verily Nominate First G-protein-coupled receptor Target for Therapeutic Development DKK 25 million to development of databases supporting medical research ‘Define your own success’: Duke leaders talk success, failure at symposium honoring Nobel Laureate Robert Lefkowitz Integral Molecular Secures Nearly $900K in NIH Funding to Discover Antibodies Against Difficult and Conserved Protein Targets GPCR Therapeutics Expands Pipeline into Fibrosis with a Combination Approach Targeting LPA1 GPCR Events, Meetings, and Webinars October 25 - 27, 2023 | 3rd Annual Meeting IRN I-GPCRNet November 2 - 4, 2023 | GPCR Retreat- Registration Closed November 15 - 17, 2023 | MPGPCR Conference November 20 - 23, 2023 | ASCEPT Annual Scientific Meeting February 3 - 7, 2024 | SLAS2024 International Conference and Exhibition March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating Conference April 5 - 10, 2024 | AACR Annual Meeting May 13 - 17, 2024 | 20th Annual PEGS Boston Summit May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Europe 2024 Conference and Exhibition June 2 - 4, 2024 | Chemotactic Cytokines GPCR Jobs NEW Senior Scientist, In vitro pharmacology - Crinetics Pharmaceuticals NEW Senior Director, In vitro pharmacology - Crinetics Pharmaceuticals In vivo Antibody Discovery Research Scientist In Vitro Biologist/Molecular Pharmacologist Senior Vice President, Oncology Clinical Research Scientist (level I or II) Research Fellow Research Technician II - Surgery Post-Doc Research Associate Research Technician Explore Dr. GPCR Ecosystem

(May 22 - 26, 2023) 2nd LEAPS Meets Life Sciences Conference. (June 4 - 8, 2023). 2023 Molecular Pharmacology (GRS) Seminar GRC. (June 10 - 11, 2023).

Let’s dive into the Classified GPCR News from April 22nd to 28th, 2024 Adhesion GPCRs Dysfunction of latrophilin 1 (ADGRL1/LPHN1) increases the risk of obesity GPCR Activation and Signaling Variable CGRP family peptide Inflammatory Signaling at the Endosome GPCR Binders, Drugs, and more Discovery and development of macrocyclic peptide for mapping G-protein-coupled receptor agonists Development of a synthetic relaxin-3/INSL5 chimeric peptide Phosphorylation and G-Protein Mediated Signaling Networks June 25 - 29, 2024 | FENS Forum 2024 NEW July 8

Classified GPCR News  Let’s dive into the   Classified GPCR News from September 16th to 22nd, 2024 Industry Issue of Molecular Pharmacology GPCR Events, Meetings, and Webinars September 30 - October 3, 2024 | 22nd Germline mutations in a G protein identify signaling cross-talk in T cells Comparative analysis of formyl peptide receptor 1 and formyl peptide receptor 2 reveals shared and preserved signalling profiles GPCRs in Cardiology Conformational Dynamics and Signaling in Drug Discovery Flavors of GPCR signaling bias Glucagon-like peptide

September 18, 2024 | FREE Webinar - The value of GPCR cell-based assays in drug discovery NEW September 22 , 2024 | Biomolecular Horizons 2024 September 30 - October 3, 2024 | 22nd Discovery on Target October

in your account settings Below is your Classified GPCR News at a glance for January 16th to January 22th Revealing the tissue-level complexity of endogenous glucagon-like peptide-1 receptor expression and signaling (May 22 - 26, 2023) 2nd LEAPS Meets Life Sciences Conference. (June 4 - 8, 2023). 2023 Molecular Pharmacology (GRS) Seminar GRC. (June 10 - 11, 2023).

Endocrine Metabolic GPCRs  Join the Endocrine Metabolic GPCRs event in Birmingham, UK, on April 22-23 Let’s dive into the Classified GPCR News from January 22nd to 28th, 2024 GPCR Activation and Signaling

Check out the weekly Classified GPCR News from October 16th to 22nd, 2023.

Below is your Classified GPCR News at a glance for May 22 to 28, 2023. (June 4 - 8, 2023). 2023 Molecular Pharmacology (GRS) Seminar GRC. (June 10 - 11, 2023).

GPCR Activation and Signaling New simulation insights on the structural transition mechanism of Bovine Protease-activated receptor 2 (PAR2)-targeting peptide derivatives for positron emission tomography ( Structural Understanding of Peptide-Bound G Protein-Coupled Receptors: Peptide-Target Interactions. (May 22 - 26, 2023) 2nd ERNEST Training School. (February 20 - March 3, 2023). GEM2023. Scientist, Drug Metabolism and Pharmacokinetics PhD Opportunity - Investigation Of The Role Of The Formyl Peptide

include 15 receptors involved in regulating body homeostasis and metabolism, and they are activated by peptide movement of the receptor's extracellular domain (ECD), facilitating the partial disengagement of the peptide Graaf, C., et al., Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March Harikumar, K.G., et al., Glucagon-like peptide-1 receptor dimerization differentially regulates agonist ., Lateral allosterism in the glucagon receptor family: glucagon-like peptide 1 induces G-protein-coupled

Structural and Molecular Insights into GPCR Function Insights on the G protein-coupled receptor helix 8 solution structure and orientation using a neurotensin receptor 1 peptide Illuminating the neuropeptide Positive Topline Data from its Phase 2a Obesity Study and Capsule to Tablet PK Study for its Oral Non-Peptide Findings At Endo 2024 For Atumelnant In Two Ongoing, Open-Label Studies For The Treatment Of Congenital Adrenal