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December 2021 "30/11/2021 Confo will work together with Regeneron to apply its GPCR drug discovery platform VIB spin-off Confo Therapeutics today announced that it has entered into a collaborative agreement with Regeneron Pharmaceuticals, Inc. whereby Confo’s technology platform, which uses conformationally selective 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

March 2022 Confo Therapeutics Doses First Subjects In Phase 1 Clinical Trial Of CFTX-1554 For The Treatment Of Neuropathic Pain "— Confo’s first drug candidate moves into clinical development — Ghent, Belgium – March 10, 2022 – Confo Therapeutics, a leader in the discovery of medicines targeting G-protein coupled

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.

GPCRs in Cardiology, Endocrinology, and Taste Clinical, Pathophysiologic, Genetic, and Therapeutic Progress Secures $150 Million in Series B Financing to Advance Pipeline of Novel GPCR-targeted Medicines OMass Therapeutics Directors Crinetics Pharmaceuticals Announces Inducement Grants Under Nasdaq Listing Rule 5635(c)(4) Confo Therapeutics CEO, Cedric Ververken, will join WuXi AppTec's upcoming online series "BOLD: Innovation

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

This week's highlight: Congratulations to the GPCR Therapeutics team for their publication on improving Orion's COO, Shared Innovative Insights at LSBC Central European Life Science Investment Conference GPCR Therapeutics &D and Late-Stage Development Progress Parker Moss to Join Exscientia as EVP, Corporate Development Confo Therapeutics Nominated for 'Deal of the Year (>€500 Million)' Award at European Lifestars Awards GPCR

diffusion, offset kinetics, and rebinding ✅ Real-world examples of how residence time—not potency—predicts therapeutic The slow-offset compound stays on target longer, maintains therapeutic effect as concentrations drop, DrugResidenceTime #AllostericModulation #CytosolicKinetics #PK #PD #CellPermeabilityAssays #PAMPA #Caco2 #TherapeuticKinetics

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 and G-CLIPS join forces to revolutionize transmembrane proteins characterization in drug discovery Confo Therapeutics Appoints Stephen Dowd As Chief Business Officer Septerna Announces Novel GPCR-targeted

Novartis bolsters innovative medicines strategy and renal pipeline with agreement to acquire Chinook Therapeutics Confo Therapeutics Enters Into Research Collaboration For GPCR-Targeting Antibody Discovery With AbCellera

GPCR Symposium on 'GPCRs as Therapeutic Modalities' Showcase your project with a 1-minute abstract video Bolsters Leadership Team as the Company Advances its Multi-Product Pipeline Toward Clinical Studies Confo Therapeutics Appoints Dieter Weinand, Former CEO Of Bayer Pharmaceuticals, As Independent Chairman Addex 21st Annual Global Healthcare Conference CEO Raymond Stevens to Speak at STAT Future Summit on Obesity Therapeutics Function and Biased Signaling" at the DOT NEW October 3, 2023 | FREE Seminar: Changing paradigm on Therapeutics

GPCR Symposium about 'GPCRs as Therapeutic Modalities' rocked it! recommended by NICE for acute migraines Addex mGlu2 NAM Cognition Program Receives €4 Million Grant Confo Therapeutics Appoints Stephen Dowd As Chief Business Officer Call for GPCR Papers opnMe GPCR Route 66 Lefkowitz's Career at Duke October 3, 2023, | FREE Seminar: Changing paradigm on Therapeutics targeting

from the atomic-level quaternary structure of short-lived GPCR oligomers in live cells Industry News Confo Therapeutics Announces EUR 60M Series B Financing to Advance a Pipeline of Novel GPCR-Modulating Therapies

November 7th : Drug Disposition in Physiological Tissues as a Therapeutic Variable. December 5th : Unique Exploitable GPCR-Ligand Behaviors for Therapeutic Benefit. Trial with SEP-786, a Novel Oral Small Molecule PTH1R Agonist for the Treatment of Hypoparathyroidism Confo Therapeutics Announces Publication in Nature Communications Demonstrating First-Ever Structure of a Complex Between an Antibody-based Agonist and a Class A GPCR Regulating Hunger and Satiety OMass Therapeutics

Industry News Design Pharmaceuticals has a new website Confo Therapeutics Announces Global Licensing Antiverse raises €2.8M for its computational antibody drug discovery platform Antiverse identifies therapeutic

cAMP-PKA-CREB signaling pathway based on network pharmacology and bioinformatics analysis Unveiling the therapeutic News Monash University pharmaceutical scientists honoured in NHMRC Research Excellence Awards Domain Therapeutics Clinical Study Evaluating Effects of NBI-1065890, a Second-Generation VMAT2 Inhibitor, in Healthy Adults Confo Therapeutics Secures VLAIO Grant Supporting Drug Discovery & Development In Endocrine And Metabolic Diseases How biotech companies are using AI to design drugs GPCR Therapeutics Announces Publication in

adipose tissue size more effectively than exendin, suggesting that biased agonism can lead to distinct therapeutic In conclusion, biased agonism at the GLP-1R represents a promising strategy for optimizing therapeutic continues to grow, it is likely to play an increasingly important role in the design of next-generation therapeutics Christopoulos, Signalling bias in new drug discovery: detection, quantification and therapeutic impact Drucker, D.J., Mechanisms of Action and Therapeutic Application of Glucagon-like Peptide-1.  

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

Therapeutic potential of opioid receptor heteromers in chronic pain and associated comorbidities. Industry News Confo Therapeutics Enters into Collaboration Agreement with Daiichi Sankyo to Discover SMILES-based de novo molecular generation with curriculum and deep reinforcement learning 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

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

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

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 Inc (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

Applications of Fluorescent Probes in Confocal Imaging of GPCRs: From Live to Fixed Cells GPCRs are present How Fluorescent Probes Enable High-Resolution Confocal Imaging of GPCRs To study the dynamics of GPCRs A High Content Screening focused microscope that has a confocal-like mode as well. Exploring the Applications of Confocal Fluorescence Microscopy in GPCR Research In GPCR research one Figure 2.Left panel, confocal microscopy of living cells incubated for 1h at 37ºC with CELT-327.

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

March 2022 "Explicyte grants Domain Therapeutics exclusivity on data related to GPCR implicated in immunoresistance 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