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November 2021 "Nov. 15, 2021 LONDON – There’s not yet proof of the pudding, but Omass Therapeutics Ltd .’s new structure-based technology has passed a key test, in enabling the discovery of orally available

December 2021 "Geneva, Switzerland, December 17, 2021 – Addex Therapeutics Ltd (SIX: ADXN and Nasdaq:

Therapeutic potential of opioid receptor heteromers in chronic pain and associated comorbidities. Structural and Molecular Insights into GPCR Function Predicted Three-Dimensional Structure of the GCR1 Structural insights into constitutive activity of 5-HT6 receptor. Industry News Confo Therapeutics Enters into Collaboration Agreement with Daiichi Sankyo to Discover Therapeutics Reports Fourth Quarter and Full Year 2022 Financial Results and Recent Highlights Salipro

October 2022 "We describe production of the human A2A adenosine receptor (A2AAR), a class A G protein-coupled receptor (GPCR) for 19F-NMR and single-molecule fluorescence (SMF) spectroscopy. We explain in detail steps shared between the two sample preparation strategies, including expression and isolation of A2AAR and assembly of A2AAR in lipid nanodiscs and procedures for incorporation of either 19F-NMR or fluorescence probes. Protocols for SMF experiments include sample setup, data acquisition, data processing, and error analysis. For complete details on the use and execution of this protocol, please refer to Wei et al. (2022) and Sušac et al. (2018)." Read more at the source #DrGPCR #GPCR #IndustryNews

July 2022 "Ad Hoc Announcement Pursuant to Art. 53 LR Geneva, Switzerland, July 22, 2022 – Addex Therapeutics

Odorant G protein-coupled receptors as potential therapeutic targets for adult diffuse gliomas: a systematic Glioma is the most common adult malignant brain tumor and requires novel therapeutic strategies to improve genomic and transcriptomic profiles of ORs in glioma, we suggest that ORs are potential biomarkers and therapeutic

October 2022 Mechanism of enhanced sensitivity of mutated β-adrenergic-like octopamine receptor to amitraz in honeybee Apis mellifera: An insight from MD simulations "Background: Amitraz is one of the critical acaricides/insecticides for effective control of pest infestation of Varroa destructor mite, a devastating parasite of Apis mellifera, because of its low toxicity to honeybees. Previous assays verified that a typical G protein-coupled receptor, β-adrenergic-like octopamine receptor (Octβ2R), is the unique target of amitraz, but the honeybee Octβ2R resists to amitraz. However, the underlying molecular mechanism of the enhanced sensitivity or toxicity of amitraz to mutated honeybee Octβ2RE208V/I335T/I350V is not fully understood. Here, molecular dynamics simulations are employed to explore the implied mechanism of the enhanced sensitivity to amitraz in mutant honeybee Octβ2R." Read more at the source #DrGPCR #GPCR #IndustryNews

June 2022 "G protein-coupled receptors (GPCRs) represent a major therapeutic target class as they play In 2019, 5 out of 20 first-in-class approved therapeutic agents targeted GPCRs.

Modulator Research Collaboration for Substance Use Disorders "Geneva, Switzerland, August 15, 2022 - Addex Therapeutics

Allosteric Modulator Pharmacology to Treat Dyskinesia and Other Movement Disorders with Tim Dyer Addex Therapeutics "Tim Dyer is the Co-Founder and CEO of Addex Therapeutics, which is focusing on the pharmacology known

Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, though as yet unrealised, therapeutic

Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, though as yet unrealized, therapeutic

Phase 1 studies in Japan with JNJ-40411813 (ADX71149) "Geneva, Switzerland, November 15, 2021 – Addex Therapeutics

Screening Platform Ad Hoc Announcement Pursuant to Art. 53 LR Geneva, Switzerland, April 6, 2022 - Addex Therapeutics

Orchestrate the Interface between Health and Disease GPCRs arguably represent the most effective current therapeutic Given the tremendous success of GPCRs as therapeutic targets, considerable focus has been placed on the ability of these therapeutics to modulate diseases by acting at cell surface receptors.

and the complexity of the central nervous system (CNS) pose a challenge for developing successful therapeutics Emerging GPCR Therapeutic Targets in CNS Drug Discovery GPCRs have been studied for decades, but there Of the traditional GPCRs, CBRs are gaining ground as potential therapeutic targets in several CNS diseases One of the best tools to study therapeutic targets are fluorescent ligands , which are very useful in G-Protein-Coupled Receptors in CNS: A Potential Therapeutic Target for Intervention in Neurodegenerative

It was early structure-based pharmacology. Dr. This approach reveals: Hidden target overlap New therapeutic hypotheses “Off-target” effects that may They are structural strategies for tuning physiology. 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

tumor progression Methods & Updates in GPCR Research GPCR Signaling: A Study of the Interplay Between Structure into schizophrenia pipeline GPCR Dynamics Reveal Mechanisms for Drug Discovery DMS: Linking Protein Structure To Function AbbVie Completes Acquisition of Cerevel Therapeutics Nxera Pharma attended the Drug Discovery Ecosystem Summit Tectonic Therapeutic Announces Closing of Merger with AVROBIO as well as Concurrent Private Placement of $130.7 Million Tectonic Therapeutic Announces US IND Clearance for Lead Program

insights into the 5-HT2C receptor as a therapeutic target for substance use disorders Leigh Walker IPO to $331m Nxera Pharma and Antiverse Enter Collaboration To Design Novel GPCR- Targeted Antibody Therapeutics Using Generative AI Zombie Fungi Hijack Hosts’ Brains GPCR Therapeutics, Inc. has received Orphan Drug 20th World Congress of Basic and Clinical Pharmacology GPCR Jobs Scientist I Cell Biology - Tectonic Therapeutic insights into the 5-HT2C receptor as a therapeutic target for substance use disorders Targeting muscarinic

