Hello everyone! Check out our latest coverage of GPCRs this week, featuring 15 insightful research papers and industry updates. Stay informed with the latest GPCR research and industry news. This week's highlight includes congrats to: Cam Sinh Lu, for his first Dr. GPCR contributor article Extracellular signal-regulated kinases – a potential pathway for GPCR-targeted drug discovery Nicola J Smith, Lauren T May, and Natasha L Grimsey for their work on Highlights and hot topics in GPCR research from 'Down Under' Dr. GPCR University Today marks the final day of the Dr. GPCR University workshop on Advanced Data Analysis for GPCR Pharmacology, led by the esteemed Dr. Sam Hoare. It's been a remarkable experience with participants joining us from around the globe. We're thrilled to announce that Dr. Terry Kenakin will return for two consecutive courses in September and October 2024. Stay tuned for more details, and be ready to register in July 2024. Dr. GPCR Podcast We have thrilling news—Episode 153 of the Dr. GPCR Podcast featuring Dr. Jacek Mokrosiński is live! Titled "Embracing Networking for Professional Growth" Our podcast episodes are now available in video format on our website. Revisit your favorite episodes and catch up on any you’ve missed. Tune in and enjoy the visual experience! Dr. GPCR Matchmaking Read Mark's job spotlight article for a Principal Scientist in In Vitro Pharmacology! Mark recently discussed this exciting opportunity with Beth Fleck, Director of In Vitro Pharmacology at Crinetics Pharmaceuticals! GPCR Event Highlight We are delighted to announce our first in-person event in collaboration with the Adhesion GPCR Consortium: The 11th Adhesion GPCR Workshop will be held in vibrant Mexico City from October 23 to 25, 2024. Join the global GPCR community and share your research—submit your abstract using this form. We are also seeking sponsors to support this exciting event that unites scientists worldwide to explore all aspects of adhesion GPCR biology. Interested in sponsoring? Please email us at Hello@DrGPCR.com. Let’s dive into the Classified GPCR News from May 20th to 26th, 2024. Adhesion GPCRs Adhesion G Protein-Coupled Receptor Gpr126 (Adgrg6) Expression Profiling in Diseased Mouse, Rat, and Human Kidneys GPCR Activation and Signaling Differential regulation of G protein-coupled receptor-associated proteins in the caudate and the putamen of cynomolgus macaques following chronic ethanol drinking GRK5 is required for adipocyte differentiation through ERK activation GPCR Binders, Drugs, and more Flipping the GPCR Switch: Structure-Based Development of Selective Cannabinoid Receptor 2 Inverse Agonists Development of Putative Bivalent Dicovalent Ligands for the Adenosine A1 Receptor GPCRs in Cardiology, Endocrinology, and Taste Sodium/Potassium ATPase Alpha 1 Subunit Fine-tunes Platelet GPCR Signaling Function and is Essential for Thrombosis GPCRs in Oncology and Immunology Enterococcus-derived tyramine hijacks α2A-adrenergic receptor in intestinal stem cells to exacerbate colitis The EBI2 receptor is coexpressed with CCR5 in CD4+ T cells and boosts HIV-1 R5 replication Methods & Updates in GPCR Research Evaluation and comparison of colorimetric outputs for yeast-based biosensors in laboratory and point-of-use settings Quantitative proteomics reveals CLR interactome in primary human cells Exploiting Cell-Based Assays to Accelerate Drug Development for G Protein-Coupled Receptors TOR signaling regulates GPCR levels on the plasma membrane and suppresses the Saccharomyces cerevisiae mating pathway Reviews, GPCRs, and more Highlights and hot topics in GPCR research from 'Down Under' Apelin receptor dimer: Classification, future prospects, and pathophysiological perspectives Structural and Molecular Insights into GPCR Function Bilayer lipids modulate ligand binding to atypical chemokine receptor 3 Industry News New cannabinoid CB1 receptor antagonists disclosed in Inversago patent Orion Biotechnology will be attending BIO 2024 Antiverse is attending BIO 2024 Septerna to Present Preclinical Data from GPCR Drug Discovery Engine at ENDO 2024 The Promise of Oxytocin: Novel Approaches for Targeting Oxytocin Receptors in Autism Spectrum Disorder and Psychiatric Disorders GPCR Events, Meetings, and Webinars NEW June 1 - 4, 2024 | ENDO 2024 NEW June 3 - 6, 2024 | BIO 2024 June 2 - 7, 2024 | Chemotactic Cytokines June 4, 2024 | Live Webinar ‘It All Starts With a Protein – Protein Sciences as a Key to Success in Drug Discovery’ June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein Mediated Signaling Networks June 25 - 29, 2024 | FENS Forum 2024 October 2024 | Biologics US 2024 October 2 - 4, 2024 | 9th GPCRs in Medicinal Chemistry October 23 - 25, 2024 | 11th Adhesion GPCR Workshop July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology 2026 GPCR Jobs HIGHLIGHT Principal Scientist, In vitro pharmacology NEW Senior Scientist - Receptor Pharmacology NEW PostDoctoral Scientist Senior Research Associate/Associate Scientist, Protein Science Post-Doctoral Fellow—Pharmacology/Cell Biology/Biochemistry Post Doctoral Fellow Postdoc Position Senior Associate Scientist - Global Research Technologies Novo Nordisk Scientist I - Global Research Technologies Novo Nordisk Join Dr. GPCR Ecosystem

