December 2021 OMass Therapeutics 's founder, Carol Robinson , has been awarded the prestigious Louis-Jeantet Franklin Medal in Chemistry from The Franklin Institute yesterday for contributions to the field of mass

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

Chemistry, former president of the Royal Society of Chemistry and Founder of (and ongoing consultant to) OMass Therapeutics , which is based at Oxford Science Park, has been awarded the 2022 Louis-Jeantet Prize

2 Epilepsy Clinical Study’s Independent Interim Review Committee Recommends Continuing Study Addex Therapeutics Research Council (ERC) Addex Reports Q1 2023 Financial Results And Provides Corporate Update Structure Therapeutics Reports First Quarter 2023 Financial Results and Recent Highlights OMass Therapeutics presented at the Therapeutics Sosei Heptares 2022 ESG report Exscientia Announces Sixth Molecule Created Through Generative GPCR Events, Meetings, and Webinars ASPET 2023 - American Society for Pharmacology and Experimental Therapeutics

GPCRs in Cardiology, Endocrinology, and Taste Clinical, Pathophysiologic, Genetic, and Therapeutic Progress Methods & Updates in GPCR Research Evaluation of Drug Responses to Human β2AR Using Native Mass Spectrometry Septerna Secures $150 Million in Series B Financing to Advance Pipeline of Novel GPCR-targeted Medicines OMass Therapeutics was shortlisted for ‘Life Sciences and Health Tech Company of the Year’ in the 2023 Thames Directors Crinetics Pharmaceuticals Announces Inducement Grants Under Nasdaq Listing Rule 5635(c)(4) Confo Therapeutics

This week's highlights: Driving Pharma Innovation in Oncology: Domain Therapeutics' Success Proven by GPCR Symposium on GPCRs as Therapeutic Modalities is on September 22nd. Industry News Omass Therapeutics Celebrates a Series of Recent Publications by their Scientists. Discover a New Way To Develop Drugs Without Side Effects Driving Pharma Innovation in Oncology: Domain Therapeutics

for identification of potential agonists of FFAR4 for type 2 diabetes mellitus therapy Industry News OMass Therapeutics Welcomes Melissa Faris as Chief Business Officer Septerna: Revitalizing G-Protein Coupled (ANDA) Litigation PostEra Announces a Research Collaboration with Amgen to Discover Small Molecule Therapeutics

July 2022 "July 19, 2022 07:00 AM Eastern Daylight Time BOSTON-- Tectonic Therapeutic , Inc. a pre-clinical

Therapeutic potential of allosteric modulators for the treatment of gastrointestinal motility disorders GPCRs in Oncology and Immunology Clinical, pathophysiologic, genetic and therapeutic progress in Primary News Sosei Heptares and Neurocrine Biosciences won Out-Licensing Deal of the Year from Locust Walk Omass Therapeutics 2022 Review Sosei hooks millions from Eli Lilly alliance Septerna was selected as one of Use Disorders AbbVie recruits a GPCR team in Oxford, buying out a fledgling biotech for $255M+ Domain Therapeutics

, GPCRs, and more RGS proteins and cardiovascular Angiotensin II Signaling: Novel opportunities for therapeutic Japan for Daridorexant (ACT-541468), a Dual Orexin Receptor Antagonist for the Treatment of Insomnia OMass Therapeutics Releases First Protein Structures in PDB, Advances Lupus Therapy Research Structure Therapeutics

February 2022 " Ermium Therapeutics Announces the Formation of a Scientific Advisory Board comprising

A New Wave of GPCR Drug Discovery GPCRs are considered highly druggable, with GPCR-targeting therapeutics Within the last two years, three investments stand out: · Tectonic Therapeutics: received $80 USD Series A round to develop small molecule drugs against difficult-to-drug GPCRs. · Domain Therapeutics Developing Small Protein Therapeutics with a Novel Discovery Platform One way to overcome the challenges About Orion Biotechnology Orion’s mission is to unlock the therapeutic potential of previously undruggable

its best-in-class and first-in-class immuno-oncology programs STRASBOURG, France & MONTREAL- Domain Therapeutics

May 2022 "Seoul, South Korea, 28 April 2022 – GPCR therapeutics , Inc., a venture-backed clinical stage

