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.

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Get ready for an expedition, GPCR explorers! Embark on another exciting exploration of the unknown realms of GPCR research. Welcome back to your weekly GPCR quest! This Week’s Highlights: Congrats to: John Teye Azietaku , our great contributor, for his article Class B1 GPCR Dimerization: Unveiling Its Role in Receptor Function and Signaling Sonja Peter , Brian Bender , Chris De Graaf   for their excellent work on Comparative Study of Allosteric GPCR Binding Sites and Their Ligandability Potential Today, we started the Principles of Pharmacology II   course! Thank you to all participants in Dr. Terry Kenakin's educational initiative this fall! Your dedication has greatly enriched the learning experience. Let’s keep fostering a collaborative environment for sharing ideas and expanding knowledge! We had a blast at the 11th Adhesion GPCR Workshop 2024 ! The 11th Adhesion GPCR Workshop 2024 was a successful event that brought together experts, researchers, and enthusiasts worldwide to explore Adhesion GPCRs. The presentations and discussions sparked new ideas and collaborations, shaping the future of the field. We thank all participants for their inspiring contributions and passion. Classified GPCR News  Let’s dive into the   Classified GPCR News from October 21st to 27th, 2024 Industry News UNC School of Medicine to Receive $3-Million Award from ARPA-H’s Sprint for Women’s Health Nxera Pharma Wins Biotech Company of the Year and Financing Deal of the Year at the Citeline Japan Awards 2024 GPCR therapies: Eight promising biotechs hacking the cell signaling pathway From Structure to Solution: How Structural Biology Informs the Development of Drugs Targeting G Protein-Coupled Receptors Olfactive Biosolutions Establishes Scientific Advisory Board GLP-1s like Ozempic are among the most important drug breakthroughs ever Goldman-backed drug developer Septerna raises $288 mln in US IPO Call for GPCR Papers Deadline: Nov 1, 2024. Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and Webinars November 5 - 7, 2024 | 16th Annual PEGS Europe   November 25 - 27, 2024 | 1st Virtual GPCR Forum Conference November 26 - 28, 2024 | GPCRs-Targeted Drug Discovery Summit Europe July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology GPCR Jobs Scientist I Cell Biology - Tectonic Therapeutic PhD fellowship in GPCR mechanosensing Senior Scientist, GPCR Pharmacology Research Associate - Professor Graeme Milligan Postdoc in Molecular Pharmacology - The Hauser Group Postdoctoral Scholar – iPSC in cardiac and endothelial cell function Protein Biochemist/Structural Biologist Senior Scientist/Staff Scientist, Computational Chemistry GPCR Activation and Signaling A gain of function variant in RGS18 candidate for a familial mild bleeding syndrome Fusarium graminearum Ste2 and Ste3 Receptors Undergo Peroxidase-Induced Heterodimerization when Expressed Heterologously in Saccharomyces cerevisiae The beta 2 adrenergic receptor cross-linked interactome identifies 14-3-3 proteins as regulating the availability of signaling-competent receptors GPCRs in Neuroscience Astrocyte Gi-GPCR signaling corrects compulsive-like grooming and anxiety-related behaviors in Sapap3 knockout mice Orphan GPCRs in Neurodegenerative Disorders: Integrating Structural Biology and Drug Discovery Approaches Altered PLCβ/IP3/Ca2+ Signaling Pathway Activated by GPRCs in Olfactory Neuronal Precursor Cells Derived from Patients Diagnosed with Schizophrenia Sphingosine 1-phosphate receptor subtype 1 (S1P1) activity in the course of Alzheimer's disease GPCRs in Oncology and Immunology Characterization, expressional and evolutionary analysis of five fish-specific CCRs (CCR4La, CCR4Lc, CCR12a1, CCR12a2, and CCR12b) in largemouth bass (Micropterus salmoides) The pyruvate-GPR31 axis promotes transepithelial dendrite formation in human intestinal dendritic cells Methods & Updates in GPCR Research Generation of CRISPR/Cas9 modified human iPSC line with correction of heterozygous mutation in exon 6 of the CaSR gene Reviews, GPCRs, and more Insight into structural properties of viral G protein-coupled receptors and their role in the viral infection: IUPHAR Review 41 Structural and Molecular Insights into GPCR Function Comparative Study of Allosteric GPCR Binding Sites and Their Ligandability Potential Molecular Dynamics (MD) Simulations Provide Insights into the Activation Mechanisms of 5-HT2A Receptors Investigating the Effect of GLU283 Protonation State on the Conformational Heterogeneity of CCR5 by Molecular Dynamics Simulations Become a Premium Member! Get your 5-day free trial TODAY!