September 2022 Regulator of G Protein Signaling 20 Correlates with Long Intergenic Non-Coding RNA (lincRNAs

Remember to check out the weekly Classified GPCR News from August 14 to 20, 2023 Adhesion GPCRs Amelioration November 2 - 4, 2023) MPGPCR Conference (November 15 -17, 2023) ASCEPT Annual Scientific Meeting (November 20

Hello GPCR people! We have great news! This week we’ve curated 18 GPCR papers, 1 new event, 9 industry news, and 3 job opportunities! Take a few minutes, and dive into our GPCR coverage! We welcome GPCR paper suggestions! Submit your publications to Hello@DrGPCR.com for consideration. This week's highlight: Thank you to Dr. Tobias Langenhan for his papers to highlight suggestions GAIN Domain Unfolding in Adhesion GPCRs Molecular Sensing in Adhesion GPCR Dissociation Physiological Force Modulation in Drosophila Neurons Dr. David Gloriam and his team present GproteinDb in 2024 Are you looking to hire? Or maybe looking for your next opportunity? Let Mark Schmeizl, our Chief Matchmaker help. Contact him by filling out this form. Our November Dr. GPCR Newsletter is now available. This month's video newsletter features Dr. Alix Rouault as our special guest. Subscribe now! Don't miss the upcoming episodes of Dr.GPCR Podcast featuring Dr. Neil Grimsey and Dr. Katarzyna Marcinkiewicz. Now check out the weekly Classified GPCR News from November 20th to 26th, 2023. Adhesion GPCRs The Posttraumatic Increase in the Adhesion of GPCR EMR2/ ADGRE2 to Circulating Neutrophils Is Not Related to Injury Severity Unveiling Mechanical Activation: GAIN Domain Unfolding and Dissociation in Adhesion GPCRs Molecular sensing of mechano- and ligand-dependent adhesion GPCR dissociation GPCR Activation and Signaling GPR101: Modeling a constitutively active receptor linked to 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 Modeling Studies and Biological Assays GPCRs in Oncology and Immunology RGS5 maintaining vascular homeostasis is altered by the tumor microenvironment High Metabolite Concentrations in Portal Venous Blood as a Possible Mechanism for Microbiota Effects on the Immune System, and Western Diseases Lactate receptor GPR81 drives breast cancer growth and invasiveness through regulation of ECM properties and Notch ligand DLL4 Chemokine N-terminal-derived peptides differentially regulate signaling by the receptors CCR1 and CCR5 Chemokine Cxcl1-Cxcl2 heterodimer is a potent neutrophil chemoattractant Methods & Updates in GPCR Research GproteinDb in 2024: new G protein-GPCR couplings, AlphaFold2-multimer models and interface interactions Experimental modulation of physiological force application on leg joint neurons in intact Drosophila melanogaster Reviews, GPCRs, and more Catecholamine Derivatives: Natural Occurrence, Structural Diversity, and Biological Activity Advances in steroid research from the pioneering neurosteroid concept to metabolomics: New insights into pregnenolone function Molecular characterization of lumpy skin disease virus from recent outbreaks in Pakistan Structural and Molecular Insights into GPCR Function Structural and signaling mechanisms of TAAR1 enabled preferential agonist design Proteome-wide structural analysis quantifies structural conservation across distant species Industry News Avantor's (AVTR) New Offerings to Aid Cell and Gene Therapy Suite Avantor® Expands Cellular Science Offerings with Multispan Cell Engineering and Assay Services $3bn sales potential for drug Sosei Heptares wants back from GSK Novartis drops subpoena request in trade-secret spat with Takeda Novartis showcases significant data updates from Kisqali®, iptacopan and Scemblix® at SABCS and ASH Research reveals pro-phagocytic function and structural basis of GPR84 signaling Advancements in Precision Medicine: Superluminal Medicines Inc. Showcases Innovative AI-Driven Drug Design at BRIC AI 2023 Workshop Salipro Biotech AB Celebrates Milestones in CryoEM Structures and In Vitro Binding Assays Through Collaboration with Sanofi Genentech and NVIDIA Enter Into Strategic AI Research Collaboration to Accelerate Drug Discovery and Development GPCR Events, Meetings, and Webinars January 16 - 19, 2024 | 23rd Annual PEP Talk February 3 - 7, 2024 | SLAS2024 International Conference and Exhibition NEW February 11 - 14, 2023 | 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 Chemistry April 4 - 7, 2024 | American Physiology Summit April 5 - 10, 2024 | AACR Annual Meeting April 22 - 23, 2024 | Endocrine Metabolic GPCRs May 13 - 17, 2024 | 20th Annual PEGS Boston Summit May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Europe 2024 Conference and Exhibition June 2 - 7, 2024 | Chemotactic Cytokines October 2 - 4, 2024 | 9th GPCRs in Medicinal Chemistry July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology 2026 GPCR Jobs - Contact Mark Schmeizl NEW Scientist NEW Lead Researcher NEW Post-Doctoral Fellow Sr Scientist in Obesity, Muscle, and Metabolism Post-Doctoral Fellow Research Associate I, Tissue Culture Post-Doc Research Associate Postdoctoral Fellow Explore Dr. GPCR Ecosystem

(February 20 - March 3, 2023). (April 20 - 21, 2023) SLAS Europe 2023 Conference and Exhibition.

(April 20 - 21, 2023) Swiss Biotech Day (April 24 - 25, 2023) SLAS Europe 2023 Conference and Exhibition

