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  • GPCRs in Pharmacology

    This comprehensive course is designed to provide an in-depth exploration of key concepts in pharmacology, offering a nuanced understanding of drug interactions and mechanisms of action. The curriculum is divided into four modules, each focusing on essential aspects of pharmacological principles. Whether you are a healthcare professional, researcher, or student in the life sciences, this course will enhance your knowledge and critical thinking skills in the field of pharmacology.

  • Step 1

    Start off your program by giving some basic information about what participants can expect to learn. Introduce the topic and provide a basic outline of what's to come. Consider adding a questionnaire to ask participants what they hope to take away from the experience, or a quiz to test their understanding before getting started.

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    Break down your content into manageable steps. Use videos, images, and text to explain your main points, and set clear expectations and goals. You can also include files and audio as additional resources.

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Posts (543)

  • 📰 GPCR Weekly News, May 13 to 19, 2024

    Hello everyone! Make sure you get our latest coverage of GPCRs for this week. We've got 15 insightful GPCR research papers and updates from the industry. Stay informed and up to date with the latest GPCR research and industry news. This week's highlight includes congrats to: John Teye Azietaku for his first contributor article on Illuminating GPCR Research: FRET and BRET-Based Sensors Shed Light on Cellular Signaling Abigail Walker, Aylin Hanyaloglu, et al., for their study on Constitutive internalisation of EP2 differentially regulates G protein signalling Ethan Dintzner, Demet Araç, et al. for their work on The far extracellular CUB domain of the adhesion GPCR ADGRG6/GPR126 is a key regulator of receptor signaling Jiankun Lyu, Brian Shoichet, Bryan Roth, et al. for their research on AlphaFold2 structures guide prospective ligand discovery Dr. GPCR University We launched the Dr.GPCR University workshop on Advanced Data Analysis for GPCR Pharmacology led by Dr. Sam Hoare three weeks ago, and it's been fantastic with all the participants from across the world. Mark your calendars for September and October 2024! We are excited to announce that Dr. Terry Kenakin will return with two back-to-back classes. Stay tuned for further details, as we plan to open registrations for both courses in July 2024. Dr. GPCR Podcast Exciting news! Episode 152 with Dr. Arthur Christopoulos is now live, titled "A Brief History of Allosteric Modulators." Dive into this fascinating topic and gain valuable insights from one of the leading experts in the field. Don't miss out—check it out now! And here's something even better: the video versions of our podcast episodes are now available to the public on our website! Re-watch your favorite episodes and catch up on any you have missed. Our most recent episode features our very own Dr. GPCR Board. Tune in and enjoy! Dr. GPCR Matchmaking Meet Mark Schmeizl, our Chief Matchmaker. Whether you’re hiring top talent or seeking a new career opportunity, Mark’s expertise ensures successful matches. Ready to get started? If you're looking to hire, fill out this form. If you want to be hired, fill out this form. And don’t miss our job opportunity spotlight for a Principal Scientist in In Vitro Pharmacology! Mark discussed this position with Beth Fleck, Director of In Vitro Pharmacology at Crinetics Pharmaceuticals! Dr. GPCR Symposia Explore GPCRs with our Premium Membership! Access recorded material from previous events, including the Dr. GPCR Summit editions. Our symposium on Structural Insights into GPCR Activation is postponed. Mark your calendar for the GPCRs as Therapeutic Targets symposium on October 11th, 2024. In the meantime, visit Dr. GPCR Symposia and learn from experts in the field. GPCR Event Highlight We are thrilled to announce our first in-person event in collaboration with the Adhesion GPCR Consortium: The 11th Adhesion GPCR Workshop, which will be held in vibrant Mexico City from October 23 to 25, 2024. Get ready to share your research with the global GPCR community! Submit your abstract using this form. We are also seeking sponsors to support this exciting event, which unites scientists worldwide to explore all facets of adhesion GPCR biology. If you're interested in sponsoring, please email us at Hello@DrGPCR.com. Let’s dive into the Classified GPCR News from May 13th to 19th, 2024. GPCR Activation and Signaling Constitutive internalisation of EP2 differentially regulates G protein signalling ArreSTick motif controls β-arrestin-binding stability and extends phosphorylation-dependent β-arrestin interactions to non-receptor proteins Identification of Gα12-vs-Gα13-coupling determinants and development of a Gα12/13-coupled designer GPCR GPR160 regulates the self-renewal and pluripotency of mouse embryonic stem cells via JAK1/STAT3 signal pathway A fluorescently-tagged tick kinin neuropeptide triggers peristalsis and labels tick midgut muscles The far extracellular CUB domain of the adhesion GPCR ADGRG6/GPR126 is a key regulator of receptor signaling GPCR Binders, Drugs, and more Silicon-Rhodamine Functionalized Evocalcet Probes Potently and Selectively Label Calcium Sensing Receptors In Vitro, In Vivo, and Ex Vivo GPCRs in Neuroscience Novel pharmacological targets for GABAergic dysfunction in ADHD GPCRs in Oncology and Immunology Exploration of prognostic and treatment markers in hepatocellular carcinoma via GPCR-related genes analysis Reviews, GPCRs, and more GPR56, an Adhesion GPCR with Multiple Roles in Human Diseases, Current Status and Future Perspective Structural and Molecular Insights into GPCR Function A homotrimeric GPCR architecture of the human cytomegalovirus revealed by cryo-EM Antibodies expand the scope of angiotensin receptor pharmacology Structural and dynamic insights into the activation of the μ-opioid receptor by an allosteric modulator Structural Insights into Partial Activation of the Prototypic G Protein-Coupled Adenosine A2A Receptor AlphaFold2 structures guide prospective ligand discovery Industry News Roche reports positive Phase Ib results for its dual GLP-1/GIP receptor agonist CT-388 in people with obesity Septerna to Present Preclinical Data from GPCR Drug Discovery Engine at ENDO 2024 𝐈𝐧𝐭𝐫𝐨𝐝𝐮𝐜𝐢𝐧𝐠 𝐀𝐋𝐋𝐎𝐃𝐃: 𝐀𝐥𝐥𝐨𝐬𝐭𝐞𝐫𝐲 𝐢𝐧 𝐃𝐫𝐮𝐠 𝐃𝐢𝐬𝐜𝐨𝐯𝐞𝐫𝐲 GPCR Events, Meetings, and Webinars May 27 - 29, 2024 | SLAS Europe 2024 Conference and Exhibition June 2 - 7, 2024 | Chemotactic Cytokines NEW 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 Research Associate/Associate Scientist, Protein Science NEW 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

