< GPCR News < GPCRs in Oncology and Immunology Gallein, G protein βγ subunits inhibitor, suppresses the TGF-α-induced migration of hepatocellular carcinoma cells via inhibition of the c-Jun N-terminal kinase Published date November 13, 2024 Abstract "G protein-coupled receptor (GPCR) signaling regulates a wide range of pathophysiological cell functions via G protein α and βγ subunits. Small molecules targeting the subunits of Gα and Gβγ have been developed as cancer therapeutics. We have previously reported that transforming growth factor-α (TGF-α) induces the migration of human hepatocellular carcinoma (HCC) HuH7 cells through the activation of AKT, p38 mitogen-activated protein kinase (MAPK), Rho-kinase and c-Jun N-terminal kinase (JNK). This study aims to determine whether Gβγ subunits regulate the TGF-α-induced migration of HCC HuH7 cells using gallein, a Gβγ subunits inhibitor. The Janus family of tyrosine kinase (JAK)/signal transducer and activator of transcription 3 (STAT3) signaling pathway was also involved in the regulation of the migration. Gallein significantly reduced the TGF-α-induced cell migration. In contrast, fluorescein, a gallein-related compound that has no effect on Gβγ subunits, failed to affect the cell migration. Gallein suppressed the TGF-α-stimulated phosphorylation of JNK without affecting the phosphorylation of epidermal growth factor receptor, AKT, p38 MAPK, target protein of Rho-kinase and STAT3. Conversely, fluorescein did not attenuate the phosphorylation of JNK. These results strongly suggest that Gβγ subunits act as positive regulators in TGF-α-induced migration of HCC cells via the JNK signalling pathway." Authors Rie Matsushima-Nishiwaki, Yoh Honda, Haruhiko Tokuda, Osamu Kozawa Source Contribute to the GPCR News Coming soon Become a Contributor Classified GPCR News Call for GPCR papers GPCR Industry News Adhesion GPCRs GPCR Events, Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research GPCRs in Neuroscience GPCRs in Cardiology, Endocrinology, and Taste GPCRs in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling More from Dr. GPCR Create an account and get our contributors articles in your inbox Subscribe to the Dr. GPCR Monthly Newsletter today! Follow the Dr. GPCR News and get weekly notifications about the GPCR field Share < Previous Next >

Get the GPCR's news in your inbox Contributor Articles Dr. GPCR Monthly Newsletter Weekly GPCR News about the GPCR field Sign Up Latest Classified GPCR News Adhesion GPCRs September 25, 2024 The G Protein-Coupled Receptor GPR56 Is an Inhibitory Checkpoint for NK Cell Migration Read More September 12, 2024 Loss of cardiomyocyte-specific Adhesion G Protein Coupled Receptor G1 (ADGRG1/GPR56) promotes pressure overload-induced heart failure Read More September 5, 2024 The G protein-coupled receptor ADGRG6 maintains mouse growth plate homeostasis through IHH Signaling Read More Read more Adhesion GPCR articles Articles from Ecosystem Contributors April 2, 2024 GPCRs are not simple on-off switches: deep dive into GPCR-ligand interactions Read More April 16, 2024 From DNA day to GPCR genomics Read More May 14, 2024 Illuminating GPCR Research: FRET and BRET-Based Sensors Shed Light on Cellular Signaling Read More Read more articles from our Contributors Call for GPCR papers August 29, 2024 Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology Read More September 6, 2023 opnMe GPCR Route 66+ project Read More October 1, 2022 GPCRs: Signal Transduction Read More GPCR Binders, Drugs, and More November 12, 2024 Kinetic Basis for the Design of Azobenzene-Based Photoswitchable A2a Adenosine Receptor Ligands Read More November 1, 2024 PGE2 Binding Affinity of Hemocyte Membrane Preparations of Manduca sexta and Identification of the Receptor-Associated G Proteins in Two Lepidopteran Species Read More October 1, 2024 Target-based discovery of antagonists of the tick (Rhipicephalus microplus) kinin receptor identifies small molecules that inhibit midgut contractions Read More Receptor Activation and Signaling in GPCRs November 16, 2024 A non-canonical mechanism of GPCR activation Read More November 14, 2024 cGMP-dependent pathway and a GPCR kinase are required for photoresponse in the nematode Pristionchus pacificus Read More November 8, 2024 Visualization of endogenous G proteins on endosomes and other organelles Read More UniversityPrice Premium Monthly $ 24.99 24.99$ Every month Immerse yourself into the GPCR World Valid for 12 months + 5 day free trial Start Free Trial Live and Recorded Courses Exclusive access to early bird special Access to previous events recordings Premium Yearly $ 249.99 249.99$ Every year Immerse yourself into the GPCR World 5 day free trial Start Free Trial Live and Recorded Courses Exclusive access to early bird special Access to previous events recordings Become Dr. GPCR Strategic Partner

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Principles of Pharmacology in Drug Discovery II Advanced Methods for the Optimization of Candidate Selection Dr. Terry Kenakin Advanced Methods for the Optimization of Candidate Selection This course continues with the basics learned in Course 1 and extends the ideas to apply GPCR utilization in drug therapy . Specifically, the ideas discussed cover the complex pleiotropic behaviors of GPCRs and how these may be exploited for new drug discovery. Receptor data shows how GPCR control of cellular function goes far beyond simple second messenger production (i.e., calcium, cAMP), and these new behaviors are being used to create novel GPCR therapies. The five-lecture series describes essential additional elements to GPCR discovery programs that extend the discovery process and increase therapeutic opportunity. Registrants will learn: 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. Registrations start on Monday, July 15th, 2024 Classes will be live from Zoom on Thursdays from 10 am to 11:30 am EST. Sessions will include a 1-hour live lecture plus 30 minutes of Q&A. Participants who complete the course will get an online certification signed by the professor and the Dr.GPCR Team. A splendid time is guaranteed for all. What are the main objectives of the course? Allow registrants to appreciate the great versatility of GPCRs and how small molecules can affect their behavior for therapeutic benefit. What will students gain from taking this course? Learn how to therapeutically exploit GPCRs (Physiology’s ‘Swiss Army Knife’) wide repertoire of ways to control cell function. Apply unique pharmacologic assays and unconventional ligands to unveil GPCR activities. Adjust ligand kinetics and tissue disposition for optimal therapeutic activity. Are there any specific textbooks or readings students should be aware of? Pharmacology in Drug Discovery and Development (3rd ed.) T>P> Kenakin, Elsevier or ''A Pharmacology Primer' (6th ed.) T.P. Kenakin, Elsevier. Register today! Early-bird registration is over. Principles of Pharmacology II $ 675 675$ +$20.25 Transaction fee Advanced Methods for the Optimization of Candidate Selection Valid for 6 months Select Subscribe to Dr. GPCR's Newsletter to be the first to know about the next courses! What would you like to learn today?

