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  • The Five Traps of Ignoring Kinetics

    In drug discovery, equilibrium constants look tidy. But biology isn’t tidy. Kinetics in Drug Discovery: Your Edge If you’re still treating potency as a static number, you’re missing It’s a shift in how expert drug hunters see pharmacology. But discovery doesn’t. Here, you’ll find: Weekly lectures  that sharpen the tools you actually use in discovery A growing on-demand

  • PH-Binding Motif in PAR4 Oncogene: From Molecular Mechanism to Drug Design

    We propose that Pc(4-4) may serve as a powerful drug not only toward PAR-expressing tumors but also for

  • 📰 GPCR Weekly News, March 25 to March 31, 2024

    Terry Kenakin’s Applying Pharmacology to Drug Discovery course. discovery and development GPCRs in Neuroscience Scutellaria baicalensis Georgi stems and leaves flavonoids Discovery & Development In Endocrine And Metabolic Diseases How biotech companies are using AI to design drugs GPCR Therapeutics Announces Publication in PNAS Using Cutting Edge Spectroscopy to Detect GPCR Discovery Chemistry April 4 - 7, 2024 | American Physiology Summit April 5 - 10, 2024 | AACR Annual

  • Design Pharmaceuticals Closes $5 Million Pre-series A Round to Accelerate Commercialization of ...

    Pharmaceuticals Closes $5 Million Pre-series A Round to Accelerate Commercialization of Ultrahigh Throughput Drug Discovery Platform "April 12, 2022 07:00 AM Eastern Daylight Time CAMBRIDGE, Mass. --Design Pharmaceuticals, a company redesigning small molecule drug discovery, today announced the closing The proceeds will be used to further build the company’s discovery platform and operations. Design Pharmaceuticals’ platform is based on ultrahigh-throughput technologies that biomine drug-like

  • 📰 GPCR Weekly News, December 4 to 10, 2023

    , and more Design and structural validation of peptide-drug conjugate ligands of the kappa-opioid receptor discovery of GPCR signaling Illuminating the understudied GPCR-ome Industry News Sosei Heptares’ Partner Exhibition February 11 - 14, 2024 | 2024 BPS Annual Meeting March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Summit March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29 , 2024 | Ligand Recognition and Molecular Gating Conference April 1 - 4, 2024 | 19th Annual Drug Discovery

  • 📰 GPCR Weekly News, October 16 to 22, 2023

    , and more Pharmacologically targeting intracellular allosteric sites of GPCRs for drug discovery Targeting discovery Application of bioluminescence resonance energy transfer to quantitate cell-surface expression Pharma Intelligence Awards Japan 2023 BioMap and Sanofi to co-develop AI modules for biotherapeutic drug discovery Novartis Kisqali® NATALEE analysis reinforces consistent reduction in risk of recurrence across Pharmaceuticals Senior Director, In vitro pharmacology - Crinetics Pharmaceuticals In vivo Antibody Discovery

  • 📰 GPCR Weekly News, September 4 to 10, 2023

    GPCR, was featured as Superluminal Medicines Launches to Drug Protein Conformations in a Flash. Discovery Domain Therapeutics CEO Pascal Neuville to Discuss Game-Changing GPCR-Targeting Immunotherapies discovery Confo Therapeutics Appoints Stephen Dowd As Chief Business Officer Septerna Announces Novel Discovery with Cryo-EM September 25 - 28, 2023 | Discovery On Target September 27 - 28, 2023 | Training Seminar "The Renaissance in GPCRs as Drug Targets: Allosteric Function and Biased Signaling" at the

  • Embark on a GPCR Adventure: Your Weekly Research Expedition! | Oct 21-27, 2024

    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 Discovery Summit Europe July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology Discovery Approaches Altered PLCβ/IP3/Ca2+ Signaling Pathway Activated by GPRCs in Olfactory Neuronal

  • Inside Out: Mapping GPCRs from Membrane Codes to Market Moves

    on-demand course on non-canonical GPCR behaviors and a podcast episode tracing 30 years of GPCR-RAMP discovery modules reveal how location bias, intracellular signaling, and ligand kinetics can be leveraged to expand drug discovery horizons and fine-tune candidate selection.  

