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- GPCR News Flash! Top Updates You Can't-Miss! + University CheatSheet is finally available! ❄ Dec 2 - 8, 2024
Hello, hello GPCR Buddies! It's starting to look a lot like Christmas at Dr. GPCR! 🎉 Conformational coupling between extracellular and transmembrane domains modulates holo-adhesion GPCR Don't get left in the dust—upgrade now and keep your GPCR gossip game strong! Classified GPCR News Let’s dive into the Classified GPCR News from December 2nd to 8th, 2024 Industry function GPCR Activation and Signaling P2X7R-primed keratinocytes are susceptible to apoptosis via GPCR-Gβγ-pERK
- Genome-wide identification of 216 G protein-coupled receptor (GPCR) genes from the marine water ...
Genome-wide identification of 216 G protein-coupled receptor (GPCR) genes from the marine water flea Diaphanosoma celebensis G protein-coupled receptors (GPCRs) are considered to have originated from early evolution of eukaryotic species, therefore, the genome-wide identification of GPCR genes can provide Here, we identified a total 216 full-length GPCR genes in the marine water flea Diaphanosoma celebensis In this study, these results may provide a better understanding on the evolution of GPCRs, and expand
- Pharmacophore-guided Virtual Screening to Identify New β 3 -adrenergic Receptor Agonists
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- The Impact of CB1 Receptor on Nuclear Receptors in Skeletal Muscle Cells
Quantitative real-time probe-based polymerase chain reaction (qRT-PCR) assays are deployed in order to This can be deduced from the qRT-PCR assays; triggering CB1 receptors amplifies both NR4A1 and NR4A3 Read more at the source #DrGPCR #GPCR #IndustryNews
- Dynamic recognition of naloxone, morphine and endomorphin1 in the same pocket of µ-opioid receptors
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- Actions of Parathyroid Hormone Ligand Analogues in Humanized PTH1R Knockin Mice
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- Differential binding of Δ9-tetrahydrocannabinol derivatives to type 1 cannabinoid receptors (CB1)
Introduction Cannabinoid receptors are GPCRs, and two main types exist, CB1R and CB2R. for CB1R in live cells and the PHERAstar FSX is the ideal microplate reader for characterizing the GPCR-ligand
- Glyco-sulfo hotspots in the chemokine receptor system
Check the original article at https://pubmed.ncbi.nlm.nih.gov/36729338/ #GPCR #DrGPCR#Ecosystem
- Structural perspectives on the mechanism of signal activation, ligand selectivity and allosteric...
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- Structural dynamics of Smoothened (SMO) in ciliary membrane and its interaction with membrane lipids
September 2022 "The Smoothened receptor (SMO, a 7 pass transmembrane domain, Class F GPCR family protein Read more at the source #DrGPCR #GPCR #IndustryNews
- Design and validation of recombinant protein standards for quantitative Western blot analysis of...
antibody-antigen interaction-based approaches for quantitative analysis of G protein-coupled receptor (GPCR GPCRs in general and cannabinoid CB1 receptor in particular show a progressive tendency to aggregate This renders full-length recombinant GPCRs useless for analytical purposes, a problem that can be overcome Read more at the source #DrGPCR #GPCR #IndustryNews
- Mechanism of enhanced sensitivity of mutated β-adrenergic-like octopamine receptor to amitraz in...
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- GPR84 signaling promotes intestinal mucosal inflammation via enhancing NLRP3 inflammasome activation
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- A robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery.
GPCRs are not suitable for antibody use due to steric hindrance and reverse binding, thus, other strategies This modification is small enough to not affect GPCR expression or activity.[21–23] The Tag-lite® binding It has been applied to different GPCR binding assays, such as CXCR4, opioid receptors, CCK1 and CCK2. Protein-Protein Interaction Analysis with Time-Resolved FRET and Snap-Tag Technologies: Application to GPCR
- Regulator of G Protein Signaling 20 Correlates with Long Intergenic Non-Coding RNA (lincRNAs)...
