expressed in CA1 hippocampal neurons, selectively reduces CaV 3.2 and CaV 3.3 currents GPCR Binders, Drugs Addex and Indivior Extend Research Term Of Substance Use Disorder Gabab Positive Allosteric Modulator Discovery GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit | February 21-23, Boston. Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential.

Nevertheless, the GloSensor™ cAMP assay can be applied to analyze signaling by a wide range of GPCRs for drug discovery" Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "As important drug targets, G protein-coupled receptors (GPCRs) play pivotal roles in a wide differences impeded the use of predicted structure models in the functional study and structure-based drug

Read about the newest discoveries in GPCR research 🙌 Save the dates: November 2 - 4: We're sponsoring Ozempic kidney trial after early signs of success Sosei and PharmEnable extend neurological disease drugs at the Citeline Pharma Intelligence Awards Japan 2023 Salipro Biotech and Icosagen Launch Antibody Discovery Collaboration Cryo-EM in Drug Discovery GPCR Events, Meetings, and Webinars NEW October 19, 2023 | ERNEST Pharmaceuticals Senior Director, In vitro pharmacology - Crinetics Pharmaceuticals In vivo Antibody Discovery

Justin English on "Empowering Drug Discovery for the GPCR Community"! hiPSC-cardiomyocytes to GPCR and ion channel targeting compounds: A microphysiological system for cardiac drug

A number of strategies have been applied to develop CB2 ligands to achieve closer to 'drug-like' properties

A number of strategies have been applied to develop CB2 ligands to achieve closer to 'drug-like' properties

GPCR Binders, Drugs, and more An antibody-drug conjugate targeting GPR56 demonstrates efficacy in preclinical GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit, (February 21 - 23, 2023) Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. design PhD student at the Department of Drug Design and Pharmacology Computational drug design postdoc of Drug Design and Pharmacology Software / database development postdoc at the Department of Drug Design

for GPCR characterization through imaging, and as possible new tools used for target validation in drug

GPCR Binders, Drugs, and more Novel targets for potential therapeutic use in Diabetes mellitus. Artificial Intelligence for Drug Discovery Call for GPCR Papers GPCRs: Signal Transduction. Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. GPCR Jobs Computational drug design PhD student at the Department of Drug Design and Pharmacology Computational drug design postdoc at the Department of Drug Design and Pharmacology Software / database development

New ligands and new GPCR behaviors that produce unique drug profiles (i.e. intracellular ligands and November 7th: Drug Disposition in Physiological Tissues as a Therapeutic Variable. November 21st: Unconventional GPCR Ligands as Drugs. October 14th to 20th, 2024 Industry News Ghent based Confo Therapeutics is leveraging GPCR expertise as a discovery Discovery Summit Europe July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology

GPCR Binders, Drugs, and more Development of a V5-tag-directed nanobody and its implementation as an GPCRs in Cardiology, Endocrinology, and Taste Insights on discovery, efficacy, safety and clinical applications Exscientia is the Sniper of the AI Drug Discovery Industry Indivior Announces Q2/H1 2023 Financial Results Symposium (August 31 - September 1, 2023) NEW 3rd Transatlantic ECI GPCR Symposium (September 7 - 8, 2023) Discovery Interactions of GPCRs, Ion Channels, and Transport Proteins (March 24 - 29, 2024) GPCR Jobs Director, Discovery

Let's set sail towards exciting discoveries and groundbreaking achievements together! Highlights: Our fearless leader, Yamina Berchiche , is gearing up to rock the mic today at the 22nd Discovery November 21st : Unconventional GPCR Ligands as Drugs. of Molecular Pharmacology GPCR Events, Meetings, and Webinars September 30 - October 3, 2024 | 22nd Discovery Discovery Summit Europe July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology

Needed to Reactivate Antitumor Immune Response Garry Pairaudeau, CTO of Exscientia discuss transforming drug discovery using their AI-driven platform Salipro Biotech Expands Global Intellectual Property Portfolio IRN I-GPCRNet (October 25 - 27, 2023) GPCR Retreat (November 2 - 4, 2023) Structure, Mechanism, and Drug

GPCR Binders, Drugs, and more MRAP2 regulates energy homeostasis by promoting primary cilia localization GPCR Signaling Measurement and Drug Profiling with an Automated Live-Cell Microscopy System. Industry News Inversago Pharma to Participate at the 2023 SVB Securities Global BioPharma Conference Orbit Discovery Deadline February 12, 2023 GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential.

