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- New Resources in GPCRdb
GPCR on the 24th of June! This time, the GPCRdb team ( Dr. David Gloriam , Dr. demonstrate the newest resources of the GPCRdb: 1) the new G protein resources and 2) the structural analysis platform Reserve your spot for free at: https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #GPCR #GPCRs #DrGPCR
- GRK2 in cardiovascular disease and its potential as a therapeutic target
G protein-coupled receptors (GPCRs) are critical myocardial signal transducers which regulate cardiac Additionally, GPCR dysregulation underlies multiple models of cardiac pathology, and most pharmacological A recent focus on GPCR intracellular-regulating proteins such as GPCR kinases (GRKs) has uncovered GRK2 These data support the premise that GRK2 should be at the forefront of a novel investigative drug search Read more at the source #DrGPCR #GPCR #IndustryNews
- Arginine 125 Is an Essential Residue for the Function of MRAP2
Read more at the source #DrGPCR #GPCR #IndustryNews
- Dual loss of regulator of G protein signaling 2 and 5 exacerbates ventricular myocyte arrhythmias...
essential to maintaining proper cardiac output and circulation, is regulated by G protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Emerging approaches for decoding neuropeptide transmission
processing, release from dense core vesicles, and ability to activate G-protein-coupled receptors (GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE
- GPCRS: AN ODYSSEY FROM STRUCTURE, SIGNALING AND REGULATION TO THERAPEUTICS
meeting is to bring together a highly interdisciplinary group of scientists to exchange new experimental data Spatial-temporal signaling of GPCRs and physiological functions; 2. GPCRs as environmental sensors; 3. New approaches to GPCR drug discovery. This timely meeting will not only provide an inclusive forum for communication, but also a platform for
- G protein-coupled receptor kinase type 2 and β-arrestin2: Key players in immune cell functions...
representative proteins that regulate the transduction and trafficking of G protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Comparative study of neuropeptide signaling systems in Hemiptera
Here, 33 neuropeptide precursors and 48 putative neuropeptide G protein-coupled receptor (GPCR) genes Read more at the source #DrGPCR #GPCR #IndustryNews
- Fusion protein strategies for cryo-EM study of G protein-coupled receptors
microscopy (cryo-EM) is used extensively to determine structures of activated G protein-coupled receptors (GPCRs However, applying it to GPCRs without signaling proteins remains challenging because most receptors lack In GPCR crystallography, inserting a fusion protein between transmembrane helices 5 and 6 is a highly The fusion strategies explored here are likely applicable to cryo-EM interrogation of other GPCRs and Read more at the source #DrGPCR #GPCR #IndustryNews
- 📰 GPCR Weekly Buzz: Exciting Schedule Shifts for Principles of Pharmacology I & II | August 12-18, 2024
miss out on insightful resources like ' Applying Pharmacology to Drug Discovery ' and ' Advanced Data Analysis for GPCR Pharmacology .' GPCR Event Spotlight 11th Adhesion GPCR Workshop Location: Mexico City Dates: October 23-25, Let’s dive into the Classified GPCR News from August 12th to 18th, 2024 Adhesion GPCRs Heterogeneity screening using Spectral Shift for GPCRs October 23 - 25, 2024 | 11th Adhesion GPCR Workshop November
- Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell...
Originally, β-arrestins were identified for their contribution to GPCR desensitization to agonist-mediated However, current investigations have now recognized that in addition to GPCR arresting (hence the name Read more at the source #DrGPCR #GPCR #IndustryNews
- GASP1 enhances malignant phenotypes of breast cancer cells and decreases their response to...
Read more at the source #DrGPCR #GPCR #IndustryNews
- Opposite Effects of Src Family Kinases on YAP and ERK Activation in Pancreatic Cancer Cells...
Previously, we identified potent positive crosstalk between insulin/IGF-1 receptors and G protein-coupled (GPCR Here, we show that a combination of insulin and the GPCR agonist neurotensin induced rapid activation Read more at the source #DrGPCR #GPCR #IndustryNews
- The expression and clinical significance of GPR39 in colon cancer
GPR39 is a GPCR which can interact with Zn and modulate the colonocytes' survival. study, we compared GPR39 expression between colon cancers and tumor-adjacent tissues by retrieving TCGA data of several other biomarkers including PPARG, EPCAM, and PD-L1 was investigated by re-analyzing TCGA data , qPCR, and IHC. Read more at the source #DrGPCR #GPCR #IndustryNews
- GRK2 selectively attenuates the neutrophil NADPH-oxidase response triggered by β-arrestin recruiting
pro-inflammatory neutrophil response, signaling downstream of an agonist-activated G protein-coupled receptor (GPCR Among the family of GPCR kinases (GRKs) that regulate receptor phosphorylation and signaling termination analysis of subcellular fractions revealed a cytosolic localization. " Read more at the source #DrGPCR #GPCR
- Nuclear localization of histamine receptor 2 in primary human lymphatic endothelial cells
we report the subcellular localization of histamine receptor 2 (H2R), a G protein-coupled receptor (GPCR A growing number of GPCRs have been shown to be localized in the nucleus and contribute toward transcriptional At the same time, H2R as a GPCR imparts many unresolved questions, such as the functional relevance of In this aspect, our present data shed new light on the unexplored H2R signaling mechanisms. Read more at the source #DrGPCR #GPCR #IndustryNews
- The NPXXY Motif Regulates β-Arrestin Recruitment by the CB1 Cannabinoid Receptor
August 2022 "Background: Activation of signaling effectors by G-protein coupled receptors (GPCRs) depends participate in a molecular mechanism to trigger β-arrestin recruitment. " Read more at the source #DrGPCR #GPCR
- G protein coupling and activation of the metabotropic GABAB heterodimer
September 2022 "Metabotropic γ-aminobutyric acid receptor (GABABR), a class C G protein-coupled receptor (GPCR However, little is known about the mechanism for GP coupling and activation for class C GPCRs. This mechanism provides fresh insights into the mechanistic details of class C GPCRs activation expected Read more at the source #DrGPCR #GPCR #IndustryNews
- Adenosine receptor signalling in Alzheimer's disease
Emerging evidence suggests adenosine G protein-coupled receptors (GPCRs) are promising therapeutic targets Read more at the source #DrGPCR #GPCR #IndustryNews
- Endothelin-1 Stimulates PAI-1 Protein Expression via Dual Transactivation Pathway Dependent ROCK...
