International Conference and Exhibition February 11 - 14, 2024 | 2024 BPS Annual Meeting NEW March 13 - 15

Hello there! We have some exciting updates for all the GPCR enthusiasts out there. This week, we have a comprehensive coverage of 12 GPCR research papers. Additionally, we have six industry news. And if you're looking for a new job opportunity, we have one job ad. This week's highlight includes congrats to: Luca Franchini and Cesare Orlandi for their research on Deorphanization of G Protein Coupled Receptors (GPCRs): a historical perspective Monserrat Avila-Zozaya article on From DNA day to GPCR genomics Dr. GPCR University Hurry! 17 out of the 25 spots have been filled! Team Registrations are also available!  You have until May 3rd, 2023 to register. We are pleased to announce five full scholarship opportunities for Dr. Hoare's workshop for individuals who live and work in developing countries. Please complete this form to take advantage of this opportunity on a first-come, first-served basis. We also ask that you share this with your colleagues. We define a developing country based on World Bank Classifications for its 2024 fiscal year. Join our upcoming Dr. GPCR University hands-on workshop with Dr. Samuel Hoare on Advanced data analysis for GPCR pharmacology, which will be held on Thursdays between May 9th and May 30th, 2024, from 10 am to 12 pm EDT. The workshop includes: Four x 2-hour Zoom sessions One-on-one meeting with Dr. Hoare Access to Dr. GPCR Ecosystem group Access to course materials and recordings Completion certificate One-year Dr. GPCR Ecosystem Premium Membership (restrictions apply) Early bird discount on future courses (restrictions apply) Check our conversation with Dr. Sam Hoare about this hands-on workshop HERE ⬇⬇⬇ Dr. GPCR Symposia Join us on June 7th for our symposium on Structural and Molecular Insights into GPCR Function. Stay tuned for more details. Premium members get access to on-demand content from past events. Submit a few slides for a poster presentation to showcase your research and network with our community. Fill out this form to get started! Don't forget to give us your feedback by completing our survey if you've participated in our symposiums. Dr. GPCR Matchmaking Did you check out our first job opportunity spotlight for a Principal Scientist In Vitro Pharmacology? Our Chief Matchmaker, Mark Schmeizl, had a great conversation about this position with Beth Fleck, Director of In Vitro Pharmacology at Crinetics Pharmaceuticals! Don't miss out! Also, if you are looking to hire or be hired, Mark Schmeizl can help you find your perfect match. Mark has experience connecting candidates with employers and will work with you to understand your needs and preferences to ensure a successful match. Contact Mark today to get started. Let’s dive into the Classified GPCR News from April 15th to 21st, 2024 GPCR Activation and Signaling Beneath the surface: endosomal GPCR signaling The M3 muscarinic acetylcholine receptor can signal through multiple G protein families Rapid elucidation of agonist-driven regulation of the neurokinin 1 receptor using a GPCR phosphorylation immunoassay GPCR Binders, Drugs, and more Identification of 1,3,8-triazaspiro[4.5]decane-2,4-dione Derivatives as a Novel Delta Opioid Receptor-Selective Agonist Chemotype GPCRs in Neuroscience Calcium-sensing receptor regulates Kv7 channels via Gi/o protein signalling and modulates excitability of human induced pluripotent stem cell-derived nociceptive-like neurons Characterization of myoinhibitory peptide signaling system and its implication in larval metamorphosis and spawning behavior in Pacific abalone The role of orphan G protein-coupled receptors in pain GPCRs in Oncology and Immunology Deciphering a GPCR-lncRNA-miRNA Nexus: Identification of an Aberrant Therapeutic Target in Ovarian Cancer Methods & Updates in GPCR Research Alared: Solvatochromic and Fluorogenic Red Amino Acid for Ratiometric Live-cell Imaging of Bioactive Peptides Cascaded amplifying circuit enables sensitive detection of fungal pathogens In Silico Analyses of Vertebrate G-Protein-Coupled Receptor Fusions United With or Without an Additional Transmembrane Sequence Indicate Classification into Three Groups of Linkers Reviews, GPCRs, and more Deorphanization of G Protein Coupled Receptors (GPCRs): a historical perspective Industry News Addex Therapeutics Reports Full Year 2023 Financial Results And Provides Corporate Update Aelis Farma announces the Last Patient, Last Visit in its clinical phase 2b trial with AEF0117 for the treatment of cannabis use disorder Orion Biotechnology will be presenting at the 19th Biopharma Drug Discovery Nexus Salipro Biotech will participate in BioKorea2024 Domain Therapeutics Appoints Sean A. MacDonald as Chief Executive Officer Nxera Pharma Announces Exclusive Supply and Distribution Agreement with Handok for PIVLAZ™ in South Korea Amgen To Present Tezspire® Phase 2A COPD Data At ATS 2024 GPCR Events, Meetings, and Webinars April 17 – May 1, 2024 | FREE ASPET Virtual Award Lecture Series 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 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 NEW Postdoc Position Principal Scientist, In vitro pharmacology Senior Associate Scientist - Global Research Technologies Novo Nordisk Scientist I - Global Research Technologies Novo Nordisk Postdoctoral Associate Research Technologist I Senior Scientist- Internal Medicine Research Unit Postdoctoral Scholar – Synaptic physiology, optical imaging, substance use disorder, pharmacology Join Dr. GPCR Ecosystem