CINVESTAV, Mexico City, Mexico October 23-25 Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE Oct 23 - 9:00 AM Registration & Coffee with light breakfast Read More 9:50 AM Welcoming Remarks Read More 10:00 AM Student Flash Presentations Health and Disease, Metabolism, Nervous System, Proteomics and Transcriptomics, Receptor Structure, Signaling and Activation Mechanism Abhishek Kumar Singh · Alex Torrelli-Diljohn · Emmanouil Kyrloglou · Vasiliki Karagiannakou · Lara-Sophie Brodmerkel · Rashed Rezwan Parag · Hailey Steichen · Tyler Bernadyn · Jesse Stillwell Read More 12:00 PM Coffee Break with lights snacks Read More 12:30 PM State of the Art Talk Adhesion GPCR in Mechanobiology Tobias Langenhan Read More 1:00 PM Plenary Lecture Identification and Functional Characterization of Adhesion GPCRs As Steroid Hormone Receptors and Hearing and Balance Receptors Jinpeng Sun Read More 2:00 PM Complimentary Lunch Read More 3:00 PM Session I Tethered agonist - dependent/independent activation mechanism in AGPCRs Signe Mathiasen · Demet Araç · Andrew Dates · Frank Kwarcinski · Peng Xiao Read More 4:30 PM Leaving for City Center Read More 5:00 PM Mexico City Nocturnal Tour, Food and drinks Read More Oct 24 - 9:00 AM Session II AGPCR signaling pathways and trafficking Yuling Feng · Monserrat Avila Zozaya · Erwin G. Van Meir · Pal Kasturi Read More 10:30 AM Coffee Break with lights snacks Read More 11:00 AM Session III Molecular tools and biosensors directed at AGPCR signaling and function Stephanie Häfner · Laurent Sabbagh · Ana Lilia Moreno Salinas Read More 12:00 PM Session IV AGPCRs signaling in the nervous system Joseph Duman · Simeon R. Mihaylov · Anne Bormann Read More 1:00 PM Complimentary Lunch Read More 2:00 PM Posters Caroline Formstone · Jianxiang Xue · Virginea de Araujo Farias · Szymon P. Kordon · Tingzhen Shen · Bill Huang · Júlia Rosell · Sheila Ribalta-Mena · Mariam Melkumyan Read More 3:00 PM Session V Structural mechanisms of AGPCR signaling and function Fabian Pohl · Sumit Bandekar · Florian Seufert Read More 4:00 PM Board meeting/General assembly Welcome to Join Read More 5:00 PM Leave for dinner reception Read More 5:30 PM Complimentary Reception dinner Read More Oct 25 - 9:00 AM Session VI AGPCRs shaping the nervous system Yimin Zou · Dimitris Placantonakis · Nicole Perry-Hauser Read More 10:00 AM Coffee Break with lights snacks Read More 10:30 AM Session VII Physiological and pathological roles of AGPCRs in the nervous system Beatriz Blanco Redondo · Willem Berend Post Read More 11:10 AM Dr. GPCR Community Presentation Monserrat Avila Zozaya Read More 11:30 AM Session VIII Physiological and pathological roles of AGPCRs in the periphery Cheng-Chih Hsiao · Anastasia Georgiadi · Douglas Tilley Read More 12:30 PM Complimentary Lunch Read More 1:30 PM Session VIII * Physiological and pathological roles of AGPCRs in the periphery Tobias Langenhan · Anastasia Georgiadi · Douglas Tilley · Hee-Yong Kim · Alain Garcia De Las Bayonas · Gabriela Aust Read More 2:50 PM Session IX / Technology capsule: Light on aGPCR signaling and function NovoiSMART - A new platform for GPCR antibody drug discovery Gavin Zhang Read More 3:20 PM Coffee Break with pastries announcement of the aGEM award Read More 4:00 PM Closing remarks Read More Jinpeng Sun Identification and Functional Characterization of Adhesion GPCRs As Steroid Hormone Receptors and Hearing and Balance Receptors Bill Huang Self-Cleavage of GPR110 SEA Domain and Its Impact on GAIN Domain Autoproteolysis Andrew Dates Heterogeneity of Tethered Agonist Signaling in Adhesion G Protein-Coupled Receptors Pal Kasturi Site Specific N-Glycosylation Of The N-Terminal Fragment Of ADGRG6 Drives Proteolytic Processing, Trafficking And Signalling Ana Lilia Moreno Salinas Characterizing hADGRE5/CD97 Activation and Signaling: A Mechanical Stimulation BRET-Based Approach (MS-BRET) Florian Seufert Unveiling the GPS Cleavage Mechanism in ADGRL1 with QM/MM Willem Berend Post The Adhesion GPCR Latrophilin Interacts With The Notch Pathway To Control Germ Cell Proliferation Tobias Langenhan The CELSR/ADGRC Homolog Flamingo Is Not Autoproteolytically Processed By The GAIN Domain Rashed Rezwan Parag Novel isoforms of adhesion G protein coupled receptor B1 (ADGRB1/BAI1) generated from an alternative promoter in intron 17 Emmanouil Kyrloglou GPR124 Mediates Adhesion Of Leukemic Stem Cells To Their Niche And Leads To Myeloid Skewing Virginea de Araujo Farias Anti-Tumorigenic Role of Brain Angiogenesis Inhibitor 3 (BAI3) in WNT-Activated Medulloblastomas Szymon P. Kordon Conformational And Functional Coupling Between Extracellular and Transmembrane Regions of a Holo-Adhesion GPCR Frank Kwarcinski Discriminating between the extracellular scaffolding and G protein signaling roles of GPR56/ADGRG1 via the characterization of a non-cleavable point mutant knock-in mouse, H381S Erwin G. Van Meir Adhesion GPCR BAI1/ADGRB1 can block IGF1R-mediated growth signalling, increase radiosensitivity and augment survival in medulloblastoma. Laurent Sabbagh bioSens-All: A Multiparametric BRET-Based Platform for Comprehensive Profiling of adhesion GPCR Signaling and Pharmacology-Enabling Drug Discovery Fabian Pohl Structural Determinants Of GAIN Domain Autoproteolysis And Cleavage Resistance Of Adhesion G Protein-Coupled Receptors Beatriz Blanco Redondo Uncovering the signaling pathway of the ADGRA homolog Remoulade in Drosophila Douglas Tilley ADGRF5-mediated regulation of cardiac health and disease Abhishek Kumar Singh Adgrg6/Gpr126 is Required for Myocardial Notch Activity and N-cadherin Localization to Attain Trabecular Identity Lara-Sophie Brodmerkel GAIN Domain Dynamics And Its Relevance For Adhesion GPCR Signaling In Vivo Caroline Formstone Interrogating The Role Of CELSR1 (ADGRC1) In Breast Cancer Mariam Melkumyan GPR110 modulates anxiety-like behaviors and memory function in mice potentially through neuronal and neuroimmune alterations during neurodevelopment Signe Mathiasen Signaling Properties of ADGRL3 Monserrat Avila Zozaya The ADGRF5/GPR116 receptor is a key regulator of lymphatic endothelial cell identity and function Simeon R. Mihaylov Bai1 Is A Novel Neuronal Substrate Of The Psychiatric Risk Kinase TNIK Sumit Bandekar Structural studies of the CELSR1 extracellular region reveal a compact multidomain module of fourteen domains which regulates signaling Nicole Perry-Hauser Adhesion G protein-coupled receptor latrophilin-3 (ADGRL3) modulation of dopaminergic neurotransmission Anastasia Georgiadi Adhesion GPCR GPR116/Adgrf5 controls a lineage of anti-thermogenic adipocytes with implications for adaptive thermogenesis during prolonged cold exposure Jesse Stillwell Next Generation MBD2 inhibitors for Brain Cancer Therapy Hailey Steichen Identification of Differentially Expressed Gpr116 (Adgrf5) Transcript Variants in Mouse Kidney Sheila Ribalta-Mena Endocytic Cues Determine the Signaling Profile of Adhesion GPCR ADGRL1 / Latrophilin-1 Jianxiang Xue Generation and characterization of collecting duct specific GPR56 knockout mice Demet Araç An ECR-Mediated and TA-independent Mechanism of aGPCR Activation: Direct Communication of Extracellular Region with Transmembrane Domain in a Holo-Adhesion GPCR Yuling Feng Localization of putative ligands for adhesion G protein-coupled receptors in mouse tissues. Joseph Duman BAI1/ADGRB1-mediated Regulation of Mitochondrial Morphology in Axons Yimin Zou ADGRCs in glutamatergic synapse formation, maintenance and degeneration Cheng-Chih Hsiao ADGRG1/GPR56 regulates survival of terminally differentiated CD8+ T cells Alain Garcia De Las Bayonas The Adhesion GPCR Cupidon Regulates Mating In The Closest Relatives Of Animals Alex Torrelli-Diljohn Investigating The Role of ADGRB3 Loss of Expression in Brain Tumor Formation in Li-Fraumeni Syndrome Tyler Bernadyn Elucidating The Role Of GPR97/ADGRG3 In Neutrophil Biology Tingzhen Shen Deorphanization Of The Adhesion GPCRs GPR110 and GPR116 Júlia Rosell Tethered Agonist Dependent ADGRL3 Signaling Activity In The G12/13 Pathway Peng Xiao Tethered Peptide Activation Mechanism of Adhesion GPCRs Stephanie Häfner The NTF Release Sensor Approach for Drug Discovery for Human Adhesion GPCRs Anne Bormann Intricacies Of Complex Assembly And Ligand Interaction In The Adhesion GPCR Latrophilin/Cirl Dimitris Placantonakis Antibody-drug conjugates targeting CD97 in glioblastoma Gabriela Aust Critical role for CD97/ADGRE5 in the induction of allergic airway inflammation Hee-Yong Kim Characterization of Phenotypes Associated with GPR110 Deletion Vasiliki Karagiannakou A single cell GPCR map of thermogenic fat Gavin Zhang NovoiSMART - A new platform for GPCR antibody drug discovery

