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Glioblastoma multiforme (GBM) is the most common and aggressive primary brain tumour in adults. Treatments include surgical resection, radiotherapy, and chemotherapy. Despite this, the prognosis remains poor, with an impacted quality of life during treatment coupled with brain tumour recurrence; thus, new treatments are desperately needed. In this review, we focus on recent advances in G-protein-coupled receptor (GPCR) targets. To date, the most promising targets are the chemokine, cannabinoid, and dopamine receptors, but future work should further examine the melanocortin receptor-4 (MC4R), adhesion, lysophosphatidic acid (LPA) and smoothened (Smo) receptors to initiate new drug-screening strategies and targeted delivery of safe and effective GBM therapies. Read full article

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.

August 2022 "Despite the importance of members of the GPCR superfamily as targets of a broad range of effective medicines many GPCRs remain poorly characterised. GPR84 is an example. Expression of GPR84 is strongly up regulated in immune cells in a range of pro-inflammatory settings and clinical trials to treat idiopathic pulmonary fibrosis are currently ongoing using ligands with differing levels of selectivity and affinity as GPR84 antagonists. Although blockade of GPR84 may potentially prove effective also in diseases associated with inflammation of the lower gut there is emerging interest in defining if agonists of GPR84 might find utility in conditions in which regulation of metabolism or energy sensing is compromised. Here, we consider the physiological and pathological expression profile of GPR84 and, in the absence of direct structural information, recent developments and use of GPR84 pharmacological tool compounds to study its broader role and biology. " Read more at the source #DrGPCR #GPCR #IndustryNews

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

July 2022 Confo Therapeutics receives €1.7 million VLAIO grant for further research on GPCR modulators for rare diseases "29/06/2022 Confo Therapeutics, founded in 2015 as a spin-off from VIB and VUB, announced The grant should help expand Confo Therapeutic’s research on G protein-coupled receptor (GPCR) drug candidates

August 2022 A correlation study of adhesion G protein-coupled receptors as potential therapeutic targets

VIB spin-off Confo Therapeutics today announced that it has entered into a collaborative agreement with in disease-relevant conformations, will be applied with the goal of enabling the discovery of novel therapeutic

We’re glad to have Peter's dedication, experience, and passion in building innovative therapeutics."

August 2022 "Geneva, Switzerland, August 18, 2022 - Addex Therapeutics (SIX and Nasdaq: ADXN), a clinical-stage

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 "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

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.

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

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

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.

September 2022 "The follicle-stimulating hormone receptor (FSHR) belongs to the glycoprotein hormone receptors, a subfamily of G-protein-coupled receptors (GPCRs). FSHR is involved in reproductive processes such as gonadal development and maturation. Structurally, the extensive extracellular domain, which contains the hormone-binding site and is linked to the transmembrane domain by the hinge region (HR), is characteristic for these receptors. How this HR is involved in hormone binding and signal transduction is still an open question. We combined in vitro and in situ chemical crosslinking, disulfide pattern analysis, and mutation data with molecular modeling to generate experimentally driven full-length models. These models provide insights into the interface, important side-chain interactions, and activation mechanism. The interface indicates a strong involvement of the connecting loop. A major rearrangement of the HR seems implausible due to the tight arrangement and fixation by disulfide bonds. The models are expected to allow for testable hypotheses about signal transduction and drug development for GPHRs." Read more at the source #DrGPCR #GPCR #IndustryNews

Biopharma returns to MC4R; Recursion completes Exscientia acquisition, signaling a fresh AI–GPCR chapter; OMass–Genentech

GPCRs in Neuroscience Orphan receptor GPR88 as a potential therapeutic target for CNS disorders - an Industry News Coherus to Acquire Surface Oncology Confo Therapeutics and AbCellera partner on GPCR-targeting Patent in Japan Proteros Biostructures GmbH Revolutionizes Metabolic Disorder Treatments Structure Therapeutics (June 28 - 30, 2023) NEW FREE Seminar Antibodies targeting Membrane Proteins - From Antigen to New Therapeutics 2024) GPCR Jobs NEW Professor in Cardiovascular Pharmacology Scientist I / Scientist II DOE (Native Mass

This week's highlights: Kudos to our partner, GPCR Therapeutics, for partnering with Bridge Biotherapeutics 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 Study Neurocrine opening two Phase 1 trials in oral Parkinson’s therapies Bearing Fruit: Deep Apple Therapeutics Launches to Screen AI-Generated Virtual Libraries AbbVie to Acquire Cerevel Therapeutics in Transformative

et al. for their fantastic review on Molecular and structural insights into the 5-HT2C receptor as a therapeutic 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 proteins in obesity and diabetes mellitus Molecular and structural insights into the 5-HT2C receptor as a therapeutic

How do molecules make the leap from laboratory concept to therapeutic reality? miss the forest for the trees The critical importance of translation —turning lab data into meaningful therapeutic

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