G protein-coupled receptors (GPCRs) are membrane-bound proteins that sense external stimuli and relay signals inside the cell, resulting in various physiological outcomes. While GPCRs can exist as monomers, some types, like class C GPCRs, are obligate dimers, either as homodimers or heterodimers, with distinct conformations in both their inactive and active states [1, 2]. The possibility of dimerization in class A and class B GPCRs, however, has been more controversial, despite increasing evidence that these receptors can also form dimers. These dimeric forms, which can either be transient or stable, are believed to influence the function and regulation of GPCRs—a process known as receptor cross-talk [3]. For example, dimerization has been shown to affect signaling pathways in class A dopamine receptors like D1/D2 and D1/D3, which exhibit distinct pharmacological profiles in their dimeric form compared to their monomeric counterparts [4]. Class B1 GPCRs are an important subclass of GPCRs that include 15 receptors involved in regulating body homeostasis and metabolism, and they are activated by peptide hormones [5]. Recent studies suggest that class B1 GPCRs can form both homodimers and heterodimers, which may play a crucial role in modulating receptor function and ligand signaling. These dimeric interactions may contribute to the phenomenon of biased agonism, where ligands produce different signaling outcomes depending on the receptor conformation or dimerization state. Examples of class B1 GPCRs forming homodimers include the secretin receptor (SecR)[6] and GLP-1R [7], while GLP-1R is also known to heterodimerize with the GIPR in recombinant cell system [8]. Research using techniques like bioluminescence resonance energy transfer (BRET) and fluorescence resonance energy transfer (FRET) has revealed that GLP-1R homodimerization occurs via transmembrane helix 4 (TM4), which forms the interface for both homo- and heterodimers [9]. These studies also show that disrupting the dimerization of GLP-1R results in decreased high-affinity binding to its natural ligand, GLP-1, while selectively affecting receptor signaling. Such findings suggest that dimerization is critical for regulating GPCR function, particularly with respect to biased agonism, which may alter downstream signaling outcomes based on the receptor's dimeric state. One of the most intriguing examples of class B1 GPCR dimerization involves the secretin receptor (SecR). SecR dimerization enhances the receptor’s signaling efficiency by increasing its dynamics in a G protein-dependent manner [6]. This dimerization allows the N-terminal activation domain of the receptor to repeatedly engage and disengage from the receptor’s core, which is crucial for G protein recruitment. As a result, dimerized SecR receptors exhibit higher rates of G protein activation and release, improving both binding affinity and signaling potency. Additionally, the dimeric state allows rotational movement of the receptor's extracellular domain (ECD), facilitating the partial disengagement of the peptide while maintaining high-potency signaling. In summary, dimerization in class B1 GPCRs is an emerging area of research that has far-reaching implications for our understanding of GPCR function and signal transduction. While class B1 GPCRs were initially thought to function primarily as monomers, mounting evidence suggests that their ability to form dimers—whether homodimers or heterodimers—plays a critical role in regulating receptor function, ligand binding, and downstream signaling. This insight not only enhances our understanding of class B1 GPCR biology but also opens new avenues for developing therapeutic agents that target specific receptor dimer states to modulate signaling in diseases related to metabolism and homeostasis.     References   1.          Gusach, A., J. García-Nafría, and C.G. Tate, New insights into GPCR coupling and dimerisation from cryo-EM structures.  Current Opinion in Structural Biology, 2023. 80 : p. 102574. 2.          Bouvier, M., Oligomerization of G-protein-coupled transmitter receptors.  Nat Rev Neurosci, 2001. 2 (4): p. 274-86. 3.          Guo, W., et al., Crosstalk in G protein-coupled receptors: Changes at the transmembrane homodimer interface determine activation.  Proceedings of the National Academy of Sciences, 2005. 102 (48): p. 17495-17500. 4.          Perreault, M.L., et al., Heteromeric dopamine receptor signaling complexes: emerging neurobiology and disease relevance. Neuropsychopharmacology, 2014. 39 (1): p. 156-68. 5.          Graaf, C., et al., Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March to Therapeutic Successes.  Pharmacol Rev, 2016. 68 (4): p. 954-1013. 6.          Harikumar, K.G., et al., Impact of secretin receptor homo-dimerization on natural ligand binding.  Nature Communications, 2024. 15 (1): p. 4390. 7.          Harikumar, K.G., et al., Glucagon-like peptide-1 receptor dimerization differentially regulates agonist signaling but does not affect small molecule allostery.  Proc Natl Acad Sci U S A, 2012. 109 (45): p. 18607-12. 8.          Schelshorn, D., et al., Lateral allosterism in the glucagon receptor family: glucagon-like peptide 1 induces G-protein-coupled receptor heteromer formation.  Mol Pharmacol, 2012. 81 (3): p. 309-18. 9.          Wootten, D., et al., Allostery and Biased Agonism at Class B G Protein-Coupled Receptors.  Chem Rev, 2017. 117 (1): p. 111-138.