Homology modeling relies on using the known structure of a homologous protein as a template to model The introduction of AlphaFold2 marked a major advancement in the field of GPCR structure prediction. to known structures. crucial for understanding how drugs can selectively target different receptor conformations to achieve therapeutic Ligand discovery from a dopamine D3 receptor homology model and crystal structure.

November 7th : Drug Disposition in Physiological Tissues as a Therapeutic Variable. December 5th : Unique Exploitable GPCR-Ligand Behaviors for Therapeutic Benefit. Generate:Biomedicines Announces Multi-Target Collaboration with Novartis to Discover and Develop Protein Therapeutics with SEP-786, a Novel Oral Small Molecule PTH1R Agonist for the Treatment of Hypoparathyroidism Confo Therapeutics an Antibody-based Agonist and a Class A GPCR Regulating Hunger and Satiety OMass Therapeutics Expands

20th World Congress of Basic and Clinical Pharmacology GPCR Jobs Scientist I Cell Biology - Tectonic Therapeutic Hauser Group Postdoctoral Scholar – iPSC in cardiac and endothelial cell function Protein Biochemist/Structural anxiety-related behaviors in Sapap3 knockout mice Orphan GPCRs in Neurodegenerative Disorders: Integrating Structural correction of heterozygous mutation in exon 6 of the CaSR gene Reviews, GPCRs, and more Insight into structural properties of viral G protein-coupled receptors and their role in the viral infection: IUPHAR Review 41 Structural

This week brings sharp new insights into how minor changes in ligand structure can flip GPCR function Explore the Cheatsheet GPCR Publication Highlights   — Minimal Structural Variation of GPR84 Full Agonist Collaboration is the catalyst—let’s redefine what’s possible in GPCR-driven therapeutics.   

pose significant challenges to traditional structural analysis methods. and remarkable scalability, providing crucial structural insights for drug development. challenges is crucial to fully harness AI's potential in accelerating drug discovery and optimizing therapeutic AlphaFold2 structures guide prospective ligand discovery. Accurate structure prediction of biomolecular interactions with AlphaFold 3.

Our partner, Domain Therapeutics, will attend the SACHS 23rd annual biotech event in Europe. Dr. Christopher Langmead and colleagues' work on the 5-HT2C receptor as a therapeutic target for substance GPCR Symposium on ''GPCRs as Therapeutic Modalities' Share your project with a 1-minute abstract video into the 5-HT2C receptor as a therapeutic target for substance use disorders Industry News Crinetics teams up with addiction treatment maker Indivior to make digital therapeutics for substance use disorders

April is the month of DNA Day, a special day commemorating the discovery of the DNA double helix structure GPCR-targeted drugs, and the exploration of GPCRs as key regulators of physiological processes and therapeutic microscopy, have allowed us to understand the structural dynamics during receptor activation. drug discovery and design targeting GPCRs, leading to the development of novel therapeutics. Structural bioinformatics analysis of variants on GPCR function.

diabetes to cancer, fibrosis, and CNS disorders — GPCRs  are at the heart of the world’s most pressing therapeutic Class in Drug Discovery GPCRs regulate countless physiological processes, making them a goldmine for therapeutic But the real  excitement is in what’s next: Biased signaling  for selective therapeutic effects. Orphan GPCRs  with untapped therapeutic potential. you’re in early discovery or clinical development, the strategies here could open doors in your own therapeutic

These receptors respond to a variety of signals by undergoing structural changes that activate internal Twenty transition structures generated from overlapping particle subsets along this pathway provide a From the initial GTP binding, the structures highlight critical shifts in the α5 helix and the α-helical Concurrently, the α1 helix extends, propagating structural changes throughout the G protein. puzzles and underscores the importance of understanding cellular processes at the molecular level for therapeutic

GPCR Partner, Domain Therapeutics, for their nomination of the best-in-class CCR8 antibody candidate, History and function of the lactate receptor GPR81/HCAR1 in the brain: a putative therapeutic target G protein-coupled receptors as targets for transformative neuropsychiatric therapeutics. Structural and Molecular Insights into GPCR Function Identification of a potential structure-based GPCR Domain Therapeutics announces nomination of best-in-class CCR8 antibody candidate, DT-7012, further strengthening

the development of more selective drugs capable of modulating specific signaling pathways, improving therapeutic This allows for tailoring the half-life of nanobodies to increase their therapeutic window depending its conformation, protects the Schiff base, and prevents protein degradation, potentially offering therapeutic Nanobodies: A Review of Generation, Diagnostics and Therapeutics. Structural biology.