In addition, as an intermediary of G protein-coupled receptor (GPCR) signaling, the functions of ROCK Read more at the source #DrGPCR #GPCR #IndustryNews
- Adenosine receptor signalling in Alzheimer's disease
Emerging evidence suggests adenosine G protein-coupled receptors (GPCRs) are promising therapeutic targets Read more at the source #DrGPCR #GPCR #IndustryNews
- VAMP2: a crucial player in the delivery of MOR to the synapse
Transporting Protein-coupled receptors (GPCRs) to the synapse, where they are involved in neurotransmission From a general overview, after GPCRs synthesis in the endoplasmic reticulum, GPCRs are transported to In the context of GPCR recycling, this process is complex and highly regulated that involves multiple These data are fascinating because in the case of MOR, which is a receptor with several splicing variants /vesicle-associated-membrane-protein-2-is-a-cargo-selective-v-snare-for-a-subset-of-gpcrs #GPCR #DrGPCR
- Orion Shares New Data on its Latest Best-in-Class Drug Candidate
), today announced that it will be presenting important new data at both LSX World Congress and TIDES His presentations will describe Orion’s drug discovery platform, one of the fastest drug discovery solutions in the industry for targeting peptidergic GPCRs. Hartley will also present new data on Orion’s CCR2 antagonist, OB-004, demonstrating the ability of this powerful platform to rapidly identify best-in-class GPCR drug candidates."
- GPCR Updates: Celebrating Breakthroughs, New Course Launches Soon, and Exclusive Discounts! | Aug 26 - Sep 1, 2024
Hello GPCR Community, Stay up-to-date with the latest GPCR research, including breakthrough studies, protein-coupled receptor structural landscape: Major milestones and future directions . 🎉 New Course Dates GPCR Event Spotlight Discovery on Target’s 19th Annual GPCR-Based Drug Discovery Targeting G Protein-Coupled Classified GPCR News Let’s dive into the Classified GPCR News from August 26th to September 1st, 2024 Papers Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings
- Comparative studies of AlphaFold, RoseTTAFold and Modeller: a case study involving the use of...
G-protein-coupled receptor (GPCR) proteins are particularly interesting since they are involved in numerous work directly compares the performance of these novel deep learning-based protein modeling methods for GPCRs We collected the experimentally determined structures of 73 GPCRs from the Protein Data Bank. Read more at the source #DrGPCR #GPCR #IndustryNews
- GPR110, a receptor for synaptamide, expressed in osteoclasts negatively regulates osteoclastogenesis
Although some G-protein coupled receptors (GPCRs) were reported to play roles in osteoblast function, GPR110 belongs to adhesion GPCR and was the functional receptor of N-docosahexaenoyl ethanolamine (also Read more at the source #DrGPCR #GPCR #IndustryNews
- Developing the Cannabinoid Receptor 2 (CB2) pharmacopoeia: past, present, and future
October 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, Promising preclinical data supports the applicability of CB2 activation in autoimmune and inflammatory Read more at the source #DrGPCR #GPCR #IndustryNews
- GPCR voltage dependence controls neuronal plasticity and behavior
G-protein coupled receptors (GPCRs) play a paramount role in diverse brain functions. Almost 20 years ago, GPCR activity was shown to be regulated by membrane potential in vitro, but whether the voltage dependence of GPCRs contributes to neuronal coding and behavioral output under physiological Here we show that muscarinic GPCR mediated neuronal potentiation in vivo is voltage dependent. crucial involvement of GPCR voltage dependence in neuronal plasticity and behavior.
- Developing the Cannabinoid Receptor 2 (CB2) pharmacopeia: past, present, and future
August 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, though Promising preclinical data support the applicability of CB2 activation in autoimmune and inflammatory Read more at the source #DrGPCR #GPCR #IndustryNews
- Targeting mGluR2/3 for treatment of neurodegenerative and neuropsychiatric diseases
Read more at the source #DrGPCR #GPCR #IndustryNews