Principles of Pharmacology in Drug Discovery I Techniques for Effective Lead Optimization of Candidate Molecules Dr. Terry Kenakin Techniques for Effective Lead Optimization of Candidate Molecules GPCRs have been and arguably still are the most prolific and fertile therapeutic drug targets; this course describes the essential pharmacologic techniques and knowledge required to create a GPCR Target Program aimed at the discovery of new Drugs. The course will focus on the methods used to quantify GPCR ligand activity (agonists, antagonists, modulators) and the process of characterizing the mechanism of action of ligands to enable the prediction of activity in vivo systems. In general, registrants will receive a comprehensive understanding of the unique science of pharmacology and how it can describe drug action in system-independent ways. Registrants will learn: Essentials of measuring pharmacologic activity of ligands (affinity, efficacy, co-operativity). Application of this knowledge to determine the mechanism of action of new GPCR ligands. The required elements of a comprehensive and effective GPCR Discovery. Modules: October 3rd: GPCR Project Initiation and Design for Discovery of New Molecules. October 10th: Drug Affinity: Measurement of Antagonism (Binding and Function) / Classifying Antagonists. October 17th: Agonists and Efficacy: A New World of GPCR Efficacies / Biased Signaling. October 24th: Allosteric Modulators: NAMs, PAMs, Special Properties, Methods to quantify the allosteric effect. Registrations start on Monday, July 15th, 2024. Classes will be live from Zoom on Thursdays from 10 am to 11:30 am EST. Sessions will include a 1-hour live lecture plus 30 minutes of Q&A. Participants who complete the course will get an online certification signed by the professor and the Dr.GPCR Team. A splendid time is guaranteed for all. Registration over Subscribe to Dr. GPCR's Newsletter to be the first to learn about the next courses! What would you like to learn today?

