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Coupled with their ability to respond to a highly diverse range of chemical stimuli, they represent the therapeutic

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

September 2022 "Background G protein-coupled receptor (GPCR) is the most targeted protein family by the FDA-approved drugs. GPCR-kinase 3 (GRK3) is critical for GPCR signaling. Our genomic analysis showed that GRK3 expression correlated with poor prognosis of gastric adenocarcinoma (GAC) patients. However, GRK3’s functions and clinical utility in GAC progression and metastases are unknown. Methods We studied GRK3 expression in normal, primary, and metastatic GAC tissues. We identified a novel GRK3 inhibitor, LD2, through a chemical-library screen. Through genetic and pharmacologic modulations of GRK3, a series of functional and molecular studies were performed in vitro and in vivo. Impact of GRK3 on YAP1 and its targets was determined." Read more at the source #DrGPCR #GPCR #IndustryNews

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

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

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

Dr Brennan has extensive experience across all phases of clinical development, and across multiple therapeutic

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

March 2022 "Geneva, Switzerland, March 7, 2022 – Addex Therapeutics (SIX: ADXN, Nasdaq: ADXN), a clinical-stage

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.

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

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

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

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

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

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

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

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 triterpenes isolated from Cryptostegia grandiflora against Candida auris FKBP12 Development and therapeutic Southwest Award Winner Monlunabant by Inversago Pharma for Metabolic Syndrome: Likelihood of Approval Tectonic Anti-Seizure Activity in Epilepsy Models Biophysicists decipher functionality of adrenaline-binding receptor Tectonic

Bryan Roth and Brian Krumm for their study on Molecular glues as potential GPCR therapeutics Drs. breast cancer progression by suppressing the MMP8-mediated antitumorigenic effects GPR56: A potential therapeutic via site-selective activation of mTOR GPCR Binders, Drugs, and more Molecular glues as potential GPCR therapeutics $10 Million from AbbVie as Collaboration Targeting Neurological Diseases Achieves First R&D Milestone Tectonic