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

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 repurposing demonstrates mutation-agnostic efficacy in pre-clinical retinopathy models Reviews, GPCRs

A central question of GPCR drug discovery is to understand what determines the agonism or antagonism small changes to the ligands that invert their pharmacological activity and thus helps to guide the drug This approach can be readily applied to any drug target."

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

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

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

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

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

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

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

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

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 Non-equilibrium molecular simulation approaches are proven to be useful in this purpose.

This concept is gaining significant attention in drug discovery, especially in the context of G protein-coupled The concept of biased agonism has been effectively leveraged in drug discovery, as demonstrated by the Tirzepatide's success underscores the potential of designing drugs that selectively target beneficial Christopoulos, Signalling bias in new drug discovery: detection, quantification and therapeutic impact Nat Rev Drug Discov, 2013. 12 (3): p. 205-16. 2.         

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. November 25 - 27, 2024 | 1st Virtual GPCR Forum Conference November 26 - 28, 2024 | GPCRs-Targeted Drug class C orphan GPCR GPR179 involved in visual processing Reliability of AlphaFold2 Models in Virtual Drug

Kenakin and Hoare on '   Applying Pharmacology to Drug Discovery ' and ' Advanced Data Analysis for GPCR target coverage with real-time kinetics Discovering new ligands and unique GPCR behaviors for innovative drug cAMP Olanzapine manipulates neuroactive signals and may onset metabolic disturbances GPCR Binders, Drugs GPCRs and mRNA antigens enable drug discovery and development Mapping GPCR-RAMP complexes with MolBoolean Using Medium-Throughput Reporter Gene Assay GPCR Therapeutics Optimizes the Joint Development of New Drugs

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

vivo target coverage with real-time kinetics Discovering new ligands and GPCR behaviors for unique drug mechanism of bitter taste receptor agonist-mediated relaxation of airway smooth muscle GPCR Binders, Drugs breathe new life into schizophrenia pipeline GPCR Dynamics Reveal Mechanisms for Drug Discovery DMS: Structure To Function AbbVie Completes Acquisition of Cerevel Therapeutics Nxera Pharma attended the Drug , Meetings, and Webinars September 18, 2024 | FREE Webinar - The value of GPCR cell-based assays in drug

GPCR University We're thrilled to share that all spots for the Applying Pharmacology to Drug Discovery GPCR Partnered Events 3rd GPCRs - Targeted Drug Discovery Summit  Join us at the 3rd GPCRs Targeted Drug human and Drosophila Functional diversification of cell signaling by GPCR localization GPCR Binders, Drugs 14, 2024 | 2024 BPS Annual Meeting NEW 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

GPCR Event Spotlight Discovery on Target’s 19th Annual GPCR-Based Drug Discovery Targeting G Protein-Coupled Register today for the GPCR Drug Discovery Conference and save $200 with discount code “ DRGPCR24 ”. sensitive biosensor platform; Carterra Ultra™ ushers in a new frontier in fragment and small molecule drug Engaging multiple sclerosis by drugging a “simple” GPCR. This technique for studying cell receptors could have sweeping implications for drug development DeepCure

cell signaling pathway From Structure to Solution: How Structural Biology Informs the Development of Drugs Biosolutions Establishes Scientific Advisory Board GLP-1s like Ozempic are among the most important drug breakthroughs ever Goldman-backed drug developer Septerna raises $288 mln in US IPO Call for GPCR Papers November 25 - 27, 2024 | 1st Virtual GPCR Forum Conference November 26 - 28, 2024 | GPCRs-Targeted Drug Sapap3 knockout mice Orphan GPCRs in Neurodegenerative Disorders: Integrating Structural Biology and Drug