Hello GPCR Passenger, Welcome aboard the GPCR train as it sets off on its journey. We are excited to have you back at your usual GPCR stop for the week. Let's explore the newest developments in GPCR research and community news together! This Week’s Highlights: Congrats to: Monserrat Avila-Zozaya , our incredible contributor, for her fantastic article on Profiling Immune Cell and Platelet Transcriptomes , and we want to wish her the best of luck on her talk today at the 11th Adhesion GPCR Workshop about ' Breaking Barriers: My Journey from Mexico to the Heart of the Dr. GPCR Ecosystem and beyond .' We all are cheering for you! Gunnar Schulte for his excellent work on International Union of Basic and Clinical Pharmacology CXV: The Class F of G Protein-Coupled Receptors Avoid delaying it further! Registrations end TOMORROW for Principles of Pharmacology II Don't let this opportunity slip away to reserve your spot in our upcoming course ! Seize the chance to enhance your understanding and expertise in pharmacology under the guidance of the renowned expert Dr. Terry Kenakin . Participants will acquire knowledge in: The powerful applications of new cellular assays to determine GPCR ligand behavior in different functional systems. Understanding real-time kinetics to predict activity and in vivo target coverage. New ligands and new GPCR behaviors that produce unique drug profiles (i.e. intracellular ligands and signaling, location bias, signaling bias). Modules: October 31st: The Eyes to See- The Importance of Pharmacologic Assays. November 7th: Drug Disposition in Physiological Tissues as a Therapeutic Variable. November 14th: The Application of GPCR Ligand Kinetics to Candidate Design. November 21st: Unconventional GPCR Ligands as Drugs. December 5th: Unique Exploitable GPCR-Ligand Behaviors for Therapeutic Benefit. *Lessons are every Thursday at 10 AM EST. Reasons to Consider Enrolling Now: Exciting Q&A Session and Group Discussions Don't miss out on the opportunity to get your questions answered by our knowledgeable teacher or initiate a lively discussion in the exclusive group dedicated to the course! Outstanding Educational Opportunities at an Unbeatable Value Our courses provide top-notch education at a competitive price. Tailored Learning Experience Designed for Your Needs Enhance your learning journey with access to our extensive library of recorded sessions. High Praise from Our Happy Students Past students highly endorse our programs, praising our faculty's engaging content and expertise in simplifying complex GPCR pharmacology concepts for practical use in academic and industrial settings. Exclusive Deal for Scientists in Developing Nations If you reside and work in a developing country, complete this form for free access to Dr. Kenakin's upcoming course. We aim to make education accessible to all! Act now to become a part of our prestigious learning community! Classified GPCR News  Let’s dive into the   Classified GPCR News from October 14th to 20th, 2024 Industry News Ghent based Confo Therapeutics is leveraging GPCR expertise as a discovery engine - multiple partners have already signed on to the science Lundbeck signs $2.5B check for Longboard, seeing blockbuster potential in epilepsy med Call for GPCR Papers Deadline: Nov 1, 2024. Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and Webinars November 5 - 7, 2024 | 16th Annual PEGS Europe   November 25 - 27, 2024 | 1st Virtual GPCR Forum Conference November 26 - 28, 2024 | GPCRs-Targeted Drug Discovery Summit Europe July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology GPCR Jobs Scientist I Cell Biology - Tectonic Therapeutic Senior Scientist, GPCR Pharmacology Research Associate - Professor Graeme Milligan Postdoc in Molecular Pharmacology - The Hauser Group Postdoctoral Scholar – iPSC in cardiac and endothelial cell function Protein Biochemist/Structural Biologist Senior Scientist/Staff Scientist, Computational Chemistry Postdoc in GPCR mechanosensing   GPCR Activation and Signaling Opioid receptors reveal a discrete cellular mechanism of endosomal G protein activation Amylin receptor subunit interactions are modulated by agonists and determine signaling Distinct role of GRK3 in platelet activation by desensitization of G protein-coupled receptors GPCRs in Cardiology, Endocrinology, and Taste Latrophilin-2 Deletion in Cardiomyocyte Disrupts Cell Junction, Leading to D-CMP Steviol rebaudiosides bind to four different sites of the human sweet taste receptor (T1R2/T1R3) complex explaining confusing experiments GPCRs in Neuroscience An emerging multi-omic understanding of the genetics of opioid addiction A FMRFamide-like neuropeptide FLP-12 signaling regulates head locomotive behaviors in C. elegans GPCRs in Oncology and Immunology In Silico Design of Novel RGS2-Galpha-q