3rd Annual Meeting IRN I-GPCRNet November 2 - 4, 2023 | GPCR Retreat- Registration Closed November 15

(May 14 - 19, 2023) PEGS Boston (May 15 - 19, 2023) 8th and final ERNEST Meeting in Crete. FREE Symposium - IPI Surfacing (June 15, 2023) Training School on “Cell-based assays to study Adhesion

Greetings, Pioneers of GPCR Science! Embark on this week’s thrilling updates in GPCR research, learning opportunities, and industry developments. Don’t just stay informed—immerse yourself, expand your knowledge, and become a trailblazer in the field! This Week’s Highlights: Celebrating Excellence: Wessel A. C. Burger , Arthur Christopoulos , David M. Thal , et al., for their groundbreaking work on Positive allosteric modulation of a GPCR ternary complex Unlock Your Learning: Limited Spots Available! There are only 5 spots left for our upcoming courses, so seize the chance to learn from the best in the field. 🚨 Hurry to reserve your spot for the Principles of Pharmacology I & II BUNDLE before the Early Bird Deadline on September 27 . With just one week left, becoming a premium member is all it takes to benefit from this discount! Not a premium member yet?  No worries – you can sign up for a 5-day FREE trial! Gain access to over 500 minutes of recorded classes in our  GPCR courses   taught by Drs. Terry Kenakin  and Sam Hoare ! Every Thursday at 10 AM EST: Principles of Pharmacology I Dates: October 3, 10, 17, 24 (four sessions) Topics: Pharmacologic activity measurement, mechanisms of action, and GPCR discovery strategies. Registration deadline: September 27, 2024 Principles of Pharmacology II Dates: October 31, November 7, 14, 21, December 5 (five sessions) (we skipped Thanksgiving, of course!) Topics: New cellular assays, real-time kinetics, and unique GPCR behaviors. Registration deadline: October 25, 2024 🔥 Why You Should Enroll Now: Cost-effective & Distinctive Educational Experience Affordable courses that maintain high-quality standards. Adaptable Learning Access recorded sessions at your convenience to enhance your understanding. Our Students Highly Recommend Us! Previous students praise the course content and our exceptional service. Join us for an exciting discussion with Dr. Terry Kenakin to gain insights and prepare for upcoming courses. Don't miss this valuable opportunity! Exclusive Deal for Scientists Residing and Working in Developing Nations If you live and work  in a developing country, please complete this form to enjoy complimentary access to Dr. Kenakin's upcoming courses. Our goal is to ensure that education is within reach for everyone! Secure your spot today and dive into the evolving world of GPCRs! GPCR Event Spotlight Discovery on Target’s 19th Annual GPCR-Based Drug Discovery Targeting G Protein-Coupled Receptors for New Therapeutic Options 📍  Boston, MA 📅 October 2 -3, 2024 Join leading scientists to investigate the most recent advancements in GPCR-targeted drug development, incorporating machine learning, innovative biophysical methods, and medicinal chemistry. Register today for the GPCR Drug Discovery Conference and save $200 with discount code “ DRGPCR24 ”. 11th Adhesion GPCR Workshop    📍  Mexico City 📅 October 23-25, 2024 Engage with your peers and delve into the latest developments in adhesion GPCR biology. The full agenda is now available; check it here ! If you want to enhance your brand, email Hello@DrGPCR.com  for sponsorship opportunities. Classified GPCR News  Let’s dive into the   Classified GPCR News from September 9th to 15th, 2024 Industry News MBX aims for $136M IPO to take potential rival to Ascendis' Yorvipath into phase 3 Certa Therapeutics Announces International Non-Proprietary Name for its First-in-class GPR68 Inhibitor Asengeprast (FT011) AlphaProteo generates novel proteins for biology and health research Innovate UK announced the winners of its Transforming Cancer Therapeutics grant, which focuses on developing life-changing cancer treatments. 𝗦𝘂𝗺𝗺𝗮𝗿𝘆 𝗼𝗳 𝘁𝗵𝗲 𝗿𝗲𝘀𝘂𝗹𝘁𝘀 𝗼𝗳 𝗔𝗘𝗙𝟬𝟭𝟭𝟳 𝗣𝗵𝗮𝘀𝗲 𝟮𝗯 𝗶𝗻 𝗖𝗨𝗗 Nxera Pharma’s Partner Centessa Announces Positive Interim Phase 1 Clinical Data with its Novel Orexin Receptor 2 (OX2R) Agonist, ORX750, in Acutely Sleep-Deprived Healthy Volunteers Cumulus raising $50M, spinning GPR68 small molecules into GIO New treatments being developed for schizophrenia Crinetics Pharmaceuticals Announces September 2024 Inducement Grants Under Nasdaq Listing Rule 5635(c)(4) Call for GPCR Papers Deadline: Nov 1, 2024. Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and Webinars September 5 - 6, 2024 | 4th Transatlantic ECI GPCR Symposium September 18, 2024 | FREE Webinar - The value of GPCR cell-based assays in drug discovery September 22, 2024 | Biomolecular Horizons 2024 September 30 - October 3, 2024 | 22nd Discovery on Target October 2024 | Biologics US 2024   October 2 - 4, 2024 | 9th GPCRs in Medicinal Chemistry October 17, 2024 | Unprecedented fragment-based screening using Spectral Shift for GPCRs October 23 - 25, 2024 | 11th Adhesion GPCR Workshop November 5 - 7, 2024 | 16th Annual PEGS Europe   NEW 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 HIGHLIGHT Research Associate - Professor Graeme Milligan HIGHLIGHT Postdoc in Molecular Pharmacology - The Hauser Group NEW Postdoctoral Scholar – iPSC in cardiac and endothelial cell function NEW Protein Biochemist/Structural Biologist Senior Scientist/Staff Scientist, Computational Chemistry Postdoc in GPCR mechanosensing   Postdoctoral Position Postdoctoral research position Adhesion GPCRs Loss of cardiomyocyte-specific Adhesion G Protein Coupled Receptor G1 (ADGRG1/GPR56) promotes pressure overload-induced heart failure GPCR Activation and Signaling Positive allosteric modulation of a GPCR ternary complex GPCR Binders, Drugs, and more Progress on the development of Class A GPCR-biased ligands GPCRs in Cardiology, Endocrinology, and Taste CRTC1 in Mc4r-expressing cells is required for peripheral metabolism and systemic energy homeostasis Eiken syndrome with parathyroid hormone resistance due to a novel parathyroid hormone receptor type 1 mutation: clinical features and functional analysis GPCRs in Neuroscience Gain control of sensory input across polysynaptic circuitries in mouse visual cortex by a single G protein-coupled receptor type (5-HT2A) GPCRs in Oncology and Immunology The power of many: Multilevel targeting of representative chemokine and metabolite GPCRs in personalized cancer therapy GPR97 depletion aggravates imiquimod-induced psoriasis pathogenesis via amplifying IL-23/IL-17 axis signal pathway Structural and Molecular Insights into GPCR Function Exploring the constitutive activation mechanism of the class A orphan GPR20 Become a Premium Member! 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Hello Readers👋, We're excited to share our weekly newsletter with you. Keep up-to-date with the latest research and advancements in the field with our convenient, weekly news delivered to your inbox. You can always adjust your email preferences in your account settings. Below is your Classified GPCR News at a glance for January 9th to January 15th, 2023. GPCR Activation and Signaling New simulation insights on the structural transition mechanism of Bovine Rhodopsin activation. Mandibulofacial dysostosis with alopecia results from gain-of-ETAR function via allosteric effects on ligand binding. GPCR Binders, Drugs, and more Modelling altered signalling of G-protein coupled receptors in inflamed environment to advance drug design. Protease-activated receptor 2 (PAR2)-targeting peptide derivatives for positron emission tomography (PET) imaging. GPCRs in Cardiology, Endocrinology, and Taste Gender Differences in GRK2 in Cardiovascular Diseases and its Interactions with Estrogen. GPR97 deficiency ameliorates renal interstitial fibrosis in mouse hypertensive nephropathy. Reviews, GPCRs, and more Isolation and functional identification of secretin family G-protein coupled receptor from Y-organ of the mud crab, Scylla olivacea. Structural and Molecular Insights into GPCR Function Thermodynamic architecture and conformational plasticity of GPCRs. Structural Understanding of Peptide-Bound G Protein-Coupled Receptors: Peptide-Target Interactions. Cryo-EM structures of orphan GPR21 signaling complexes. GPCR Allostery: a View from Computational Biology. The molecular associations in clathrin-coated pit regulate β-arrestin-mediated MAPK signaling downstream of μ-opioid receptor. Industry News Trevena Enrolls First Subject in TRV045 Proof-of-Concept Trial Evaluating S1PR Mechanism of Action and Target Engagement Novo Nordisk's GLP-1 for Type II diabetes approved for first-line treatment The Lundbeck Foundation is awarding DKK 174 million in grants to seven ‘mind-bending’ research collaborations GPCR Therapeutics Announces Launch of US Phase 2 Trial of GPC-100 in Multiple Myeloma Call for GPCR Papers GPCRs: Signal Transduction. Deadline February 12, 2023 Current Technologies To Understand G-Protein-Coupled Receptor Molecular Pharmacology. Deadline January 30, 2023. GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit | February 21-23, Boston. SLAS2023 International Conference and Exhibition (February 25 - March 1). SLAS 2023 Building Biology in 3D Symposium. (April 20-21, 2023) SLAS Europe 2023 Conference and Exhibition. (May 22 - 26, 2023) 2nd ERNEST Training School. (February 20 - March 3, 2023). GEM2023. (March 14-17, 2023). 8th and final ERNEST Meeting in Crete. (May 3-7, 2023). The Illuminating the Understudied Druggable Proteome Conference. (June 4-8, 2023). 2023 Molecular Pharmacology (GRS) Seminar GRC. (June 10 -11, 2023). Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. (June 11-16, 2023). 19th World Congress of Basic & Clinical Pharmacology 2023. (July 2 - 7). GPCR Jobs Biotechnology and Biological Sciences Doctoral Training Programme Senior QM Manager Director of Molecular Pharmacology, Discovery Biology Staff Scientist/Senior Staff Scientist, Disease Biology and Translational Sciences Senior Scientist, Drug Metabolism and Pharmacokinetics PhD Opportunity - Investigation Of The Role Of The Formyl Peptide Receptor 2 In Diabetic Retinopathy PhD Opportunity - Novel P2y Receptor Ligands For Drug Discovery Explore Dr. GPCR Ecosystem