Hello GPCR Passenger, Welcome aboard the GPCR train as it sets off on its journey. We are excited to have you back at your usual GPCR stop for the week. Let's explore the newest developments in GPCR research and community news together! This Week’s Highlights: Congrats to: Monserrat Avila-Zozaya , our incredible contributor, for her fantastic article on Profiling Immune Cell and Platelet Transcriptomes , and we want to wish her the best of luck on her talk today at the 11th Adhesion GPCR Workshop about ' Breaking Barriers: My Journey from Mexico to the Heart of the Dr. GPCR Ecosystem and beyond .' We all are cheering for you! Gunnar Schulte for his excellent work on International Union of Basic and Clinical Pharmacology CXV: The Class F of G Protein-Coupled Receptors Avoid delaying it further! Registrations end TOMORROW for Principles of Pharmacology II Don't let this opportunity slip away to reserve your spot in our upcoming course ! Seize the chance to enhance your understanding and expertise in pharmacology under the guidance of the renowned expert Dr. Terry Kenakin . Participants will acquire knowledge in: The powerful applications of new cellular assays to determine GPCR ligand behavior in different functional systems. Understanding real-time kinetics to predict activity and in vivo target coverage. New ligands and new GPCR behaviors that produce unique drug profiles (i.e. intracellular ligands and signaling, location bias, signaling bias). Modules: October 31st: The Eyes to See- The Importance of Pharmacologic Assays. November 7th: Drug Disposition in Physiological Tissues as a Therapeutic Variable. November 14th: The Application of GPCR Ligand Kinetics to Candidate Design. November 21st: Unconventional GPCR Ligands as Drugs. December 5th: Unique Exploitable GPCR-Ligand Behaviors for Therapeutic Benefit. *Lessons are every Thursday at 10 AM EST. Reasons to Consider Enrolling Now: Exciting Q&A Session and Group Discussions Don't miss out on the opportunity to get your questions answered by our knowledgeable teacher or initiate a lively discussion in the exclusive group dedicated to the course! Outstanding Educational Opportunities at an Unbeatable Value Our courses provide top-notch education at a competitive price. Tailored Learning Experience Designed for Your Needs Enhance your learning journey with access to our extensive library of recorded sessions. High Praise from Our Happy Students Past students highly endorse our programs, praising our faculty's engaging content and expertise in simplifying complex GPCR pharmacology concepts for practical use in academic and industrial settings. Exclusive Deal for Scientists in Developing Nations If you reside and work in a developing country, complete this form for free access to Dr. Kenakin's upcoming course. We aim to make education accessible to all! Act now to become a part of our prestigious learning community! Classified GPCR News  Let’s dive into the   Classified GPCR News from October 14th to 20th, 2024 Industry News Ghent based Confo Therapeutics is leveraging GPCR expertise as a discovery engine - multiple partners have already signed on to the science Lundbeck signs $2.5B check for Longboard, seeing blockbuster potential in epilepsy med Call for GPCR Papers Deadline: Nov 1, 2024. Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and Webinars November 5 - 7, 2024 | 16th Annual PEGS Europe   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 GPCR Jobs Scientist I Cell Biology - Tectonic Therapeutic Senior Scientist, GPCR Pharmacology Research Associate - Professor Graeme Milligan Postdoc in Molecular Pharmacology - The Hauser Group Postdoctoral Scholar – iPSC in cardiac and endothelial cell function Protein Biochemist/Structural Biologist Senior Scientist/Staff Scientist, Computational Chemistry Postdoc in GPCR mechanosensing   GPCR Activation and Signaling Opioid receptors reveal a discrete cellular mechanism of endosomal G protein activation Amylin receptor subunit interactions are modulated by agonists and determine signaling Distinct role of GRK3 in platelet activation by desensitization of G protein-coupled receptors GPCRs in Cardiology, Endocrinology, and Taste Latrophilin-2 Deletion in Cardiomyocyte Disrupts Cell Junction, Leading to D-CMP Steviol rebaudiosides bind to four different sites of the human sweet taste receptor (T1R2/T1R3) complex explaining confusing experiments GPCRs in Neuroscience An emerging multi-omic understanding of the genetics of opioid addiction A FMRFamide-like neuropeptide FLP-12 signaling regulates head locomotive behaviors in C. elegans GPCRs in Oncology and Immunology In Silico Design of Novel RGS2-Galpha-q Interaction Inhibitors with Anticancer Activity Evolutionary diversity of CXCL16-CXCR6: Convergent substitutions and recurrent gene loss in sauropsids Noval insights and therapeutic strategies for tumor-induced kidney pathologies Methods & Updates in GPCR Research Development of a NanoBRET Assay Platform to Detect Intracellular Ligands for the Chemokine Receptors CCR6 and CXCR1 Reviews, GPCRs, and more International Union of Basic and Clinical Pharmacology CXV: The Class F of G Protein-Coupled Receptors Structural and Molecular Insights into GPCR Function Structure of endothelin ETB receptor-Gi complex in a conformation stabilized by unique NPxxL motif Ligand-induced conformational changes in the β1-adrenergic receptor revealed by hydrogen-deuterium exchange mass spectrometry Become a Premium Member! 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August 2022 "Join Us in Boston for Discovery On Target 2022! Discovery on Target (DOT) highlights advances in current and emerging “hot” targets and technologies, as well as target validation strategies for the discovery and development of novel therapeutic agents ranging from biologics to small molecules." Read more at the source #DrGPCR #GPCR #IndustryNews

Alterations in gene expression appear in pathways related to primary cilia (PC). Accordingly, in these hiPSC-derived hNPCs and neurons, we observe a shortening of PC. Additionally, we detect a shortening of PC in PINK1 -deficient human cellular and mouse models of familial Furthermore, in sPD models, the shortening of PC is accompanied by increased Sonic Hedgehog (SHH) signal Inhibition of this pathway rescues the alterations in PC morphology and mitochondrial dysfunction.

