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In this review, we focus on recent advances in G-protein-coupled receptor (GPCR) targets.

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/ and potential therapeutic targets that are activated by the same endogenous ligand, create a wide diversity #GPCR #DrGPCR

March 2022 "Geneva, Switzerland, March 7, 2022 – Addex Therapeutics (SIX: ADXN, Nasdaq: ADXN), a clinical-stage media at 16:00 CET (15:00 GMT / 10:00 EST / 07:00 PST) the same day. " Read more at the source #DrGPCR #GPCR

Peter joined Tectonic to help chart new territory in GPCR science. We’re glad to have Peter's dedication, experience, and passion in building innovative therapeutics." Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 Karuna Therapeutics Announces Positive Results from Phase 3 EMERGENT-2 Trial of KarXT in Schizophrenia "BOSTON--(BUSINESS WIRE)--Aug. 8, 2022-- Karuna Therapeutics, Inc. Read more at the source #DrGPCR #GPCR #IndustryNews

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 Biology; Domain Therapeutics patents new PAR2 antagonists. 🔍 This Week in Dr. 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.

GPCR podcast! 🥁 Drum rolls, please! Our guest is the wonderful Dr. Rosie Dawaliby! GPCR Ecosystem paid membership ➡️ https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ep-84-with-rosie-dawaliby #gpcr #drgpcr

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

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

April 2022 Addex Therapeutics Completes Patient Enrollment For Dipraglurant Blepharospasm Phase 2 Clinical Study "Geneva, Switzerland, April 13, 2022 - Addex Therapeutics Ltd (SIX: ADXN, Nasdaq: ADXN), a clinical-stage Read more at the source #DrGPCR #GPCR #IndustryNews

December 2021 "30/11/2021 Confo will work together with Regeneron to apply its GPCR drug discovery platform VIB spin-off Confo Therapeutics today announced that it has entered into a collaborative agreement with technology platform, which uses conformationally selective VHH antibodies – ConfoBodies® – to stabilize GPCRs in disease-relevant conformations, will be applied with the goal of enabling the discovery of novel therapeutic antibody drug candidates. " Read more at the source #DrGPCR #GPCR #IndustryNews

GPCR Summit 2022. Mark your calendar for October 10th and 16th. ➡️ https://www.ecosystem.drgpcr.com/ #gpcr #drgpcr

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

G protein-coupled receptors (GPCRs) are among the most promising drug targets. Specifically controlling the activity of GPCR dimers with ligands is a good approach to clarify their This region corresponds to the sodium ion binding site in class A GPCRs that controls the basal state reveal the possibility of developing allosteric compounds able to specifically modulate the activity of GPCR

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Chemokine receptors (CKRs) belong to a subfamily of G-protein-coupled receptors (GPCRs) and play a crucial helix (TM7) near ECL3, while the other links TM3 with ECL2, which is common to the broader class A GPCR In addition, it has a glutamate residue at position 3.45, which is not found in human class A GPCRs, binding and receptor activation will pave the way for significant advancements in the development of therapeutics Check the original article at https://pubmed.ncbi.nlm.nih.gov/37212620/ #GPCR #DrGPCR #Ecosystem

August 2022 "Geneva, Switzerland, August 18, 2022 - Addex Therapeutics (SIX and Nasdaq: ADXN), a clinical-stage Read more at the source #DrGPCR #GPCR #IndustryNews

are pursuing AI-driven drug discovery to explore new functional chemical space and precision-engineer therapeutics with enhanced potency and tailored signaling against an undrugged GPCR target. #ai #drugdiscovery #gpcr" Read more at the source #DrGPCR #GPCR #IndustryNews

This approach reveals: Hidden target overlap New therapeutic hypotheses “Off-target” effects that may GPCRs are not simple on/off switches. This reroutes discovery toward: Functionally selective ligands Better therapeutic windows More predictable What matters now is not the category , but the fit: Does the chemical matter support the therapeutic GPCR innovation is accelerating.

March 2022 Confo Therapeutics Doses First Subjects In Phase 1 Clinical Trial Of CFTX-1554 For The Treatment Confo’s first drug candidate moves into clinical development — Ghent, Belgium – March 10, 2022 – Confo Therapeutics , a leader in the discovery of medicines targeting G-protein coupled receptors (GPCRs), today announced pharmacokinetics of CFTX-1554 in healthy subjects (NCT05260658). " Read more at the source #DrGPCR #GPCR

December 2021 "Geneva, Switzerland, December 17, 2021 – Addex Therapeutics Ltd (SIX: ADXN and Nasdaq: Read more at the source #DrGPCR #GPCR #IndustryNews

In his collaboration with David Hodson, every major leap—from early ligand design to GPCR visualization Throughout his own journey—from organic chemistry to chemical biology to GPCR imaging—every pivotal step  🎧 Listen to the full episode https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/chemical-probes-for-gpcr-imaging-and-internalization

demonstrate that the chemoreceptor genes, srg-36 and srg-37, which encode G protein-coupled receptors (GPCRs Here, we show that SRG-36 and SRG-37 act as upstream GPCRs that activate EGL-30. SRG-36 and SRG-37 are GPCRs for the dauer-inducing ascaroside, ascr#5. Thus, ascaroside signaling promotes axon regeneration by activating the GPCR-Gqα pathway.

November 2022 "Some G protein-coupled receptor (GPCR) ligands act as "biased agonists" that preferentially Although GPCRs are primarily found at the plasma membrane, GPCRs can traffic to and signal from many subcellular signaling contributes to the biased signaling generated by three endogenous ligands of the GPCR observed at CXCR3, which has important implications for drugs targeting chemokine receptors and other GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE

July 2022 "Ad Hoc Announcement Pursuant to Art. 53 LR Geneva, Switzerland, July 22, 2022 – Addex Therapeutics issuance and will expire five years from their date of issuance. " Read more at the source #DrGPCR #GPCR

October 2022 "G protein-coupled receptors (GPCRs) are of considerable interest due to their importance physiological functions and in a large number of Food and Drug Administration (FDA)-approved drugs as therapeutic signaling effectors: heterotrimeric G proteins, GPCR kinases (GRKs), and β-arrestins. As new technologies are developed and applied to studying GPCR structure and their downstream effectors Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

GPCRs  are one of the most important families  of therapeutic   targets  in the pharmaceutical industry mechanism behind C5a and C5aR interaction is of high interest for the development of novel immunological therapeutics fluorescent probes have proven to be optimal tools to perform fluorescence-based assays to unlock the therapeutic Trends in GPCR Drug Discovery: New Agents, Targets and Indications. Function, Structure and Therapeutic Potential of Complement C5a Receptors.

The pace of GPCR innovation is accelerating—teams acting on today’s insights will set tomorrow’s standards

signaling is transduced by a multikinase-dependent switch controlling the apico-basal distribution of the GPCR smoothened "The oncogenic G-protein-coupled receptor (GPCR) Smoothened (SMO) is a key transducer of of HH to the apico-basal distribution of SMO and provide a novel mechanism for the regulation of a GPCR Read more at the source #DrGPCR #GPCR #IndustryNews