April 2022 Trevena Announces Receipt of First $15 million Tranche in Connection with its $40 million medicines for patients with central nervous system (CNS) disorders, today announced receipt of the first $15

September 15-16, 2022. Lübeck, Germany. Hybrid meeting.

August 2022 "The atypical chemokine receptor 1 (ACKR1) was discovered on erythrocytes as the Duffy blood group antigen ( Cutbush et al., 1950 ), also called Duffy-antigen/receptor for chemokines, or DARC ( Novitzky-Basso and Rot, 2012 ). Erythrocytes are terminally differentiated anuclear cells with no transcription and limited translation. Accordingly, within the erythroid lineage ACKR1 expression occurs first and is the highest in erythroblasts ( Duchene et al., 2017 ). Additionally, ACKR1 expression characterizes venular endothelial cells (ECs) ( Pruenster et al., 2009 ; Thiriot et al., 2017 ), including those lining bone marrow (BM) sinusoids ( Duchene et al., 2017 ). This well-established, distinctive pattern of cell expression has been directly challenged by a publication purporting ACKR1 expression in mouse BM by macrophages, but not erythroblasts and ECs, suggesting that macrophage ACKR1 engages its non-cognate ligand CD82 on hematopoietic stem cells (HSCs) to maintain their quiescence ( Hur et al., 2016 ). In light of the extensive literature, these findings have been particularly provocative, as this was the first description of ACKR1 expression by any leukocyte type and, if correct, would change current concepts of ACKR1 involvement in pathophysiology. The reported ACKR1 expression by macrophages in Hur et al. relied on using commercial anti-ACKR1 antibody FAB6695, which has neither been validated by the manufacturer nor by the authors. This prompted us to investigate the specificity of FAB6695 and scrutinize the apparent ACKR1 expression in BM macrophages" Read more at the source #DrGPCR #GPCR #IndustryNews

