December 2021 "30/11/2021 Confo will work together with Regeneron to apply its GPCR drug discovery conformations, will be applied with the goal of enabling the discovery of novel therapeutic antibody drug

and Kallyope Enter Collaboration to Identify and Validate Novel Gastrointestinal GPCR Targets for Drug Validation (TIV) strategy to leverage multiple sophisticated technologies that drive creation of new drug discovery programs in key therapeutic areas Kallyope, pioneers in drug discovery involving the gut-brain Corporation, the international biopharmaceutical company, and New York City-based Kallyope , pioneers in drug to identify and validate novel G protein-coupled receptor (GPCR) targets with a goal of creating new drug

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

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

October 2022 Case Report of a Juvenile Patient with Autism Spectrum Disorder with a Novel Combination under methylphenidate treatment but responded positively to 3 mg per day of the atypical neuroleptic drug

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

into Collaboration Agreement with Domain Therapeutics and Université de Montréal for GPCR-Targeted Drug

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

clinical trials " HTL0039732 is a novel EP4 antagonist with potential to treat a wide range of cancers in combination 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

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

February 2022 " InterAx Biotech AG and Boehringer Ingelheim take first steps towards collaborating to unlock orphan targets leveraging InterAx AI driven discovery platform. Collaborative efforts aim to accelerate and improve the prediction of first-in-class small molecule agonists for a challenging orphan GPCR for a highly relevant therapeutic need. 💊 InterAx Biotech AG discovery platform was already successfully applied in projects with biopharmaceutical companies and also used in-house to discover first-in-class compounds for a novel oncology target that are now being tested in-vivo. #ai #biotech #systemsbiology #drugdiscovery #gpcr #deeptech #orphandrugs #pharma #partnerships #AI4drugdiscovery" 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

Therefore, the identification of such modulators as drug candidates is highly desirable. fine-tune receptor conformation and signaling but also provide an opportunity to identify promising drug

cancer therapies focuses on processes such as angiogenesis, cell signaling, stemness, metastasis, and drug benefits when administered alone, but a few more have demonstrated clear improvement when administered in combination Moreover, the use of propranolol in combination therapies with other drugs has shown synergistic antitumor clinical trials in which propranolol is taking part as adjuvant therapy at single administration or in combinatorial

One such platform is the chemogenetic DREADD (designer receptor exclusively activated by designer drugs

Course Schedule and Details Every Thursday at 10 am EST Principles of Pharmacology in Drug Discovery Principles of Pharmacology in Drug Discovery II -   Advanced Methods for the Optimization of Candidate New ligands and new GPCR behaviors that produce unique drug profiles (i.e., intracellular ligands and In silico exploration of 4(α-l-rhamnosyloxy)-benzyl isothiocyanate: A promising phytochemical-based drug reveals unexpected differences in downstream pathway activation Methods & Updates in GPCR Research A combination

G-protein-coupled receptors "Recently, academic and industrial scientific communities involved in kinetics-based drug development have become immensely interested in predicting the drug target residence time. Screening drug candidates in terms of their computationally predicted residence times, which is a measure of drug efficacy in vivo, and simultaneously assessing computational binding affinities are becoming Here, we have implemented an optimized approach of combining the data derived from steered molecular

Multiple Subthreshold GPCR Signals Combined by the G-Proteins Gαq and Gαs Activate the Caenorhabditis Modulating GPCR and 14-3-3 protein interactions: prospects for CNS drug discovery. GPCR Binders, Drugs, and more Design of Drug Efficacy Guided by Free Energy Simulations of the β2 -Adrenoceptor Bioorthogonal Tethering Enhances Drug Fragment Affinity for G Protein-Coupled Receptors in Live Cells Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential.