  • Dynamic GPCR activation revealed through time-resolved Cryo-EM

    Human cells express over 800 G-protein-coupled receptors (GPCRs) to facilitate communication with the external environment. These receptors respond to a variety of signals by undergoing structural changes that activate internal G proteins, β-arrestins, and other transducers1. Capturing the dynamics of GPCR activation has always been a challenge because G protein activation in cells occurs in less than a second, reflecting the transient nature of these active states. A recent breakthrough study published in Nature by Makaía M. Papasergi-Scott and colleagues has made significant progress in this area 2. Using time-resolved cryo-electron microscopy (cryo-EM) and variability analysis to monitor the transitions of the Gs protein in complex with the β2-adrenergic receptor (β2AR) at brief sequential intervals following GTP addition, the research team identified the conformational changes that underlie G protein activation and its separation from the receptor. Twenty transition structures generated from overlapping particle subsets along this pathway provide a high-resolution description of the events driving G protein activation upon GTP binding. Unlike previous studies that provided only static snapshots, this approach captures the entire activation sequence in vivid detail. The captured structures reveal a dynamic of conformational changes initiated by the binding of an agonist isoproterenol to β2AR. This interaction significantly increases the receptor’s affinity for GTP, allowing a detailed observation of its interaction with the Gs protein in its activated state. From the initial GTP binding, the structures highlight critical shifts in the α5 helix and the α-helical domain (AHD) of the G protein. These alterations are essential for the complex mechanism of G protein activation, following GTP association with the Gα NTP binding pocket. The activation process begins with the α-helical domain (AHD) of the G protein in an open state, which is crucial for the initial binding of GTP. This early interaction sets the stage for a cascade of significant conformational changes. As GTP stabilizes and migrates towards the P loop, it causes the TCAT motif to shift, a key movement for the subsequent closure of the AHD. Concurrently, the α1 helix extends, propagating structural changes throughout the G protein. Further changes include the movement of Switch II towards the nucleotide-binding pocket and the stabilization of Switch III, both integral to the activation of the G protein. The AHD transitioning to a closed conformation prompts the β2–β3 loop to move away from the α5 helix, disrupting an ionic lock and allowing the α5 helix to start transitioning. This helix undergoes significant restructuring—it breaks and reforms closer to the TCAT motif, which is crucial for the final steps of G protein activation. This detailed process provided by the cryo-EM study offers a clear view of these dynamic states, from an inactive state (open AHD and GTP unbound) to an active state (closed AHD and GTP bound) and ultimately to the dissociation of the G protein from the receptor. This research not only deepens our understanding of a key biological process but also provides a valuable map for pharmaceutical researchers to design new therapies. With this high-resolution, dynamic view of GPCR activation, scientists can better tackle diseases by targeting specific steps within the G-protein activation cycle. This highlights the power of advanced imaging techniques like cryo-EM in solving complex biological puzzles and underscores the importance of understanding cellular processes at the molecular level for therapeutic advancements. Beyond GPCRs, the methods and insights from this study can be applied to other fast, transient biological processes. This approach is valuable for understanding the dynamics of other complex signaling pathways and molecular interactions, offering a deeper understanding of cellular processes at the molecular level. Premont, R. T. & Gainetdinov, R. R. Physiological roles of G protein-coupled receptor kinases and arrestins. Annu Rev Physiol 69, 511-534 (2007). Papasergi-Scott, M. M. et al. Time-resolved cryo-EM of G-protein activation by a GPCR. Nature (2024).

