development of its best-in-class and first-in-class immuno-oncology programs STRASBOURG, France & MONTREAL- Domain Therapeutics, a biopharmaceutical company specializing in the research and development of innovative

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

April 2022 Ono Enters into Collaboration Agreement with Domain Therapeutics and Université de Montréal and CEO: Gyo Sagara; “Ono”) today announced that it has newly signed a collaboration agreement with Domain Therapeutics S.A. (Strasbourg, France; CEO: Pascal Neuville; “Domain”) and Université de Montréal (Québec, Canada; “UdM

Transmembrane domains of GPCR dimers – a novel hot spot for drug discovery G-protein-coupled receptors GPCR dimers are therefore emerging drug targets in different therapeutic areas including depression, interaction between two receptors in a dimer involves a conformational change in the transmembrane domain

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 Therapeutics: completed a $42 Million USD Series A round to develop novel immunotherapies, including 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

share the same architecture, comprising a Venus Flytrap (VFT) module linked to the seven transmembrane domains

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 teams up with addiction treatment maker Indivior to make digital therapeutics for substance use disorders Therapeutics CEO Pascal Neuville to Discuss Game-Changing GPCR-Targeting Immunotherapies at Sachs Associates

We also show that the N-terminal region of anosmin 1, capable of binding to the PK2-binding domain of The whey acidic protein domain (WAP) is necessary for this modulatory activity, although data from GST pull-down (glutathione-S-transferase) and analysis of the N267K mutation in the fibronectin type III domain 1 (FnIII.1) suggest the cysteine-rich (CR) and the FnIII.1 domains could assist the WAP domain both

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. Scientists Discover a New Way To Develop Drugs Without Side Effects Driving Pharma Innovation in Oncology: Domain Therapeutics' Success Proven by Science Crinetics Hosting Key Opinion Leader Webinar To Discuss The

Xavier Leroy on his appointment as CEO of GIO Therapeutics! Congratulations to Domain Therapeutics for being awarded the RHU SPRINT consortium grant. Endocrinology, and Taste The Role of Gut Microbiota and Associated Compounds in Cardiovascular Health and its Therapeutic Therapeutics awarded Hospital-University Research in Health (RHU) SPRINT consortium grant to progress Xavier Leroy appointed as CEO of GIO Therapeutics GPCR Events, Meetings, and Webinars NOW!

GPCR Partner, Domain Therapeutics, for their nomination of the best-in-class CCR8 antibody candidate, History and function of the lactate receptor GPR81/HCAR1 in the brain: a putative therapeutic target G protein-coupled receptors as targets for transformative neuropsychiatric therapeutics. Domain Therapeutics announces nomination of best-in-class CCR8 antibody candidate, DT-7012, further strengthening

Congratulations to Domain Therapeutics for appointing Michael Gottlieb as Chairman and Dr. of GPCRs in various states Reviews, GPCRs, and more G Protein-coupled Receptors (GPCRs) as Potential Therapeutics modulate engagement of CCR5 by chemokines by removing key electrostatic interactions Industry News Domain Therapeutics strengthens leadership team to spearhead global development and North American expansion

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

future perspectives Non-canonical Golgi-compartmentalized Gβγ signaling: mechanisms, functions, and therapeutic Research Term Of Substance Use Disorder Gabab Positive Allosteric Modulator Discovery Collaboration Domain Therapeutics strengthens Scientific Advisory Board with appointment of immuno-oncology experts More

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 Additionally, the GRK2 interactome includes numerous proteins which interact with differential domains to modulate both beneficial and deleterious signaling pathways in the heart, indicating that these domains

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

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

GPCRs) is defined by an N-terminal large extracellular region that contains various adhesion-related domains before a canonical seven-transmembrane domain. The cleavage appears to occur at an atypical GPCR proteolysis site within the GAIN domain during an early Furthermore, in polarized MDCK cells, GPR125 is exclusively recruited to the basolateral domain of the The recruitment likely requires the C-terminal PDZ-domain-binding motif of GPR125 and its interaction

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

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

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

GPCR-p38 MAPK signaling and distinct inflammatory responses State-dependent dynamics of extramembrane domains and potential use of Opn5 and its homologs Industry News The Leading GPCR Company in Immuno-Oncology, Domain Therapeutics, Presents Groundbreaking Advancements at ESMO 2023 Novo Nordisk to Buy Hypertension Treatment

signaling in humoral immunity Industry News Neurosterix launches with $63M to Advance Allosteric Modulator Therapeutics Financial Resultsand Confirms Its 2024 Outlook Sosei Heptares officially changed their name to Nxera Domain Therapeutics to participate at premier investor and healthcare conferences Montana Molecular is joining

GPCR Symposium on GPCRs as Therapeutic Modalities on September 22nd. Domain Therapeutics announces the European Patent Office decision to grant a patent for its proprietary

constitutively active receptor linked to X-linked acrogigantism State-dependent dynamics of extramembrane domains and drug discovery in endocrinology and metabolism Reviews, GPCRs, and more Butyrate as a promising therapeutic bitopic cadherin G protein-coupled receptors that bind cry toxins of Bacillus thuringiensis Industry News Domain Therapeutics announces the promotion of Stephan Schann to the role of Chief Scientific Officer Crinetics

First Subject in Phase 1 Trial with HTL0033744, an EP4 Agonist for Inflammatory Bowel Disease (IBD) Domain Therapeutics and Chime Biologics Form Manufacturing Pact for Antibody Cancer Immunotherapy Sosei Heptares

Adhesion GPCRs Crystal Structure of the Extracellular Domains of GPR110. GPCRs in Oncology and Immunology Expanding role of CXCR2 and therapeutic potential of CXCR2 antagonists Reviews, GPCRs, and more The leukotriene B4 receptors BLT1 and BLT2 as potential therapeutic targets. Therapeutics unveiled its 2023 women-men professional equality index Octant introduces Hypatia, their New Robotic Drug Hunter GPCR Therapeutics Announces Publication in Nature Scientific Reports on Novel

GPCRs in Neuroscience G protein-coupled receptors (GPCRs) as Potential Therapeutics for Psychiatric Disorders Domain Therapeutics to present three posters at AACR 2023 annual meeting. Biotech Day (April 24 - 25, 2023) NEW ASPET 2023 - American Society for Pharmacology and Experimental Therapeutics