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Dr.GPCR Courses FAQ Dr. Terry Kenakin Principles of Pharmacology in Drug Discovery I Techniques for Effective Lead Optimization of Candidate Molecules Details Dr. Terry Kenakin Principles of Pharmacology in Drug Discovery II Advanced Methods for the Optimization of Candidate Selection Details Dr. Terry Kenakin Applying Pharmacology to Drug Discovery Watch Dr. Samuel Hoare Advanced data analysis for GPCR pharmacology Watch Premium Membership Sign up to watch the recordings and get the early-bird specials (25% Off) for the next courses Premium Monthly $ 24.99 24.99$ Every month Immerse yourself into the GPCR World Valid for 12 months + 5 day free trial Start Free Trial Premium Yearly $ 249.99 249.99$ Every year Immerse yourself into the GPCR World 5 day free trial Start Free Trial Become Dr. GPCR Strategic Partner What are the benefits of becoming a member of Dr.GPCR? As a member, you can access: Dr.GPCR Podcast videos Live GPCR events Weekly classified GPCR news Contributor articles As a premium member, you can access all the free features plus: GPCR courses with a 25% discount Private groups 30+ Symposia recorded talks GPCR Job listings GPCR Event listings Direct access to members of the GPCR community How do I sign up for a membership? To sign up, click the 'Log In/Sign Up' button at the top of the homepage and fill out the registration form. Once your registration is complete, you will receive a confirmation email. Why do I need to fill out a form and wait for approval? We carefully screen anyone signing up to the Ecosystem to ensure they are real humans working on GPCRs. We want to keep our community exclusive to the field, so we need as much information as possible to verify your identity. How long will the Sign-Up process take? We could take up to two (2) business days. I’m just a student starting in the field. 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Dr. GPCR Podcast << Back to podcast list Dr. Yamina Berchiche About Dr. Yamina Berchiche Dr. Yamina A. Berchiche is the founder of Dr. GPCR, an ecosystem designed to bring together stakeholders interested in using G-Protein Coupled Receptors (GPCRs) that control virtually everything in the body as drug targets. The mission of Dr. GPCR is to accelerate GPCR drug discovery by sharing the latest research and technology advances in the field and providing exposure to scientists through the Dr. GPCR podcast. Dr. Berchiche obtained her Master’s and Ph.D. in Biochemistry at the University of Montreal in Canada before training at Rockefeller University in New York and the National Institutes of Health in Bethesda, Maryland. She developed expertise over the past two decades studying structure/function relationships of GPCRs using live-cell bioluminescence resonance energy transfer (BRET). Her work focused on chemokine receptors, members of the GPCR family that control cell movement in the body. Dr. Yamina Berchiche on the web Website LinkedIn Facebook Twitter ResearchGate PubMed Google Scholar Dr. GPCR Ecosystem Thanks for listening to this podcast episode This short survey will help us understand your needs to bring you exciting and informative content; this short survey should take 5 minutes to fill. Listen and subscribe to where you get your podcasts. << Previous Podcast Episode Next Podcast Episode >>

Dr. GPCR Podcast << Back to podcast list Dr. Sudha Shenoy About Dr. Sudha Shenoy Dr. Sudha Shenoy is currently an Associate Professor in Medicine & Cell Biology in the Division of Cardiovascular Medicine, Duke University Medical Center. She received her Ph.D. from Oklahoma State University and completed her postdoctoral training with Dr. Robert J. Lefkowitz (Nobel Laureate, 2012) at Duke University. Dr. Shenoy’s postdoctoral research discovered that ubiquitination of mammalian G protein-coupled receptors is a tag for lysosomal degradation, whereas ubiquitination of the adaptor protein, β-arrestin, is a tag for receptor internalization and formation of signaling endosomes. Her laboratory has continued to work on identifying the molecular mechanisms that ascribe ubiquitin code on GPCRs and β-arrestins. Current efforts aim to understand the regulation of GPCR and beta-arrestin signaling in the heart and vascular endothelium by the deubiquitinating enzymes USP20 and USP33. Dr. Sudha Shenoy on the web Duke University Personal Reflections and Words of Wisdom: Story From Dr. Sudha Shenoy LinkedIn Pubmed Dr. GPCR Ecosystem Thanks for listening to this podcast episode This short survey will help us understand your needs to bring you exciting and informative content; this short survey should take 5 minutes to fill. Listen and subscribe to where you get your podcasts. << Previous Podcast Episode Next Podcast Episode >>

Dr. GPCR Podcast << Back to podcast list Dr. Graham Ladds About Dr. Graham Ladds Graham studied Biochemistry at the University of Birmingham before completing a Ph.D. in yeast pheromone signaling at Warwick. He continued to work at Warwick as a post-doc studying pro-hormone convertases before securing a 5-year independent fellowship funded through the NHS. This project enabled him to return to his interest in GPCRs. He progressed through the ranks at Warwick to become an Associate Professor before leaving in 2015 to join the Department of Pharmacology at Cambridge, where he is also a Fellow of St John’s College. In 2020, he was promoted to a Readership/Professor in Receptor Pharmacology and was elected a Fellow of the British Pharmacological Society. His research group uses a combination of pharmacological investigations and mathematical modeling to study factors that control agonist bias at GPCRs. These investigations have enabled him to foster strong collaborations with the pharmaceutical industry (GSK, Takada, and Firmenich) which have recently been enhanced through him being awarded a Royal Society Industry Fellowship to collaborate with AstraZeneca . Dr. Graham Ladds on the web Twitter ResearchGate LinkedIn Google Scholar PubMed Dr. GPCR Ecosystem Thanks for listening to this podcast episode This short survey will help us understand your needs to bring you exciting and informative content; this short survey should take 5 minutes to fill. Listen and subscribe to where you get your podcasts. << Previous Podcast Episode Next Podcast Episode >>

Dr. GPCR Podcast << Back to podcast list Dr. Katarina Nemec About Dr. Katarina Nemec " I am a pharmacist with an interest in systems pharmacology and precision medicine. Since my undergraduate studies, I have been engaged in researching molecular mechanisms that govern human (patho-)physiology and their interplay with drugs. I aim to discover new therapeutic approaches, and druggable molecules or refine canonical drug targets to create drugs with fewer adverse effects. I studied Pharmacy at the University in Ljubljana, Slovenia, and at the University of Bonn, Germany, working initially on the role of prostaglandin receptor EP4 in chronic lymphocytic leukemia. During my PhD studies in Martin Lohse lab at the Max Delbrueck Center in Berlin, I consolidated my knowledge of GPCRs pharmacology while performing various cell-based experiments to understand the binding, activation, and signaling of therapeutically relevant GPCRs. In addition, I generated various optical biosensors based on fluorescence or bioluminescence resonance energy transfer technologies (FRET, BRET) that were used for functional screens with state-of-the-art microscopy and high throughput screening to explain novel ways of GPCR modulation. I am continuing with the development of advanced screening approaches in the Madan Babu lab to progress in the understanding of spatiotemporal regulation of biased GPCR activation and signaling. I want to combine experimental approaches with data-driven discovery and adopt data science methodology to tackle relevant scientific questions on the systems pharmacology level. " Dr. Katarina Nemec on the web Babu Lab ResearchGate Google Scholar ORCID LinkedIn Twitter Dr. GPCR Thanks for listening to this podcast episode This short survey will help us understand your needs to bring you exciting and informative content; this short survey should take 5 minutes to fill. Listen and subscribe to where you get your podcasts. << Previous Podcast Episode Next Podcast Episode >>

Dr. GPCR Podcast << Back to podcast list Exploring Career Paths in GPCR Research with Dr. Jacek Mokrosiński About Dr. Jacek Mokrosiński "Jacek is a Senior Scientist at Novo Nordisk specializing in molecular pharmacology and cell-based screening technologies. He works in a multidisciplinary Chemical Biology team based at the recently established US R&D hub in Lexington, MA. Originally from Łódź, Poland, Jacek completed his Master's degree in Biology, specializing in Biochemistry at the University of Łódź. He then moved to Denmark, where he trained at the University of Copenhagen under supervision of Professor Thue W. Schwartz, and worked closely with Dr Birgitte Holst studying structural and mechanistic properties of ghrelin receptor and GPCRs involved in regulation of metabolism. After completing his Ph.D., he pursued research in genetics of metabolic regulation at the Institute of Metabolic Science - Metabolic Research Laboratories at the University of Cambridge in the team led by Professor I. Sadaf Farooqi. His research aimed at understanding molecular mechanism through which rare genetic variation may lead to or protecting from excessive body weight gain. As part of Farooqi's team, he characterized a series of novel human genetic variants identified in several GPCRs associated with obesity and other metabolic diseases, including GPR10, Melanocortin 4, Serotonin 2C and TRH receptors. Since 2021, Jacek has been working at Novo Nordisk at its research sites in the UK (Oxford) and the US (Indianapolis, Indiana and most recently Lexington, Massachusetts). He is passionate about cell-based in vitro technologies to study mechanistic properties of GPCRs and understanding the dynamics of receptor signalling. He is an avid proponent of close collaboration between industry and academia." Dr. Jacek Mokrosiński on the web ORCID ResearchGate LinkedIn Twitter Dr. GPCR AI Summary AI-generated content may be inaccurate or misleading. Always check for accuracy. Quick Recap Yamina and Jacek discussed their experiences with name mispronunciations, cultural differences, and the importance of a multidisciplinary approach in drug development. They also shared their career journeys, emphasizing the value of being open-minded, proactive, and embracing new opportunities. Lastly, they discussed their research interests, particularly in the field of GPCR, and the importance of method development, integrity, and honesty in scientific research. Next Steps Jacek will collaborate with Alex Romeo on a podcast about transitioning to the industry. In future talks and interviews, Jacek will share his stories and advice about GPCRs. Yamina will schedule a future talk with Jacek about GPCRs as therapeutic modalities. Summary Embracing Cultural Differences and Collaboration Yamina and Jacek shared their experiences with name mispronunciations and variations and discussed the importance of embracing cultural differences. They also discussed their professional backgrounds, highlighting the benefits of a multidisciplinary approach in drug development and the importance of collaboration between academia and industry. They talked about their shared passion for advancing science and improving patient outcomes, and their early interests in science and chemistry. They also shared their appreciation for documentaries showcasing manufacturing processes and the value of true experimentation in scientific research. Jacek's Career Journey and Advice Jacek and Yamina discussed Jacek's career journey, focusing on his experiences, challenges, and lessons learned. Jacek highlighted the importance of being open-minded and proactive, emphasizing that he learned by doing rather than taking specific courses. He also underscored the role of the people around him, expressing gratitude for their guidance and support. His advice was to be ready for changes and to embrace opportunities as they arise. Jacek's career path, which led him from Poland to Denmark and then to the US, exemplified his advice in action. Passion for Science and Career Journeys Yamina and Jacek discussed their passion for science and how it led them to their current careers. Jacek shared his experience of working with Piketa and how he found a job in Seda's lab at Cambridge, where he could immediately contribute due to his technical skills. Yamina agreed with Jacek's sentiments and spoke about her own journey, expressing her happiness in discussing science and reading papers. They emphasized the importance of finding a job that aligns with one's interests and strengths and being open to opportunities. They also highlighted the need for a work-life balance and the joy of a well-done job. Embracing Networking for Professional Growth Jacek and Yamina discussed the importance of building a network and being open to new opportunities. Jacek realized that being introverted doesn't mean he can't benefit from networking and interaction with others. He also highlighted the benefits of attending conferences and engaging with colleagues, sharing examples of how such interactions led to collaborations and new opportunities. Yamina agreed, emphasizing the importance of mental preparation and embracing different social situations, both virtual and in-person. They underscored the value of these interactions for professional growth and encouraged others to adopt a proactive approach to networking. Building Professional Connections Strategies Yamina and Jacek discussed the importance of building professional connections and strategies for introducing oneself to potential contacts. They emphasized the need to be mindful of the other person's time, provide clear explanations for the purpose of the connection, and offer something of value in return. They also highlighted the advantages of using LinkedIn as a tool for networking and the significance of personalizing messages to make a lasting impression. GPCR Research Interests and Collaborations Yamina and Jacek had a deep and engaging discussion about their research interests and achievements, particularly in the field of GPCR. Jacek shared his fascination with the growth hormone secretion receptor and the melanocortin 4 receptor, and their roles in regulating body weight and growth. Yamina, in turn, talked about her work on melanocortin receptors and an upcoming collaboration with a postdoc scientist. They also highlighted the importance of method development, integrity, and honesty in scientific research. The discussion revealed their interest in GPCRs as therapeutic modalities and possible future collaborations. Thanks for listening to this podcast episode This short survey will help us understand your needs to bring you exciting and informative content; this short survey should take 5 minutes to fill. Listen and subscribe to where you get your podcasts. << Previous Podcast Episode Next Podcast Episode >>

Dr. GPCR Podcast << Back to podcast list Dr. Caron Tribute Part 1 About Marc Caron Dr. Caron and his family moved to Durham, NC in 1977, following receipt of his BSc in Chemistry from Laval University and his Ph.D. from the University of Miami. He joined the faculty of Laval University School of Medicine in 1975 and then returned to join Duke’s faculty, where he remained as a James B. Duke Professor until his death. He and his laboratory members studied the mechanisms of action and regulation of hormones and neurotransmitters and how they might underlie brain and behavior disorders such as schizophrenia, Parkinson's disease, attention-deficit hyperactivity disorder, mood disorders, and addiction. Among his many honors, Dr. Caron was an investigator of the Howard Hughes Medical Institute from 1992 to 2004, a member of the American Academy of Arts & Sciences, a fellow of the American Association for the Advancement of Science, and a recipient of the Julius Axelrod Award. An authoritative and prolific scientist, with over 650 scientific publications, he is most beloved as a mentor and his relentless encouragement that shaped the careers of hundreds of scientists worldwide. About our panelists in alphabetical order and the year they first met Dr. Caron Dr. Jeffrey Benovic (1985) Dr. Michel Bouvier (1985) Dr. Kathleen Caron - Co-host- (1970) Dr. Richard Cerione (1985) Dr. Brian Kolbilka (1987) Dr. Frederik Leeb-Lundberg (1984) Dr. Robert Lefkowitz (1973) Dr. Lee Limbird (1973) Dr. David Sibley (1988) Memories our panelists shared with us Thanks for listening to this podcast episode This short survey will help us understand your needs to bring you exciting and informative content; this short survey should take 5 minutes to fill. Listen and subscribe to where you get your podcasts. << Previous Podcast Episode Next Podcast Episode >>

Dr. GPCR Podcast << Back to podcast list Dr. Nicolas Gilles About Dr. Nicolas Gilles "Dr. Nicolas Gilles is an expert in the study of animal toxins. He is pioneering the investigation of animal toxins acting on GPCRs, the largest therapeutic target class. His strongest expertise lies in therapeutic target identification and all the steps from venom manipulations, to in vivo validation. When the pharmacological properties of these new ligands are deemed exceptional, a lead optimization is realized and its therapeutic development initiates through a dedicated start-up." Dr. Nicolas Gilles on the web Google Scholar LinkedIn Dr. GPCR Thanks for listening to this podcast episode This short survey will help us understand your needs to bring you exciting and informative content; this short survey should take 5 minutes to fill. Listen and subscribe to where you get your podcasts. << Previous Podcast Episode Next Podcast Episode >>

Dr. GPCR Podcast << Back to podcast list Jacob Lee & Jin Choe About this episode In this special episode of the Dr.GPCR podcast , I sat down with the co-founders of Genemod . Jacob Lee and Jin Choe met in ninth grade in English class and have been friends since. Although both went to the same college, Jacob and Jin choose different career paths. One day as they were catching up, Jacob shared his struggles of managing samples and an incredible amount of data and projects in the lab with Jin. Our of this need Genemod was born. Today, Genemod has built a freezer management tool and a project management tool where scientists can manage their reagents, samples, and projects on one intuitive platform. The team is planning on building even more tools that will make Genemod the go-to platform for all research scientists to make research more efficient. Genemode on the web Website Jacob Lee on LinkedIn Jacob Lee on Dr. GPCR Ecosystem Jin Choe on LinkedIn Jin Choe on Dr. GPCR Ecosystem Thanks for listening to this podcast episode This short survey will help us understand your needs to bring you exciting and informative content; this short survey should take 5 minutes to fill. Listen and subscribe to where you get your podcasts. << Previous Podcast Episode Next Podcast Episode >>