  • 📰 GPCR Weekly News, May 6 to 12, 2024

    Hello everyone! Don't miss out on our latest coverage of GPCRs for this week. We have a total of 34 insightful GPCR research papers and seven updates from the industry. Stay informed and up to date with the latest GPCR research and industry news. This week's highlight includes congrats to: Drs. Sara Marsango and Graeme Milligan for their research on the Regulation of the pro-inflammatory G protein-coupled receptor GPR84 Drs. Chakit Arora, J Silvio Gutkind, and Francesco Raimondi for their work on The landscape of cancer-rewired GPCR signaling axes Affiong Ika Oqua, Dr. Alejandra Tomas, et al. for their study on Lipid regulation of the glucagon receptor family Drs. Naveen Thakur, Kenneth A Jacobson, Matthew T Eddy, et al. for their analysis on Membrane mimetic-dependence of GPCR energy landscapes Dr. GPCR University We successfully started our Dr.GPCR University workshop, 'Advanced Data Analysis for GPCR Pharmacology,’ led by Dr. Sam Hoare. Mark your calendar for September and October 2024. Dr. Kenakin will be back with two back-to-back classes. Stay tuned as we plan to open registrations for both classes in July 2024. Dr. GPCR Podcast Episode #151 is out! A special episode with our board, meet Drs. Maria Waldhoer, JoAnn Trejo, and Anne Marie Quinn. Did you watch Episode #150 of the Dr. GPCR Podcast? Join us in this episode to meet the team behind Dr. GPCR, hear anecdotes, and get important announcements. Tune in and be the first to know about the benefits coming your way! Dr. GPCR Matchmaking Mark Schmeizl, our Chief Matchmaker, can help you find your perfect match if you want to hire or be hired. 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. Dr. GPCR Symposia Learn more about GPCRs by signing up for a Premium Membership to watch all the material recorded at our previous events, including the three editions of the Dr. GPCR Summit. We have postponed our symposium on Structural Insights into GPCR Activation to a later date. Stay tuned for our next symposium on GPCRs as Therapeutics Targets on October 11th, 2024. In the meantime, visit Dr. GPCR Symposia and learn from experts in the field. GPCR Event Highlight We are thrilled to partner with the Adhesion GPCR Consortium to organize our first Dr. GPCR in-person event. Mark your calendar for October 23 - 25, 2024, as we kick off the 11th Adhesion GPCR Workshop in Mexico City. Abstract submissions and registrations will open soon. Stay tuned We are also looking for sponsors to help support this fabulous event that brings together scientists worldwide working on all aspects of adhesion GPCR biology. Please reply to this email if you'd like to sponsor this event. Let’s dive into the Classified GPCR News from April 29th to May 12th, 2024 Adhesion GPCRs Essential Role of Latrophilin-1 Adhesion GPCR Nanoclusters in Inhibitory Synapses Embryonic spatiotemporal expression pattern of Folded gastrulation suggests roles in multiple morphogenetic events and regulation by AbdA GPCR Activation and Signaling The critical importance of conditions: Reconciling GPCR functionality and biophysical findings Adrenoceptor Desensitization: Current Understanding of Mechanisms Biased agonists of GPR84 and insights into biological control GPR84 in physiology-Many functions in many tissues Regulation of the pro-inflammatory G protein-coupled receptor GPR84 Function and regulation of GPR84 in human neutrophils Large-scale deorphanization of Nematostella vectensis neuropeptide G protein-coupled receptors supports the independent expansion of bilaterian and cnidarian peptidergic systems GPCR Binders, Drugs, and more A relaxin receptor gene RpGPCR41 is involved in the resistance of Rhopalosiphum padi to pyrethroids Discovering allatostatin type-C receptor specific agonists Discovery of the Clinical Candidate IDOR-1117-2520: A Potent and Selective Antagonist of CCR6 for Autoimmune Diseases MRGPRX4 mediates phospho-drug-associated pruritus in a humanized mouse model GPCRs in Cardiology, Endocrinology, and Taste The Genetic Pathophysiology and Clinical Management of the TADopathy, X-Linked Acrogigantism Thrombosis With Thrombocytopenia and Post-COVID-Vaccination Syndrome With Anti-G-Protein-Coupled Receptor (GPCR) Antibodies Treated With Therapeutic Plasma Exchange SUCNR1 regulates insulin secretion and glucose elevates the succinate response in people with prediabetes GPCRs in Neuroscience Spatiotemporal organization of prefrontal norepinephrine influences neuronal activity Transient cAMP production drives rapid and sustained spiking in brainstem parabrachial neurons to suppress feeding The C-terminus of the prototypical M2 muscarinic receptor localizes to the mitochondria and regulates cell respiration under stress conditions GPCRs in Oncology and Immunology Wnt pathway inhibition with the porcupine inhibitor LGK974 decreases trabecular bone but not fibrosis in a murine model with fibrotic bone The orphan G protein-coupled receptor 141 expressed in myeloid cells functions as an inflammation suppressor The landscape of cancer-rewired GPCR signaling axes Methods & Updates in GPCR Research ONE-GO: Direct detection of context-dependent GPCR activity Author Correction: GPCR molecular dynamics forecasting using recurrent neural networks Glycoprotein-glycoprotein receptor binding detection using bioluminescence resonance energy transfer Bayesian network models identify cooperative GPCR:G protein interactions that contribute to G protein coupling Reviews, GPCRs, and more Molecular adaptations in response to exercise training are associated with tissue-specific transcriptomic and epigenomic signatures Lipid regulation of the glucagon receptor family Technologies for the discovery of G protein-coupled receptor-targeting biologics Lipid mediators in neutrophil biology: inflammation, resolution and beyond Exploring GPCR signaling pathway networks as cancer therapeutic targets Generation of comprehensive GPCR-transducer-deficient cell lines to dissect complexity of GPCR signaling Structural and Molecular Insights into GPCR Function Membrane mimetic-dependence of GPCR energy landscapes Structural and Computational Insights into Dynamics and Intermediate States of Orexin 2 Receptor Signaling Industry News Addex Gets Creative To Secure Funding And Its Future Reunion Neuroscience Inc. Announces $103 Million Series A Financing Co-Led by MPM BioImpact and Novo Holdings Neurocrine Biosciences Announces Initiation of Phase 1 Clinical Study Evaluating Effects of NBI-1117567 in Healthy Adults Crinetics Pharmaceuticals Reports First Quarter 2024 Financial Results and Provides Business Update Nxera Pharma Operational Highlights and Consolidated Results for the First Quarter 2024 Crinetics Pharmaceuticals To Present Advancements From Atumelnant (Crn04894) And Paltusotine Development Programs At Endo 2024 Exscientia's CEO shares a pipeline overview and learnings from being one of the first AI companies out front and to go public GPCR Events, Meetings, and Webinars 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 July 8 - 10, 2024 | 4th IRN i-GPCRnet Annual October 2024 | Biologics US 2024 October 2 - 4, 2024 | 9th GPCRs in Medicinal Chemistry July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology 2026 GPCR Jobs Post Doctoral Fellow 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 Join Dr. GPCR Ecosystem