By combining fiber photometry with FRET-based biosensors, we were able to track GPCR-dependent signaling pathways over time, and in response to drug treatments in freely-moving adult rats. After several weeks to allow biosensor expression, fiber photometry is used in order to record drug responses spectrum of neuroscience research, ranging from the study of neural circuits and behavior, to preclinical drug

X-linked acrogigantism The mechanism of Gαq regulation of PLCβ3-catalyzed PIP2 hydrolysis GPCR Binders, Drugs , and more Discovery of Guanfacine as a Novel TAAR1 Agonist: A Combination Strategy through Molecular Cellular Science Offerings with Multispan Cell Engineering and Assay Services $3bn sales potential for drug Showcases Innovative AI-Driven Drug Design at BRIC AI 2023 Workshop Salipro Biotech AB Celebrates Milestones 24 - 29, 2024 | Ligand Recognition and Molecular Gating Conference April 1 - 4, 2024 | 19th Annual Drug

regulates the fat deposition in adipose tissues of finishing pigs via cAMP/PKA pathway GPCR Binders, Drugs activation and to relieve neuropathic pain GPCRs in Oncology and Immunology Systems Pharmacodynamic Model of Combination mutations are associated with clinical response in a phase 1b/2 study of the PLK1 inhibitor onvansertib in combination Receive US$3.75 Million Payment in Multi-Target Partnership Sosei Heptares Announces Submission of New Drug NEW Team Leader Antibody Discovery Staff Scientist (AC-TAP) in Database Development at Department of Drug

Here’s a sneak peek at what you can expect: Principles of Pharmacology in Drug Discovery I - Techniques 26th, 2024 Overview: GPCRs have been and arguably still are the most prolific and fertile therapeutic drug Principles of Pharmacology in Drug Discovery II - Advanced Methods for the Optimization of Candidate FDA Accepts New Drug Applications and Grants Priority Review for Crinecerfont for Pediatric and Adult Director GPCR Drug Discovery Biologist   Post-Doctoral Scientist- Molecular Pharmacology (FDE) Research

Course Schedule and Details Every Thursday at 10 am EST Principles of Pharmacology in Drug Discovery GPCRs remain one of the most prolific and fertile therapeutic drug targets. Principles of Pharmacology in Drug Discovery II -   Advanced Methods for the Optimization of Candidate , Meetings, and Webinars September 18, 2024 | FREE Webinar - The value of GPCR cell-based assays in drug Director GPCR Drug Discovery Biologist   Post-Doctoral Scientist- Molecular Pharmacology (FDE) Join Dr

University This week marks the beginning of our first Dr.GPCR University course, 'Applying Pharmacology to Drug GPCR Partnered Events March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Summit Join us at the 3rd cadherin ectodomain GPCR Activation and Signaling GPCR signaling bias: an emerging framework for opioid drug 11 - 14, 2024 | 2024 BPS Annual Meeting February 20, 2024 | Career Opportunities in Pharmacology and Drug 24 - 29, 2024 | Ligand Recognition and Molecular Gating Conference April 1 - 4, 2024 | 19th Annual Drug

systems pharmacology (QSP) modeling is an emerging mechanistic computational approach that couples drug It has begun to play important roles in drug development for complex diseases such as cancer, including The combination of the anti-PD-L1 antibody atezolizumab and nab-paclitaxel has shown clinical activity

protease activated receptor 4 (PAR4) in mouse models of acute and chronic kidney injury GPCR Binders, Drugs somatostatin receptors 2 and 3 as cancer biomarkers beyond NET: a paired immunohistochemistry approach The combination Sosei Heptares to take back GPCR agonist after GSK changes course All-rounder among receptors inspires drug Exhibition February 11 - 14, 2023 | 2024 BPS Annual Meeting March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug 24 - 29, 2024 | Ligand Recognition and Molecular Gating Conference April 1 - 4, 2024 | 19th Annual Drug

We highly recommend exploring valuable resources such as ' Applying Pharmacology to Drug Discovery ' of CB2 cannabinoid receptor triggered by a bivalent ligand enhances cellular signaling GPCR Binders, Drugs Oryzias melastigma Industry News Cumulus Oncology and leadXpro Achieve Critical Milestone in GPR68 Drug Discovery Project Ambrosia lands $16m to ‘improve on existing GLP-1 drugs’ Opening Ceremony of Xuzhou Zhongshu Research Site and CNS Drug Innovation Forum Nxera Pharma Notes Positive Phase 2 Data for Partnered

GPCR Binders, Drugs, and more Discovery of SYD5115, a novel orally active small molecule TSH-R antagonist Multiple subthreshold GPCR signals combined by the G proteins Gαq and Gαs activate the C. elegans egg-laying In situ visualization of opioid and cannabinoid drug effects using phosphosite-specific GPCR antibodies Industry News A Current View of Allosteric GPCR Drug Discovery from the 2nd Annual GPCRs-Targeted Drug Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential.