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By combining fiber photometry with FRET-based biosensors, we were able to track GPCR-dependent signaling Read more at the source #DrGPCR #GPCR #IndustryNews

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

Topics cover new cellular assays, real-time kinetics, and unique GPCR behaviors. GPCR Event Spotlight    11th Adhesion GPCR Workshop    Location:  Mexico City Dates:  October 23-25, 2024 Connect with peers and delve into cutting-edge adhesion GPCR biology. Let’s dive into the   Classified GPCR News  from August 19th to 25th, 2024 GPCR Activation and Signaling Papers NEW Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events,

that the affinity of Fzd for Dvl was not affected by Wnt ligands, in contrast to other members of the GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

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network located on intracellular loop 2 that is subject to RNA editing, which differentially affects GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

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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

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

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

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2022 Sosei Heptares and Kallyope Enter Collaboration to Identify and Validate Novel Gastrointestinal GPCR the Sosei Heptares compound library for its industry-leading biology platform to identify potential GPCR entered a strategic research collaboration to identify and validate novel G protein-coupled receptor (GPCR drug discovery programs in the area of gastrointestinal diseases. " Read more at the source #DrGPCR #GPCR

February 2022 Septerna emerges with $100M to spark 'second golden age' of prolific drug target GPCR with Better known as GPCR, the fruitful research space has led to more than 700 approved drugs over previous The company's co-founder, GPCR pioneer and Nobel laureate Robert Lefkowitz, M.D., has 50 years of experience Read more at the source #DrGPCR #GPCR #IndustryNews

The interpretation of high and low affinity binding sites  on GPCRs.   Unlock “Rethinking Affinity” Now Only in Terry's Corner _____ #GPCR #BindingAffinity #Pharmacology

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

GPCR Weekly News Free Edition—your clear, credible signal in a noisy field. GPCR Forum to Biophysics; plus targeted summits for discovery teams planning 2025–2026. GPCR members save  50%+  (check your Weekly News code). Speed:  faster GPCR target validation and assay development. The pace of GPCR innovation is accelerating.

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.

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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

are small-lipidated peptides designed from the intracellular loops of G protein-coupled receptors (GPCRs ) that act in an allosteric manner to modulate the activity of GPCRs. the past 2 decades, pepducins have progressed initially from pharmacologic tools used to manipulate GPCR To date, pepducins designed from numerous GPCRs have been studied for their impact on pathologic conditions Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "Understanding the activation of G protein-coupled receptors (GPCRs) is of paramount importance Although many cardiovascular GPCRs have been extensively studied as model receptors for decades, new As a result, there is an ongoing need to develop novel approaches to monitor and to modulate GPCR activation nanobodies have been adopted to elucidate the structure, pharmacology, and signaling of cardiovascular GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews

transcription is endocytosis-dependent in primary hepatocytes "A number of G protein-coupled receptors (GPCRs activation by glucagon within 5 min and transit via EEA1-marked endosomes shown previously to be sites of GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

release of these hormones in the adrenals is tightly regulated by adrenal G protein-coupled receptors (GPCRs In this review, we discuss important aspects of adrenal GPCR signaling and regulation, as they pertain modulation of cardiac function in the context of chronic HF, by focusing on the 2 best studied adrenal GPCR the β-arrestins in the adrenals, 2 protein families that regulate the signaling and functioning of GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "The cannabinoid CB1 receptor is the most abundant G protein coupled receptor (GPCR) in Guided Pharmacology of Membrane Proteins (BJP 75th Anniversary). " Read more at the source #DrGPCR #GPCR

GPCR podcast with Dr. Nicole (Nicki) Perry-Hauser is now available What a fun chat! GPCR Ecosystem paid membership to enjoy everything Dr. GPCR has! ➡️https://bit.ly/3TCJVQQ #gpcr #drgpcr

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 In the same way, as in other GPCRs-G protein complexes, the structural analysis revealed that electrostatic Additionally, structural analysis of the TM5 and TM6 regions of 27 class A GPCRs coupled to Gs or Gi/ #GPCR #DrGPCR

August 2022 RAB-Symposium - Regulatory Autoantibodies Targeting GPCRs. September 15-16, 2022. GPCRs are involved in a variety of physiological and pathophysiological processes. So far, numerous therapeutics targeting GPCRs have been developed, with a focus on small molecules and Recently, functional autoantibodies targeting GPCRs have been associated with various disease-specific Read more at the source #DrGPCR #GPCR #IndustryNews

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#biotech #lifesciences #appointment #GPCR #Oncology" Read more at the source #DrGPCR #GPCR #IndustryNews

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