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Registration Date & Time Thursday, November 2nd / 11:00 AM - 1:30 PM Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Dinner 1 Date & Time Thursday, November 2nd / 8:00 PM Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Atypical Structure and Function of Typical Chemokine Receptors Date & Time Saturday, November 4th / 11:00 AM Abstract Coming Soon About Amy Ramsey "One of the principal efforts of our laboratory is to understand the physiological consequences of NMDA receptor deficiency using genetic mouse models. The NMDA receptor is a subtype of glutamate neurotransmitter receptor that regulates the formation and maintenance of synaptic connections between neurons. It plays an important role in the way that neurons wire together and change the strength of synaptic connections with experience. Our laboratory is interested in the role of NMDA receptors not only on neurons, but also on other cells of the brain such as astrocytes, oligodendrocytes, and endothelial cells. NMDA receptors are implicated in a number of brain disorders including schizophrenia, autism, and epilepsy. Our laboratory has a long-standing interest in the way that NMDA receptors contribute to the symptoms of schizophrenia. Recently, we have focused our efforts on GRIN disorder. This is a rare neurodevelopmental disorder caused by de novo mutations in the GRIN genes that encode NMDA receptors. Although symptoms of GRIN disorder appear very early in childhood, it can take years to reach the right diagnosis through genetic tests. Children with GRIN disorder experience developmental delays, intellectual impairment, visual impairments, and difficulties with daily tasks like talking and walking, feeding and toileting. Many children experience seizures that can be life-threatening. Our laboratory is working to help patients by developing genetically-modified mice that have disease-causing variants in their Grin1 gene. These mice can then be used to test dietary regimens, drugs, and adenoviral gene therapies for their ability to improve specific symptoms. The Ramsey lab uses a combination of biochemical and behavioural approaches to understand the many roles of NMDA receptors and to find treatments for debilitating brain disorders." The Ramsey Lab Amy Ramsey on the web University of Toronto Pubmed Google Scholar LinkedIn Twitter Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

< GPCR News < GPCRs in Oncology and Immunology Leukotriene B4 receptor 2 governs macrophage migration during tissue inflammation Published date December 12, 2023 Abstract "Chronic inflammation is the underlying cause of many diseases, including type 1 diabetes, obesity, and non-alcoholic fatty liver disease. Macrophages are continuously recruited to tissues during chronic inflammation where they exacerbate or resolve the pro-inflammatory environment. Although leukotriene B4 receptor 2 (BLT2) has been characterized as a low affinity receptor to several key eicosanoids and chemoattractants, its precise roles in the setting of inflammation and macrophage function remain incompletely understood. Here we used zebrafish and mouse models to probe the role of BLT2 in macrophage function during inflammation. We detected BLT2 expression in bone marrow derived and peritoneal macrophages of mouse models. Transcriptomic analysis of Ltb4r2-/- and WT macrophages suggested a role for BLT2 in macrophage migration, and studies in vitro confirmed that whereas BLT2 does not mediate macrophage polarization, it is required for chemotactic function, possibly mediated by downstream genes Ccl5 and Lgals3. Using a zebrafish model of tailfin injury, we demonstrated that antisense morpholino-mediated knockdown of blt2a or chemical inhibition of BLT2 signaling impairs macrophage migration. We further replicated these findings in zebrafish models of islet injury and liver inflammation. Moreover, we established the applicability of our zebrafish findings to mammals by showing that macrophages of Ltb4r2-/- mice have defective migration during lipopolysaccharide stimulation in vivo. Collectively, our results demonstrate that BLT2 mediates macrophage migration during inflammation, which implicates it as a potential therapeutic target for inflammatory pathologies." Authors Ebru Ermis , Titli Nargis , Kierstin Webster , Sarah A Tersey , Ryan M Anderson , Raghavendra G Mirmira Tags G-protein coupled receptor (GPCR) , Macrophage , inflammation , metabolism , mouse , zebrafish Source Contribute to the GPCR News Coming soon Become a Contributor Classified GPCR News Call for GPCR papers GPCR Industry News Adhesion GPCRs GPCR Events, Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research GPCRs in Neuroscience GPCRs in Cardiology, Endocrinology, and Taste GPCRs in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling More from Dr. GPCR Create an account and get our contributors articles in your inbox Subscribe to the Dr. GPCR Monthly Newsletter today! Follow the Dr. GPCR News and get weekly notifications about the GPCR field Share < Previous Next >

< GPCR News < GPCRs in Oncology and Immunology Context-dependent ciliary regulation of hedgehog pathway repression in tissue morphogenesis Published date November 9, 2023 Abstract "A fundamental problem in tissue morphogenesis is identifying how subcellular signaling regulates mesoscale organization of tissues. The primary cilium is a paradigmatic organelle for compartmentalized subcellular signaling. How signaling emanating from cilia orchestrates tissue organization-especially, the role of cilia-generated effectors in mediating diverse morpho-phenotypic outcomes-is not well understood. In the hedgehog pathway, bifunctional GLI transcription factors generate both GLI-activators (GLI-A) and GLI-repressors (GLI-R). The formation of GLI-A/GLI-R requires cilia. However, how these counterregulatory effectors coordinate cilia-regulated morphogenetic pathways is unclear. Here we determined GLI-A/GLI-R requirements in phenotypes arising from lack of hedgehog pathway repression (derepression) during mouse neural tube and skeletal development. We studied hedgehog pathway repression by the GPCR GPR161, and the ankyrin repeat protein ANKMY2 that direct cAMP/protein kinase-A signaling by cilia in GLI-R generation. We performed genetic epistasis between Gpr161 or Ankmy2 mutants, and Gli2/Gli3 knockouts, Gli3R knock-in and knockout of Smoothened, the hedgehog pathway transducer. We also tested the role of cilia-generated signaling using a Gpr161 ciliary localization knock-in mutant that is cAMP signaling competent. We found that the cilia-dependent derepression phenotypes arose in three modes: lack of GLI-R only, excess GLI-A formation only, or dual regulation of either lack of GLI-R or excess GLI-A formation. These modes were mostly independent of Smoothened. The cAMP signaling-competent non-ciliary Gpr161 knock-in recapitulated Gpr161 loss-of-function tissue phenotypes solely from lack of GLI-R only. Our results show complex tissue-specific GLI-effector requirements in morphogenesis and point to tissue-specific GLI-R thresholds generated by cilia in hedgehog pathway repression. Broadly, our study sets up a conceptual framework for rationalization of different modes of signaling generated by the primary cilium in mediating morphogenesis in diverse tissues." Authors Sun-Hee Hwang , Kevin Andrew White , Bandarigoda Nipunika Somatilaka , Baolin Wang , Saikat Mukhopadhyay Source Contribute to the GPCR News Coming soon Become a Contributor Classified GPCR News Call for GPCR papers GPCR Industry News Adhesion GPCRs GPCR Events, Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research GPCRs in Neuroscience GPCRs in Cardiology, Endocrinology, and Taste GPCRs in Oncology and Immunology Structural and molecular insights into GPCR function GPCR Activation and Signaling More from Dr. GPCR Create an account and get our contributors articles in your inbox Subscribe to the Dr. GPCR Monthly Newsletter today! Follow the Dr. GPCR News and get weekly notifications about the GPCR field Share < Previous Next >