Pc(4-4), a lead backbone cyclic peptide, was selected out of a mini-library, directed toward PAR2&4 PH-binding ligand activation of PAR4 induces EGF receptor (EGFR) Tyr-phosphorylation, effectively inhibited by Pc We propose that Pc(4-4) may serve as a powerful drug not only toward PAR-expressing tumors but also for Pc(4-4) may become a promising candidate for future therapeutic cancer treatment."

endogenous KISS1R signalling and physiological output in the hormone receptor-negative MDA-MB-231 and BT-20 MDA-MB-231 cells are metastatic when implanted in mice while BT-20 are not and remain epithelial-like However, KP-10 stimulation induced migration of MDA-MB-231, but not BT-20 cells, in a calcium-dependent Moreover, only BT-20 cells responded to KP-10 by increasing ERK phosphorylation in a β-arrestin-dependent

Carola Weiss is a Senior Executive with more than 20 years of international experience in the biopharmaceutical

afternoon that it would downsize its research to focus on its lead program, mavorixafor, and lay off about 20%

April 2022 "By Cliona MacSweeney | Apr 20, 2022 Cliona MacSweeney, a project director in our Translational

agonist potency (Ca2+EC50 = 24 nM, cAMPi EC50 = 6.5 nM) and pharmacokinetic properties (clearance ∼20

Founded as a spinout from the University of Dundee on 20 July 2012, Exscientia pioneered the design

Quarter 2024 Results and Provides Business Update GPCR Events, Meetings, and Webinars NEW November 18 - 20 Physiology Summit 2025 April 25 - 30, 2025 | AACR Annual Meeting 2025 May 12 - 15, 2025 | PEGS 2025 May 20

(February 20 - March 3, 2023). GEM2023. (March 14-17, 2023). (April 20 - 21, 2023) SLAS Europe 2023 Conference and Exhibition.

(February 20 - March 3, 2023). GEM2023. (March 14-17, 2023). (April 20 - 21, 2023) SLAS Europe 2023 Conference and Exhibition.

(April 20-21, 2023) SLAS Europe 2023 Conference and Exhibition. (February 20 - March 3, 2023). GEM2023. (March 14-17, 2023). 8th and final ERNEST Meeting in Crete.

In 2019, 5 out of 20 first-in-class approved therapeutic agents targeted GPCRs.

(February 20 - March 3, 2023). (April 20 - 21, 2023) SLAS Europe 2023 Conference and Exhibition.

(February 20 - March 3, 2023). (April 20 - 21, 2023) SLAS Europe 2023 Conference and Exhibition.

Vraniak’s career spans more than 20 years of financial and commercial experience in the life sciences

The chemokine system exhibits great versatility, with more than 50 chemokines interacting with over 20 first described in the CXCR4-vCCL2 structure (Qin, Kufareva et al. 2015), where a proline-cysteine (PC

We identify 69 retinopathy variants, including 20 previously uncharacterized variants, that exhibit diminished

Receptors Novo Nordisk A/S: Semaglutide 2.4 mg reduces the risk of major adverse cardiovascular events by 20% November 2 - 4, 2023) MPGPCR Conference (November 15 -17, 2023) ASCEPT Annual Scientific Meeting (November 20

a poster at AACR 2023 GPCR Events, Meetings, and Webinars NEW FREE 7th ERNEST GPCR zoominar (April 20 (April 20 - 21, 2023) Swiss Biotech Day (April 24 - 25, 2023) ASPET 2023 - American Society for Pharmacology