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Results found for "Druggable GPCR"
- Advancements in G protein-coupled receptor biosensors to study GPCR-G protein coupling
Biosensors for monitoring G protein-coupled receptors (GPCRs), the most drugged class of proteins in Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Newsletter HERE
- Allosteric modulation of GPCRs: From structural insights to in silico drug discovery
October 2022 "G protein-coupled receptors (GPCRs) play critical roles in human physiology and are one endogenous ligands (orthosteric site), allosteric modulators offer new avenues for the regulation of GPCR Recent advances in the structure determination of GPCRs bound to different types of allosteric modulators In this review, we provide a systematic analysis of the currently available GPCR structures in complex Read more at the source #DrGPCR #GPCR #IndustryNews
- Dr. Josephine (Pina) Cardarelli - Dr. GPCR Podcast
GPCR Podcast, we have Dr. Pina Cardarelli, CSO of GPCR Therapeutics. ecosystem.drgpcr.com/dr-gpcr-podcast/ #gpcr#drgpcr #podcast
- 📅 Dr. GPCR Summit 2022 is less than a month away!
GPCR Summit 2022 is less than a month away! Come live and breathe GPCRs with us and don’t forget to submit your abstract. ➡️https://bit.ly/3Q7hlnT #gpcr #drgpcr
- Dr. Thomas P. Sakmar - Dr. GPCR Podcast
GPCR podcast! Give it a listen to hear from Dr. Thomas P. Sakmar on how the molecular studies of rhodopsin paved the way to understanding #GPCRs Be sure to subscribe https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ #drgpcr #gpcr #podcast
- Residency time of agonists does not affect the stability of GPCR-arrestin complexes
September 2022 "Background and purpose: The interaction of arrestins with G-protein coupled receptors (GPCRs GPCRs that internalize without arrestin have been classified as "class A" GPCRs whereas "class B" GPCRs The interaction of arrestins with GPCRs requires both agonist activation and receptor phosphorylation Read more at the source #DrGPCR #GPCR #IndustryNews
- Statin-induced increase in actin polymerization modulates GPCR dynamics and compartmentalization
regulating the dynamics of the serotonin1A receptor, a crucial neurotransmitter G protein-coupled receptor (GPCR in understanding the modulatory role of the membrane environment on the organization and dynamics of GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews
- The Adhesion GPCR VLGR1/ADGRV1 Regulates the Ca2+ Homeostasis at Mitochondria-Associated ER Membrane
2022 "The very large G protein-coupled receptor (VLGR1, ADGRV1) is the largest member of the adhesion GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Unlock the Hidden Lives of Receptors – Are You Ready?
Imagine you're navigating a vast terrain—not on foot, but through the shape-shifting world of GPCRs.
- In vivo detection of GPCR-dependent signaling using fiber photometry and FRET-based biosensors
By combining fiber photometry with FRET-based biosensors, we were able to track GPCR-dependent signaling Read more at the source #DrGPCR #GPCR #IndustryNews
- Aβ peptides stabilize GPCRs in inactive form and trigger inverse agonism in Alzheimer's disease
August 2022 "Several G-protein coupled receptors (GPCR) are upregulated in Alzheimer's Disease (AD), This article focuses on the role of Aβ granules and their possible interaction with GPCRs that modulate Read more at the source #DrGPCR #GPCR #IndustryNews
- Dr. GPCR Virtual Cafe with Matthew Eddy - New date!
GPCR Virtual Cafe session with Dr. Matthew E. on Friday, October 7th at 1 PM ET.
- Automated micro-plate-based methods for quantifying GPCR activation
Joe Clayton from BioTek Instruments talk about automated micro-plate-based methods for quantifying #GPCR activation. https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #drgpcr #gpcr #virtualcafe
- Ligands can differentially and temporally modulate GPCR interaction with 14-3-3 isoforms
We found that some agonist-induced GPCR/14-3-3 signal intensities can rapidly decrease. could also be paralleled with GPCR/β-arrestin-2 signals, indicating diminished levels of GPCR/signal 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
- GPCR kinase phosphorylation of distal C-tail sites specifies βarrestin1-mediated signaling by...