June 2022 "June 15, 2022 06:30 AM EDT - In 2016, Abbie Celniker was promoted to partner at Third Rock

| Pharmacology 2024 January 13 - 16, 2025 | PepTalk 2025 January 25 - 29, 2025 | SLAS 2025 February 15 - 16, 2025 | Structural and Functional Approaches in GPCR Drug Discovery February 15 - 19, 2025 | BPS 27, 2025 | American Physiology Summit 2025 April 25 - 30, 2025 | AACR Annual Meeting 2025 May 12 - 15 P2Y-like receptor to its role in cancer progression Ascitic Shear Stress Activates GPCRs and Downregulates Mucin 15 to Promote OvarianCancer Malignancy Bispecific antibodies targeting BCMA or GPRC5D are highly effective

and tyrosine sulfation in their N-terminal region which seem to be widely conserved between human and murine GalNAc-type or mucin-type O-glycosylation is initiated by the transfer of Gal-NAc to a serine or threonine

| Pharmacology 2024 January 13 - 16, 2025 | PepTalk 2025 January 25 - 29, 2025 | SLAS 2025 February 15 - 16, 2025 | Structural and Functional Approaches in GPCR Drug Discovery February 15 - 19, 2025 | BPS 27, 2025 | American Physiology Summit 2025 April 25 - 30, 2025 | AACR Annual Meeting 2025 May 12 - 15 Taste Elucidating novel mechanism of action of spiperone for drug repurposing to prevent and treat murine

Pharmacology 2024 NEW January 13 - 16, 2025 | PepTalk 2025 NEW January 25 - 29, 2025 | SLAS 2025 NEW February 15 - 16, 2025 | Structural and Functional Approaches in GPCR Drug Discovery NEW February 15 - 19, 2025 2025 | American Physiology Summit 2025 NEW April 25 - 30, 2025 | AACR Annual Meeting 2025 NEW May 12 - 15 Channa punctata GPCRs in Neuroscience Neuron specific quantitation of Gαolf expression and signaling in murine

Rodríguez-Pérez , Gemma Navarro , José Labandeira-García , Rafael Franco Endomembrane GPCR signaling: 15 | Pharmacology 2024 January 13 - 16, 2025 | PepTalk 2025 January 25 - 29, 2025 | SLAS 2025 February 15 - 16, 2025 | Structural and Functional Approaches in GPCR Drug Discovery February 15 - 19, 2025 | BPS 27, 2025 | American Physiology Summit 2025 April 25 - 30, 2025 | AACR Annual Meeting 2025 May 12 - 15 classification of human odorant receptor multigene family Reviews, GPCRs, and more Endomembrane GPCR signaling: 15

This study examined the therapeutic effect of Ang-(1-7) on secondary injury observed in a murine model

medicine platform from target identification through patient selection Research will be focused on up to 15 Exscientia announced today a groundbreaking research collaboration and license agreement to develop up to 15

| Pharmacology 2024 January 13 - 16, 2025 | PepTalk 2025 January 25 - 29, 2025 | SLAS 2025 February 15 - 16, 2025 | Structural and Functional Approaches in GPCR Drug Discovery February 15 - 19, 2025 | BPS 27, 2025 | American Physiology Summit 2025 April 25 - 30, 2025 | AACR Annual Meeting 2025 May 12 - 15

receptor mRNA and protein has been recognized within myotubes and tissues of skeletal muscle from both murines Murine L6 skeletal muscle cells were used in order to clarify additional possible molecular signaling

📰 GPCR Weekly News, July 15 to 21, 2024 Hey everyone! Drum rolls, we’ve got 15 GPCR research papers, updates, industry news events, and GPCR ads curated just Submit your design by August 15, 2024, and stand a chance to have your creation represent this prestigious

Statins inhibit protein kinase D (PKD) activation in intestinal cells and prevent PKD1-induced growth of murine FREE Symposium - IPI Surfacing (June 15, 2023) Training School on “Cell-based assays to study Adhesion

and Commercialize Novel COVID-19 and Other Antibody Therapeutics for Difficult to Treat Diseases "Nov 15 --(BUSINESS WIRE)--Nov. 15, 2021-- Twist Bioscience Corporation (NASDAQ: TWST), a company enabling customers

review its pipeline during a teleconference and webcast for investors, analysts and media at 16:00 CET (15

| Pharmacology 2024 January 13 - 16, 2025 | PepTalk 2025 January 25 - 29, 2025 | SLAS 2025 February 15 - 16, 2025 | Structural and Functional Approaches in GPCR Drug Discovery February 15 - 19, 2025 | BPS 27, 2025 | American Physiology Summit 2025 April 25 - 30, 2025 | AACR Annual Meeting 2025 May 12 - 15

Flow-cytometric measurements were performed in 5, 10 and 15 min after activation."

strain C57Bl/6N) in which complementary DNA encoding the human PTH1R replaces a segment (exon 4) of the murine

Recently, it has been shown that murine Latrophilins mediate classical G-protein signals to drive synaptogenesis

of First Participant with Metabolic Syndrome in Phase 1B Clinical Trial "MONTREAL (CANADA) – March 15