Historically, ligands for GPCRs have been identified before their receptor counterparts. With the cloning revolution, several unidentified receptors have been found and were labelled as “orphan” for their endogenous ligands. Orphan GPCRs have been shown to play key roles in various physiological functions, such as sensory perception, reproduction, development, growth, metabolism, and are also linked to major diseases, such as neuroinflammatory, metabolic and autoimmune diseases. Therefore, matching a ligand to an orphan GPCRs, the process of de-orphanizing, is of great importance in order to better understanding human physiology as well as to dissect the molecular mechanism governing the involvement of these receptors in human pathology. GPR84 is an example of an orphan GPCR (Sharman et al., 2011), although it is widely accepted that medium‐chain fatty acids (MCFAs) can bind to and activate this receptor with modest potency. GPR84 is a Gi‐coupled class A GPCR mainly expressed in immune cells and microglia in the brain (Wojciechowicz & Ma'ayan, 2020). GPR84 has been shown to be an attractive target in pro‐inflammatory conditions (Gagnon et al., 2018; Suzuki et al., 2013; Vermeire et al., 2017; Wojciechowicz & Ma'ayan, 2020) and efforts have been made to discover GPR84 antagonists. In this study Marsango et al. address two key questions in GPR84 biology and pharmacology: 1. how GPR84 expression profile correlates with physiological and pathological conditions? and 2. which ligands can be used as tool compounds to study the function and biology of this receptor? Regarding the first question, GPR84 overexpression in immune cells in a range of pro‐inflammatory disorders renders it a promising target in inflammatory and fibrotic conditions, including neuroinflammation (Audoy‐Remus et al., 2015), with ongoing clinical trials in idiopathic pulmonary fibrosis (Labéguère et al., 2014). GPR84 has been additionally proposed to be a potential biomarker in different inflammatory diseases (Arijs et al., 2011; Planell et al., 2017). Some studies have also reported GPR84 involvement in pain, atherosclerosis, and even metabolic disorders (Nicol et al., 2015, Audoy‐Remus et al., 2015, Du Toit et al., 2018). Regarding the second question, there is still a lot to be done in respect to tool compounds to study the function of this receptor towards clinical validation, as well as radiopharmaceuticals, including potential PET ligands, and suitable antibodies. Recent work has shown distinct functional outcomes of agonist ligands (Pillaiyar et al., 2018) with biased properties which can help to better elucidate the molecular pharmacology of this receptor. In addition, several GPR84 ligands have been described as well as GPR84 knockout mice. Among these ligands are orthosteric agonists such as alkylpyrimidine‐4,6‐diol derivatives (Liu et al., 2016; Zhang et al., 2016) and embelin (2,5‐dihydroxy‐3‐undecyl‐1,4‐benzoquinone) which is a natural product derived from the plant Embelia ribes (Gaidarov et al., 2018) which agonizes GPR84 but, interestingly, blocks the chemokine receptor CXCR2 and the adenosine A3 receptor (Gaidarov et al., 2018). IM (3,3′‐methylenebis‐1H‐indole) has been identified as a positive allosteric modulator of GPR84, a metabolite produced in vivo from indole‐3‐carbinol, which is present at high levels in some vegetables including broccoli and kale (Wang, Schoene, Milner, & Kim, 2012, Köse et al., 2020). GPR84 antagonists include a series of dihydropyrimidinoisoquinolinones (Labéguère et al., 2014), which behave as non‐competitive antagonists of GPR84 (Labéguère et al., 2020). From these series of compounds, GLPG1205 progressed into clinical development for the potential treatment of ulcerative colitis although it did not demonstrate sufficient efficacy (Labéguère et al., 2020). Overall, GPR84 is a promising target to exploit and the investment in better tools to study its function in both disease and physiological settings will likely potentiate drug discovery campaigns against this orphan GPCR. Check the original article at here! #GPCR #DrGPCR#Ecosystem

Thus, identifying novel molecular targets for developing HF therapeutics remains a key research focus Additionally, GPCR dysregulation underlies multiple models of cardiac pathology, and most pharmacological therapeutics

April 2022 Ono Enters into Collaboration Agreement with Domain Therapeutics and Université de Montréal Gyo Sagara ; “Ono”) today announced that it has newly signed a collaboration agreement with Domain Therapeutics

August 2022 Structure Therapeutics Extends Financing, Advances Diabetes and Obesity Clinical Program and Changes Name from ShouTi " San Francisco and Shanghai – August 1, 2022 – Structure Therapeutics (Structure Therapeutics), formerly known as ShouTi Inc., today announced it closed an oversubscribed In addition, Structure Therapeutics has completed dosing in a single ascending dose (SAD) Phase 1 study

March 2022 " Explicyte grants Domain Therapeutics exclusivity on data related to GPCR implicated in Strasbourg and Bordeaux, France, March 10, 2022 – Domain Therapeutics , a biopharmaceutical company specializing their expertise to identify GPCR targets and associated biomarkers to discover and develop breakthrough therapeutic

July 2022 "I’m happy to share that I’m starting a new position as Scientific co-founder LASEREDD Therapeutics

January 2022 "Watch our CEO Tim Dyer on AlphaStreet. In his interview, Mr. Dyer provides an overview of our #allostericmodulator pipeline and the potential $4 billion market for our lead compound #dipraglurant in #PDLID (#Parkinsonsdisease levodopa-induced #dyskinesia)." Read more at the source #DrGPCR #GPCR #IndustryNews

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

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

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

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

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