September 2022 "G protein-coupled receptor (GPCR) kinases (GRKs) and arrestins mediate GPCR desensitization The spatial pattern of GPCR phosphorylation is predicted to trigger these discrete GRK and arrestin-mediated However, although necessary for some GPCRs, we found that distal C-tail sites might not be sufficient to specify recruitment of STAM1 to βarr1 for other GPCRs. Read more at the source #DrGPCR #GPCR #IndustryNews
- The Perils and Guardrails of Modifying Signalling Proteins in Bioassays
in which, the allosteric nature of GPCRs must be respected. Biased Allosteric Modulators: New Frontiers in GPCR Drug Discovery. Mini G protein probes for active G protein-coupled receptors (GPCRs) in live cells. Mini-G proteins: Novel tools for studying GPCRs in their active conformation. Cryo-EM structures of GPCRs coupled to Gs, Gi and Go.
- Pharmacologic Models
GPCR News. Elevate your pharmacology expertise. Unlock "Pharmacologic Models" now
- Confo Therapeutics receives €1.7 million VLAIO grant for further research on GPCR modulators for ...
July 2022 Confo Therapeutics receives €1.7 million VLAIO grant for further research on GPCR modulators The grant should help expand Confo Therapeutic’s research on G protein-coupled receptor (GPCR) drug candidates . " Read more at the source #DrGPCR #GPCR #IndustryNews
- Biased GPCR signaling by the native parathyroid hormone-related protein 1 to 141 relative to its...
September 2022 Biased GPCR signaling by the native parathyroid hormone-related protein 1 to 141 relative understanding on how endogenous PTHrP transduces signals through its cognate G-protein coupled receptor (GPCR understanding of the biased signaling process of a native protein hormone acting in conjunction with a GPCR 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 However, the selectivity of SNARE complex proteins to regulate the release of different types of GPCRs /vesicle-associated-membrane-protein-2-is-a-cargo-selective-v-snare-for-a-subset-of-gpcrs #GPCR #DrGPCR
- Feeder or trigger – CCR2 as a scavenger and regulator of cell migration
Although some GPCRs constitutively internalize through clathrin-coated pits independently of phosphorylation In this study, it is revealed that CCR2 scavenging role was largely independent of the classical GPCR Check the original article at https://pubmed.ncbi.nlm.nih.gov/36719944/ #GPCR #DrGPCR#Ecosystem
- Structural insights into adhesion GPCR ADGRL3 activation and Gq, Gs, Gi, and G12 coupling
November 2022 "Adhesion G-protein-coupled receptors (aGPCRs) play key roles in a diversity of physiologies A hallmark of aGPCR activation is the removal of the inhibitory GAIN domain and the dipping of the cleaved The structures also reveal the uncharted structural information of GPCR/G12 coupling. Taken together, our study lays the groundwork for understanding aGPCR activation and G-protein-coupling Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE
- 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, Secure your spot today and dive into the evolving world of GPCRs! 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
- 📰 GPCR Weekly Buzz: Exciting Schedule Shifts for Principles of Pharmacology I & II | August 12-18, 2024
Dear GPCR Community, Before diving into this week's news, prepare for an incredible learning journey! GPCR Event Spotlight 11th Adhesion GPCR Workshop Location: Mexico City Dates: October 23-25, 2024 Join us to connect with peers and explore cutting-edge adhesion GPCR biology. 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
- Breaking the Myth of High and Low Affinity Sites
The interpretation of high and low affinity binding sites on GPCRs. Unlock “Rethinking Affinity” Now Only in Terry's Corner _____ #GPCR #BindingAffinity #Pharmacology
- Join Us Today!
GPCR Ecosystem is under construction and dozens of your colleagues are enjoying its benefits! Catch up with the latest #GPCR news, start a discussion in the forum, and much more today! Join the #GPCR movement by becoming a site member for FREE! ➡️ https://www.ecosystem.drgpcr.com/ #gpcr #drgpcr
- 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.
- Glyco-sulfo hotspots in the chemokine receptor system
Check the original article at https://pubmed.ncbi.nlm.nih.gov/36729338/ #GPCR #DrGPCR#Ecosystem
- 📰 Breaking Down the Latest GPCR Discoveries: a Weekly Update (Nov 27-Dec 3, 2023)
Discover our comprehensive coverage of GPCRs, We welcome GPCR paper suggestions! GPCR Podcast featuring Dr. Neil Grimsey and Dr. Katarzyna Marcinkiewicz. in Neuroscience Targeting sensory neuron GPCRs for peripheral neuropathic pain GPCRs in Oncology and Insights into GPCR Function Fully activated structure of the sterol-bound Smoothened GPCR-Gi protein GPCR Ecosystem
- The integrin ligand SVEP1 regulates GPCR-mediated vasoconstriction via integrins α9β1 and α4β1
Read more at the source #DrGPCR #GPCR #IndustryNews