  • Ermium Therapeutics has constituted its SAB

    of a Scientific Advisory Board comprising international leaders in GPCRs pharmacology, immunology, drug discovery and development for auto-immune diseases" Read more at the source #DrGPCR #GPCR #IndustryNews

  • 📰 GPCR Weekly News, November 20 to 26, 2023

    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 Discovery and Development GPCR Events, Meetings, and Webinars January 16 - 19, 2024 | 23rd Annual PEP Discovery Summit March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29 , 2024 | Ligand Recognition and Molecular Gating Conference April 1 - 4, 2024 | 19th Annual Drug Discovery

  • 📰 GPCR Weekly News, February 27 to March 5, 2023

    Function and structure of bradykinin receptor 2 for drug discovery. discovery platform Antiverse identifies therapeutic antibodies targeting GPCRs CEO Andrew Hopkins on Exscientias AI-Driven Approach to Modern Drug Discovery Arcoscreen will present in the start-up village 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.

  • The Quiet Power of RGS Proteins: Rethinking Pain Pathways through GPCR Biology

    Watch Episode 170 What We’re Missing in Pain Research In GPCR drug discovery, receptors typically steal Serafini highlighted that in modern pain drug development, the field has remained too focused on ion Takeaway Forget what you think you know about GPCR drug targets.

  • Decoding Olfactory GPCRs: How AlphaFold and AI Are Changing the Game

    More accurate hypotheses, faster ligand discovery, and new strategies to tackle one of biology’s most From Prediction to Discovery One of Alessandro’s projects focused on receptor R5VK1 , where his team This case study highlights why computational chemistry is no longer a side tool—it’s a driver of discovery Start with our GPCR training program and get hands-on with virtual tools shaping the future of drug discovery

  • ShouTi Introduces Basecamp Bio as a Wholly Owned Subsidiary to Expand Pipeline and Partnerships

    introduced Basecamp Bio, a wholly owned subsidiary dedicated to fueling ShouTi’s pipeline and pursuing drug discovery partnerships."

  • Optimizing HTRF Assays with Fluorescent Ligands: Time-Resolved Fluorescence in GPCR Research

    Examples of HTRF donor/acceptor pairs Expanding Time-Resolved Fluorescence Applications in Drug Discovery In a recent study , we contributed to the development of a robust HTRF assay for the discovery of new A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery. A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery. HTRF: A technology tailored for drug discovery - a review of theoretical aspects and recent applications

  • How Collaboration Drives GPCR Discoveries

    The future of discovery will belong to scientists who know how to build the right partnerships and stay was a set of chemical probes that finally allowed researchers to visualize where receptors exist, how drugs No one person can be excellent at all of it — and pretending otherwise slows discovery. It is the only path to meaningful discovery. And it’s not just about capability. muscle-sparing metabolic therapies by combining GPCR pathways Creating chemical tools that finally show how drugs

  • 📰 GPCR Weekly News - January 2 to 8, 2023

    GPCR Signaling Measurement and Drug Profiling with an Automated Live-Cell Microscopy System. Twist Bioscience and Astellas Enter into Multitarget Antibody Discovery Research Collaboration Neurocrine GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit | February 21-23, Boston. Biological Sciences Doctoral Training Programme Senior QM Manager Director of Molecular Pharmacology, Discovery Discovery Explore Dr.

  • Finding needles in haystacks: Omass unveils pipeline aimed at tough-to-drug targets

    but Omass Therapeutics Ltd.’s new structure-based technology has passed a key test, in enabling the discovery of orally available small molecules aimed at intractable and poorly drugged membrane and complex-bound

  • Exscientia welcomes Richard J. Law, as their new Chief Business Officer

    partnerships and collaborations across pharma and #biotech⁠ and is an advocate for the role of #AI in drug discovery."

  • Advantages of Fluorescent Probes in GPCR Assays

    GPCRs pose a critical challenge in drug discovery: a vast therapeutic potential with many targets yet to be explored.  35% of FDA-approved drugs target GPCRs, showing their importance in numerous physiological However, over half of non-sensory GPCRs do not have drugs available in the clinic, opening the door to What are the current trends in G protein-coupled receptor targeted drug discovery? Expert Opin Drug Discov. 2023 Jul-Dec;18(8):815-820. doi: 10.1080/17460441.2023.2216014.