Advanced data analysis for GPCR pharmacology Dr. Samuel Hoare On Demand 4 modules - 8 hours total Get Started Premium Members benefits: - Subscribe and save 25% on every GPCR Course - Early-bird access - Recordings will be available < Back to GPCR courses Main objectives: Learning how to perform advanced GPCR pharmacology data analysis in support of drug discovery and GPCR research, shown with GraphPad Prism. Understanding the pharmacology data analysis framework we use for GPCRs. Appreciating the practical realities, limitations, and tradeoffs of GPCR data analysis. Learning many tips and tricks to improve your data analysis's quality, reliability, and efficiency. The participants will increase their ability to perform, understand, and communicate GPCR pharmacology data analysis to a high level, as well as expertise that can be applied in drug discovery and target research to maximize the chances of project success. The increased understanding will also be helpful for the participants in their training and education of entry-level scientists. Attendees will be provided with Prism files, Excel templates and simulators, and the PowerPoints of the workshop modules. Modules: Module 1 - Concentration-response analysis: Become a CRC super-user. Module 2 - Quantifying agonist pharmacology and biased agonism. Module 3 - Antagonist pharmacology and binding assay analysis. Module 4 - New dimensions of activity: Allosteric modulators and kinetics. Good to know: Classes will be live from Zoom on Thursdays from 10 am to 12:00 pm EST. Sessions will include a one-hour live lecture plus one hour of Q&A and discussion. Every participant will also have a 1:1 meeting with Dr. Hoare during or after the four weeks, scheduled according to the professor's availability. Participants who complete the course will get an online certification signed by the professor and the Dr.GPCR Team. Watch the recordings *Free for Premium Members Watch Your Instructor Dr. Samuel Hoare Sam Hoare is a pharmacology data analyst with 30 years experience in GPCR pharmacology. He consults with numerous pharmaceutical, biotech, life science and academic organizations in understanding and applying in vitro pharmacology data to advance drug discovery and target research. He regularly teaches courses and publishes chapters and guides on basic and advanced pharmacology and experimental design. Sam is an editor at the NIH Assay Guidance Manual. Sam specializes in kinetic analysis of drug action and is known for applying binding and signaling kinetics to the development of effective therapeutics. He worked as a pharmacology leader in the pharmaceutical industry for 15 years at Neurocrine Biosciences, guiding the in vitro biology efforts for numerous drug discovery campaigns. He completed his Ph.D. in biochemistry, studying allosteric modulation of dopamine receptors, from the University of Kent in the United Kingdom. He completed postdoctoral training at the National Institute of Mental Health, researching the pharmacological mechanisms of Class B GPCRs.

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Welcoming Remarks < Previous Session Next Session >

Dr. GPCR Podcast << Back to podcast list Lauren Celano About this episode In this special Dr. GPCR podcast episode, we sat down to chat with Lauren Celano to talk about career options for Ph.D.’s. Working in a lab allows scientists to gain amazing hard and soft skills, which opens the doors to several great careers that many have not even considered, yet. Lauren has a science background and is passionate about helping talented scientists find their dream position. She is also a speaker, connector, recruiter, and coach. Lauren Celano on the web LinkedIn Propel Careers Email: Lauren@propelcareers.com Dr. GPCR Ecosystem Thanks for listening to this podcast episode This short survey will help us understand your needs to bring you exciting and informative content; this short survey should take 5 minutes to fill. Listen and subscribe to where you get your podcasts. << Previous Podcast Episode Next Podcast Episode >>

Symposia Imm&Onc Live Talks < Back to Poster Presentations This is a Title 01 Previous Next

Dr. GPCR Podcast << Back to podcast list Dr. Yamina Berchiche About this episode In this Episode 0 of the brand new Dr. GPCR podcast , your host and founder, Dr. Yamina Berchiche introduces the very first podcast dedicated to GPCRs researcher and their work. This podcast is part of the Dr. GPCR Ecosystem, with the goal is to bring together GPCR scientists, biotech, and pharma leaders as well as suppliers working on GPCRs by providing opportunities to connect, share, form trusting partnerships, grow, and thrive together to accelerate GPCR drug discovery and improve human health. Dr. Yamina Berchiche on the web - Website - LinkedIn - PubMed - Twitter - Facebook - Dr. GPCR Ecosystem Thanks for listening to this podcast episode This short survey will help us understand your needs to bring you exciting and informative content; this short survey should take 5 minutes to fill. Listen and subscribe to where you get your podcasts. << Previous Podcast Episode Next Podcast Episode >>