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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

December 2021 OMass Therapeutics's founder, Carol Robinson, has been awarded the prestigious Louis-Jeantet

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

biggest opportunities will emerge: Building receptor-specific delivery systems for gene or peptide therapeutics

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

  ·  OMass Therapeutics  ·  Superluminal Medicines  ·  Tectonic Therapeutics  ·  and many more. , and Abilita Therapeutics. Translational Stories & Clinical Data OMass Therapeutics on long-residence MC2R antagonists. Tectonic Therapeutics on engineering a long-acting relaxin for pulmonary hypertension. Kainova Therapeutics presenting Phase 1 outcomes for their EP4 receptor antagonist in solid tumors.

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.

November 2021 "Nov. 15, 2021 LONDON – There’s not yet proof of the pudding, but Omass Therapeutics Ltd

Strong GPCR drug discovery decisions are built on structure, early risk awareness, and focused signal detection. If you work in GPCR research, clarity is leverage. The ability to access the right framework, detect risk early, and act on emerging signals determines whether programs accelerate—or stall. This week’s issue focuses on structure, early safety strategy, and the next wave of signal transduction research. Each piece is designed to help you make better decisions—faster. 🔍 This Week in Premium: Sneak Peek Industry insights: Confo nominates SSTR5 agonist antibody CFTX-2034; Lilly oral GLP-1 maintenance data; Enveda IND clearance ENV-308; Zealand explores brain-directed obesity therapies. Upcoming events: 12th Adhesion GPCR Workshop; GPCRnet International Symposium; 5th GPCRs Targeted Drug Discovery Summit. Career opportunities: Senior Scientist roles; Postdoctoral GPCR positions. Must-read publications: D2 receptor constitutively active mutants; β2AR allosteric SERS assay; CXCR4 inhibitor burixafor Phase 2. Dr. GPCR University — Reorganized for Clarity and Speed The Dr. GPCR University has undergone a structural redesign. This soft launch prioritizes usability and clarity to support stronger GPCR drug discovery decisions across teams. You can now search courses by level, topic, or instructor. Each course page includes a short trailer, defined learning outcomes, and explicit take-home messages. Full course videos stream directly from the platform, and downloadable resources are available in one place. Legacy courses will migrate into this format over the coming weeks, with live courses returning in March. In the meantime, Premium members continue to have full access to the legacy course pages. Why this matters now: Stop wasting time hunting for relevant training across fragmented platforms. Align your team around structured learning outcomes, not scattered slide decks. Identify the exact knowledge gap slowing your program—and close it efficiently. All courses remain included in Premium Membership. Preview the full University experience ➤ Already a Premium Member? Start learning here ➤ Terry’s Corner — Early Safety Assays For Better GPCR Drug Discovery Decisions Too many discovery programs fail because early safety signals were underestimated—or missed entirely. In this session, Dr. Terry Kenakin walks through the core early assays that protect your chemistry, budget, and timeline. This is not theory. It is operational pharmacology designed to prevent avoidable setbacks. Early safety frameworks directly influence GPCR drug discovery decisions, especially when timelines and capital are tight. What you gain: Detect scaffold liabilities early—hERG inhibition, mutagenicity, and mechanistic red flags. Interpret cytotoxicity data correctly—distinguish transient stress from meaningful off-target damage. Assess hepatotoxicity risk—anticipate reactive metabolites and high-risk drug–drug interactions. Since launch, Terry’s Corner has expanded to 30+ courses and three live AMAs covering binding, kinetics, efficacy, mechanism, ADME, and experimental design. It delivers repeatable depth far beyond a short-format workshop. An upcoming live Ask-Me-Anything (AMA) with Dr. Kenakin takes place February 26 at 12:00 PM EST. Subscribe to the free Kenakin Brief Newsletter to join the AMA . Premium Members get 50%+ discount when they join Terry’s Corner. Access this week’s safety framework ➤ GPCRs: Signal Transduction — Volume II (Call for Papers, Deadline March 14) Signal transduction remains central to understanding GPCR biology across health and disease. A new volume dedicated to GPCR signal transduction invites contributions spanning cellular biochemistry, mechanistic signaling, and translational implications. Submissions are welcome across formats including Original Research, Reviews, Methods, Perspectives, Hypothesis and Theory, Technology and Code, and more. This initiative brings together field experts to advance collective understanding of how GPCR-mediated signaling shapes physiology and pathology. Given the pace of mechanistic and structural insight emerging across the field, coordinated scholarly contribution is timely. Why consider contributing: Position your work within a focused, visible GPCR signaling collection. Contribute to shaping scientific direction in cellular biochemistry. Strengthen field-wide dialogue around signaling mechanisms and dysfunction. Submit your work today ➤ Why Dr. GPCR Premium Membership Gives You an Edge GPCR science is accelerating across obesity, CNS, oncology, and metabolic disease. More data. More companies. More noise. Premium Membership filters that complexity — without filtering out what matters. Each week, you receive curated, signal-focused intelligence: industry developments, classified publications, priority event tracking, curated career opportunities, and full access to Dr. GPCR University courses — now included in Premium. That means structured, searchable, expert-led training across levels and topics — without additional course fees. Premium Members also receive a 50%+ discount on Terry’s Corner , unlocking advanced pharmacology depth and live AMAs with Dr. Terry Kenakin at a significantly reduced cost. This is not commentary. It is structured access and structured education. Premium supports more confident GPCR drug discovery decisions by helping you: Detect meaningful shifts early — without wading through noise. Strengthen mechanistic understanding through organized expert frameworks. Equip your team with repeatable training resources in one place. Reduce external training spend while increasing scientific depth. It supports scientists refining expertise. It strengthens teams executing discovery programs. It equips leaders making strategic and capital decisions. When decisions compound, scattered information creates drag.Structured access creates momentum. Premium delivers that — consistently. Explore Premium Today ➤