Interestingly, RGS (Regulators of G protein signaling) proteins, which negatively regulate GPCR signaling Read more at the source #DrGPCR #GPCR #IndustryNews
- Dopamine activates astrocytes in prefrontal cortex via α1-adrenergic receptors
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- Divergent roles for the gut intraepithelial lymphocyte GLP-1R in control of metabolism, microbiota..
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- Cell-Type-Specific Effects of the Ovarian Cancer G-Protein Coupled Receptor (OGR1) on Inflammation..
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- Differences across sexes on head-twitch behavior and 5-HT2A receptor signaling in C57BL/6J mice
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- Integrative model of the FSH receptor reveals the structural role of the flexible hinge region
receptor (FSHR) belongs to the glycoprotein hormone receptors, a subfamily of G-protein-coupled receptors (GPCRs models are expected to allow for testable hypotheses about signal transduction and drug development for GPHRs Read more at the source #DrGPCR #GPCR #IndustryNews
- GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between ...
GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between Health and Disease GPCRs arguably represent the most effective current therapeutic targets for a plethora of GPCRs also possess a pivotal role in the regulation of the physiological balance between healthy and changes in organismal tissue complexity and compartmentalization, thus enabling a nuanced GPCR-based GPCRs have been long considered as controllers of communication between tissues and cells.
- TRPM3 in the eye and in the nervous system - from new findings to novel mechanisms
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- Decoding β-Arrestins: from Structure to function
Fine-tuning GPCR signaling: conformational dynamics and intracellular responses GPCR signaling is a complex Apart from G proteins, GPCRs engage other effectors for signaling modulation. GPCR kinases (GRKs) and β-arrestins are activated by agonist-bound GPCRs and interact with the receptor The diversity in GPCR signaling regulation suggests an individualized control mechanism. Recent years have seen cryo-EM dominate new GPCR structure determinations, offering insight into GPCR-effector
- TM5-TM6: structural switches that modulate the coupling of serotonin receptors to Gs or Gi
What is the molecular basis that determines that GPCRs bind selectively or promiscuously to different The discovery of the orthosteric binding pocket is of great importance in GPCRs field as it supports Additionally, structural analysis of the TM5 and TM6 regions of 27 class A GPCRs coupled to Gs or Gi/ 2.6 ± 1.6 residues shorter, concluding that the TM5-TM6 macro-switch length is conserved in class A GPCRs #GPCR #DrGPCR
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GPCR Summit from October 10th to the 16th is taking shape. GPCR Ecosystem site member, which is free! Sign up now ➡️ https://bit.ly/3eaO5PH #gpcr #drgpcr
- Join Us Now!
GPCR Summit 2022. This is a great opportunity for us to come together and talk GPCRs. Join us now ➡️ https://www.ecosystem.drgpcr.com/dr-gpcr-summit-2022 #gpcr #drgpcr
- Irreversible Drugs, Real Control: Design for Durable Target Engagement
Molecular innovation This Week’s GPCR Intelligence: The next edge in discovery isn’t louder exposure—it Breakthroughs this week: nanomedicines targeting PAR2 for sustained analgesia; Emerging Voices in GPCR GPCR Premium: Sneak Peek Industry insights: Confo VLAIO grant; Skye CB1 Ph2 miss; Chugai CT-388 in-license Upcoming events: Membrane-mimetic screening; GPCR Forum 2025; GPCR-TDD Summit Europe. Enjoy Over 50% Discount at Checkout Get Yearly Access On-Demand Now — Free 7 Day Trial ➤ DrGPCR Podcast
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GPCR Summit 2022. Mark your calendar for October 10th and 16th. ➡️ https://www.ecosystem.drgpcr.com/ #gpcr #drgpcr
- Let’s work better together!
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- β-arrestin1 promotes tauopathy by transducing GPCR signaling, disrupting microtubules and autophagy
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