  • GPCRS: AN ODYSSEY FROM STRUCTURE, SIGNALING AND REGULATION TO THERAPEUTICS

    highly diverse range of chemical stimuli, they represent the therapeutic targets for many existing drugs New approaches to GPCR drug discovery. discuss new enabling technologies in order to leverage the recent advances in the field towards new discoveries and solutions in GPCR drug discovery.

  • 📰 GPCR Weekly News, June 24 to 30, 2024

    location bias of the GPCR-dependent translatome via site-selective activation of mTOR GPCR Binders, Drugs , Meetings, and Webinars September 18, 2024 | FREE Webinar - The value of GPCR cell-based assays in drug discovery October 2024 | Biologics US 2024 October 2 - 4, 2024 | 9th GPCRs in Medicinal Chemistry October Pharmacology 2026 GPCR Jobs NEW Scientist; Biochemistry, Cellular and Mechanistic Pharmacology; Lead Discovery Director GPCR Drug Discovery Biologist HIGHLIGHT Principal Scientist, In vitro pharmacology Post-Doctoral

  • Addex Therapeutics To Release Full-Year 2021 Financial Results And Host Conference Call On March 10

    ADXN, Nasdaq: ADXN), a clinical-stage pharmaceutical company pioneering allosteric modulation-based drug discovery and development, announced today that it will issue its full-year 2021 financial results on Tim Dyer, CEO, Roger Mills, CMO and Robert Lütjens, Head of Discovery Biology, will provide a business

  • 📰 GPCR Weekly News, May 22 to 28, 2023

    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. FREE Symposium - IPI Surfacing (June 15, 2023) NEW GPCRs in drug discovery: challenges & solutions (June

  • 📰 GPCR Weekly News

    GPCR Binders, Drugs, and more Persistent challenges in the development of an mGlu7 PAM in vivo tool compound : The discovery of VU6046980. GPCR Industry News Septerna Announces the Formation of a Cross-Functional Scientific and Drug 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.

  • Community guidelines for GPCR ligand bias: IUPHAR review 32

    modulate a plethora of physiological processes and mediate the effects of one-third of FDA-approved drugs Ligands eliciting biased signalling may constitute better drugs with higher efficacy and fewer adverse The guidelines will aid consistency and clarity, as the basic receptor research and drug discovery communities

  • A robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery.

    cost-effective methodologies for screening compound libraries targeting the CBRs becomes key for identifying drugs Cannabinoids as Anticancer Drugs: Current Status of Preclinical Research. HTRF: A Technology Tailored for Drug Discovery - A Review of Theoretical Aspects and Recent Applications SLAS Discovery   2010 , 15 (10), 1248–1259. https://doi.org/10.1177/1087057110384611 . (25)      Fulp

  • 📰 GPCR Weekly News, January 30 to February 5, 2023

    Development and challenges in the discovery of 5-HT1A and 5-HT7 receptor ligands. discovery and a plan to challenge pharma in diabetes TGA’s approval of MDMA and Psilocybin for medical Discovery Upstream Bio Announces the Appointment of Marcella Ruddy, M.D., to the Board of Directors Deadline extended to March 31st, 2023 GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery drug design postdoc at the Department of Drug Design and Pharmacology Software / database development

  • GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for...

    October 2022 GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A2A Adenosine Receptor "Modulators of the G protein-coupled A2A adenosine receptor (A2AAR) have been considered promising agents to treat Parkinson's disease, inflammation, cancer, and central nervous system disorders. Herein, we demonstrate that a thiophene modification at the C8 position in the common adenine scaffold converted an A2AAR agonist into an antagonist. We synthesized and characterized a novel A2AAR antagonist, 2 (LJ-4517), with Ki = 18.3 nM. X-ray crystallographic structures of 2 in complex with two thermostabilized A2AAR constructs were solved at 2.05 and 2.80 Å resolutions. In contrast to A2AAR agonists, which simultaneously interact with both Ser2777.42 and His2787.43, 2 only transiently contacts His2787.43, which can be direct or water-mediated. The n-hexynyl group of 2 extends into an A2AAR exosite. Structural analysis revealed that the introduced thiophene modification restricted receptor conformational rearrangements required for subsequent activation. This approach can expand the repertoire of adenosine receptor antagonists that can be designed based on available agonist scaffolds." Read more at the source #DrGPCR #GPCR #IndustryNews

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