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

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

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 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. GPCR superstructures, termed receptorsomes, both at the cell surface membrane and in the intracellular domain

Nanobodies (Nbs), known as variable antigen-binding (VHH) domain or single-domain antibodies, are small 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.

This dimerization allows the N-terminal activation domain of the receptor to repeatedly engage and disengage Additionally, the dimeric state allows rotational movement of the receptor's extracellular domain (ECD only enhances our understanding of class B1 GPCR biology but also opens new avenues for developing therapeutic Graaf, C., et al., Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March to Therapeutic

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

the initial GTP binding, the structures highlight critical shifts in the α5 helix and the α-helical domain The activation process begins with the α-helical domain (AHD) of the G protein in an open state, which puzzles and underscores the importance of understanding cellular processes at the molecular level for therapeutic

In less than a decade, nanobodies, or recombinant single-domain antibody fragments from camelids, have nanobodies with tailored specificities may expand the impact of these tools for both basic science and therapeutic

Adhesion GPCRs Piconewton Forces Mediate GAIN Domain Dissociation of the Latrophilin-3 Adhesion GPCR Unveiling Mechanical Activation: GAIN Domain Unfolding and Dissociation in Adhesion GPCRs GPCR Activation Tethered Ligands that Target the µ-Opioid Receptor Design and Synthesis of Novel GPR139 Agonists with Therapeutic

Discovery on Target’s 19th Annual GPCR-Based Drug Discovery Targeting G Protein-Coupled Receptors for New Therapeutic Modalities A quick revision of how β-adrenergic receptors work and how their antagonists can achieve therapeutic Domain Nominated for Prestigious Prix Galien USA ‘Best Startup’ Award: Pioneering GPCR-Driven Immunotherapies in Cancer Treatment Structure Therapeutics Appoints Angus C. Intracellular Allosteric Probe Selective optogenetic inhibition of Gαq or Gαi signaling by minimal RGS domains

When “inhibition” becomes activation—and how that insight fuels next-gen therapeutic design. Read the Feature ➤ Summer Days: Appetite, Suntans, and GPCR Micro-Domains Two recent papers connect ciliary Why micro-domains change what “global” signaling can and can’t explain.

GPCRs in Neuroscience G protein coupled receptors as targets for transformative neuropsychiatric therapeutics GPCRs in Oncology and Immunology CCR6 as a Potential Target for Therapeutic Antibodies for the Treatment Methods & Updates in GPCR Research Solvent accessibility of a GPCR transmembrane domain probed by in-membrane Inversago Pharma will present at BBHIC 2023 Orion Biotechnology attended the Swiss Biotech Day Addex Therapeutics GPCR Events, Meetings, and Webinars ASPET 2023 - American Society for Pharmacology and Experimental Therapeutics

🎉 Conformational coupling between extracellular and transmembrane domains modulates holo-adhesion GPCR Pharmacology GPCR Jobs GPCR Molecular Pharmacologist Scientist - Biology Scientist I Cell Biology - Tectonic Therapeutic Structural Biologist Adhesion GPCRs Conformational coupling between extracellular and transmembrane domains

September 2022 "The Smoothened receptor (SMO, a 7 pass transmembrane domain, Class F GPCR family protein In the absence of HH signaling, SMO is inhibited by Patched 1 (PTC1; a 12 pass transmembrane domain protein We are able to identify the interaction of membrane cholesterols with definite sites and domains within domain (CRD) and the intracellular domain (ICD), are through residues belonging to known cholesterol-binding Structural analysis of SMO domains shows significant changes in the CRD and ICD, during the course of

This week's highlights: Kudos to our partner, GPCR Therapeutics, for partnering with Bridge Biotherapeutics tANCHOR fast and cost-effective cell-based immunization approach with focus on the receptor-binding domain acids conjugation with [Cp*Rh(H2O)3]2+ by using the meta-dynamics/FMO3 approach Industry News GPCR Therapeutics - Providing the next generation of high-impact medicines Structure Therapeutics Provides Comprehensive Launches to Screen AI-Generated Virtual Libraries AbbVie to Acquire Cerevel Therapeutics in Transformative

Congrats to the GPCR Therapeutics team for their recent paper in the American College of Clinical Pharmacology GPCR Symposium on 'GPCRs as Therapeutic Modalities'. GPCR Activation and Signaling Single-molecule analysis reveals that a glucagon-bound extracellular domain and oligomerization Molecular Insights into GPCR Mechanisms for Drugs of Abuse Industry News 'GPCR Therapeutics Nordisk to Acquire Inversago Pharma GPCR Events, Meetings, and Webinars NEW Antiverse: Reimagining Therapeutic