A conserved intracellular allosteric binding site (IABS) has recently been identified at several G protein-coupled receptors (GPCRs). Starting from vercirnon, an intracellular C-C chemokine receptor type 9 (CCR9) antagonist and previous phase III clinical candidate for the treatment of Crohn's disease, we developed a chemical biology toolbox targeting the IABS of CCR9. We first synthesized a fluorescent ligand enabling equilibrium and kinetic binding studies via NanoBRET as well as fluorescence microscopy. Applying this molecular tool in a membrane-based setup and in living cells, we discovered a 4-aminopyrimidine analogue as a new intracellular CCR9 antagonist with improved affinity. To chemically induce CCR9 degradation, we then developed the first PROTAC targeting the IABS of GPCRs. In a proof-of-principle study, we succeeded in showing that our CCR9-PROTAC is able to reduce CCR9 levels, thereby offering an unprecedented approach to modulate GPCR activity. Read full article

4565), an international biopharmaceutical company and world-leader in GPCR1-focused structure-based drug research, today announce the signing of an agreement to bring Sosei Heptares ’ cancer immunotherapy drug

binding partners on the GPCR activation mechanism, which should be taken into account in structure-based drug discovery.

Allosteric modulation of conserved motifs and helices in 5HT2BR: Advances drug discovery and therapeutic , and more Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment Application of computational methods for class A GPCR Ligand discovery. design PhD student at the Department of Drug Design and Pharmacology Computational drug design postdoc of Drug Design and Pharmacology Software / database development postdoc at the Department of Drug Design

GPCR Binders, Drugs, and more Adenosine A2A Receptor (A2AAR) Ligand Screening Using the 19F-NMR Probe GPCRs in Cardiology, Endocrinology, and Taste Discovery of paralogous GnRH and corazonin signaling systems Confo Therapeutics Enters Into Research Collaboration For GPCR-Targeting Antibody Discovery With AbCellera GPCR Events, Meetings, and Webinars GPCRs in drug discovery: challenges & solutions (June 19 - 23, 2023 I-GPCRNet (October 25 - 27, 2023) GPCR Retreat (November 2 - 4, 2023) NEW Structure, Mechanism, and Drug

Sulfo-glyco barcode - perspectives and added value in drug discovery A growing body of evidence proposes It remains to be discovered how much the modulation of these PTMs is relevant for future drug design. There are few examples of the applicability of the sulfo-glyco barcode in drug discovery.

GPCR Binders, Drugs, and more In-depth molecular profiling of an intronic GNAO1 mutant as the basis for personalized high-throughput drug screening. The application of artificial intelligence to accelerate GPCR drug discovery. its Leading AI and Cell Signalling Technology to Support Target Validation for a Sosei Heptares GPCR Discovery Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential.

GPCR Binders, Drugs, and more Inhibiting a promiscuous GPCR: iterative discovery of bitter taste receptor Eurofins Discovery Acquires CALIXAR, Expanding Integrated Drug Discovery Capabilities and Expertise. Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential.

in GPCR signaling G protein-coupled receptor-mediated autophagy in health and disease GPCR Binders, Drugs 24 - 29, 2024 | Ligand Recognition and Molecular Gating Conference April 1 - 4, 2024 | 19th Annual Drug Discovery Chemistry April 4 - 7, 2024 | American Physiology Summit April 5 - 10, 2024 | AACR Annual

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

mediator for methionine to stimulate milk synthesis in mouse mammary epithelial cells GPCR Binders, Drugs ADCS) Septerna Presents Preclinical Data at ENDO 2024 Highlighting Therapeutic Potential of its GPCR Drug Discovery Platform GPCRs and Emotional Pain: Exploring Non-Narcotic Pathways to Relief GPCR Events,

Illuminating GPCR signaling mechanisms by NMR spectroscopy with stable-isotope labeled receptors GPCR Binders, Drugs worth up to $674M 2023 Half-Year Financial Results and Exciting Developments at Aelis Farma Ion Channel Drug Chair of its Board of Directors Novo Nordisk and Evotec collaborate to launch LAB eN², a translational drug discovery accelerator, to address innovation gap in cardiometabolic diseases GPCR Events, Meetings, 2024 Conference and Exhibition June 2 - 4, 2024 | Chemotactic Cytokines GPCR Jobs NEW In vivo Antibody Discovery

April is the month of DNA Day, a special day commemorating the discovery of the DNA double helix structure The discovery of DNA's double helical structure was a scientific milestone that revolutionized molecular Genomics, in turn, played a crucial role in the discovery and sequencing of the beta-adrenergic receptor Additionally, there have been recent discoveries of the conformational changes that occur during G-protein discovery and design targeting GPCRs, leading to the development of novel therapeutics.