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Other Pages (576)

  • Advanced data analysis for GPCR pharmacology

    < Back Advanced data analysis for GPCR pharmacology 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. Your Instructor Dr. Samuel Hoare ​

  • Applying Pharmacology to Drug Discovery

    < Back Applying Pharmacology to Drug Discovery The main objective of this course is to give the registrant a good overall understanding of the unique science of pharmacology and how it can describe drug action in system-independent ways. This allows predictions of drug activity in all physiological systems, not only the system where testing is done. Techniques will be described to quantify drug activity in terms of affinity, efficacy, and allosteric function. Pharmacology is a unique discipline and is critical to drug discovery. Registrants will learn: Methods to characterize the three major drug types. What makes each drug type unique to therapeutic pharmacology? 3. Essential information is needed to characterize a drug's profile aimed at therapy. Modules: Week 1 - Fundamentals of Pharmacology Week 2 - Characterizing Agonists Week 3 - Characterizing Antagonists Week 4 - Characterizing Allosteric Modulators Good to know Registrations start on December 15th and close on February 2nd. 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. Every participant will also get the chance to have a 1:1 meeting with Dr. Kenakin during 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. A splendid time is guaranteed for all. Your Instructor Dr. Terry Kenakin ​

  • GPCR Courses

    The learning platform for the GPCR enthusiasm The Dr. GPCR Ecosystem is the ultimate resource for expanding your knowledge, making connections, and staying informed in the world of GPCR. Get started - 30 days free trial - Sign up for free! GPCR Courses Applying Pharmacology to Drug Discovery Coming Soon - Sign up for updates Read More Advanced data analysis for GPCR pharmacology Coming Soon - Sign up for updates Read More Premium Monthly $ 24.99 24.99$ Every month Immerse yourself into the GPCR World Valid for 12 months + 30 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 30 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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