Interaction Inhibitors with Anticancer Activity Evolutionary diversity of CXCL16-CXCR6: Convergent substitutions and recurrent gene loss in sauropsids Noval insights and therapeutic strategies for tumor-induced kidney pathologies Methods & Updates in GPCR Research Development of a NanoBRET Assay Platform to Detect Intracellular Ligands for the Chemokine Receptors CCR6 and CXCR1 Reviews, GPCRs, and more International Union of Basic and Clinical Pharmacology CXV: The Class F of G Protein-Coupled Receptors Structural and Molecular Insights into GPCR Function Structure of endothelin ETB receptor-Gi complex in a conformation stabilized by unique NPxxL motif Ligand-induced conformational changes in the β1-adrenergic receptor revealed by hydrogen-deuterium exchange mass spectrometry Become a Premium Member! 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Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Posters Interrogating The Role Of CELSR1 (ADGRC1) In Breast Cancer Caroline Formstone Generation and characterization of collecting duct specific GPR56 knockout mice Jianxiang Xue Anti-Tumorigenic Role of Brain Angiogenesis Inhibitor 3 (BAI3) in WNT-Activated Medulloblastomas Virginea de Araujo Farias Conformational And Functional Coupling Between Extracellular and Transmembrane Regions of a Holo-Adhesion GPCR Szymon P. Kordon Deorphanization Of The Adhesion GPCRs GPR110 and GPR116 Tingzhen Shen Self-Cleavage of GPR110 SEA Domain and Its Impact on GAIN Domain Autoproteolysis Bill Huang Tethered Agonist Dependent ADGRL3 Signaling Activity In The G12/13 Pathway Júlia Rosell Endocytic Cues Determine the Signaling Profile of Adhesion GPCR ADGRL1 / Latrophilin-1 Sheila Ribalta-Mena GPR110 modulates anxiety-like behaviors and memory function in mice potentially through neuronal and neuroimmune alterations during neurodevelopment Mariam Melkumyan Interrogating The Role Of CELSR1 (ADGRC1) In Breast Cancer Caroline Formstone Abstract "Breast cancer is the most common form of cancer amongst women. Ductal carcinomas are increasingly diagnosed but identifying which will progress to invasive disease remains difficult highlighting an urgent need for new biomarkers that distinguish ductal carcinomas on this basis. Planar cell polarity (PCP) proteins contribute to tumour growth and invasion. Recent studies identify CELSR1, a key PCP gene, as a novel biomarker for early-stage breast cancer. CELSR1 is reactivated in luminal-type ductal carcinomas. The impact of CELSR1 on cancer progression, however, is unclear. Our working hypothesis is that distinct CELSR1 protein isoforms differentially regulate tissue adhesiveness by influencing the stability/plasticity of cell-cell and cell-matrix contacts. Notably, our pilot data from luminal-type breast cancer cell lines representative of breast carcinomas with lower versus higher invasive potential reveal differential enrichment of CELSR1 protein isoforms. To test the specific hypothesis that biased expression of CELSR1 isoforms will predict invasive potential of a luminal breast carcinoma we will (a) determine, via loss-of-function assays in vitro and in vivo, whether CELSR1 protein isoforms differentially influence the stability of cell-cell and/or cell-matrix adhesions to dictate breast tumour invasive mechanism (b) quantify CELSR1 isoform expression (mRNA and protein) within patient luminal carcinoma samples exhibiting non-invasive or invasive features, the latter including heterogeneous tumours with mixed pathology. Through study of known protein isoforms of CELSR1, which would be missed in gene expression microarray analyses, we hope to illuminate the prognostic potential of CELSR1 for early-stage breast cancer." Authors & Affiliations "Klena, Ladislav University of Hertfordshire" About Caroline Formstone "Cell and developmental biologist with a focus on how planar cell polarity drives complex tissue morphogenesis. I study the cell and tissue level consequences of its failure in foetal development and of its reemployment in cancer" Caroline Formstone on the web University of Hertfordshire Generation and characterization of collecting duct specific GPR56 knockout mice Jianxiang Xue Abstract "GPR56 is a multifunctional adhesin G protein-coupled receptor involved in diverse biological processes. The role of GPR56 in the kidneys has been understudied. A recent study demonstrated that GPR56 in the glomerular endothelial cells promoted diabetic kidney disease progression via regulation of eNOS. Using RNAscope in situ hybridization (ISH) for GPR56, aquaporin 2 and NKCC2 (thick ascending limb, TAL marker), we detected GPR56 mRNA highly expressed in the collecting duct and TAL of the loop of Henle with limited expression in the proximal tubule. To determine the physiological role of GPR56 in the collecting duct, we generated a collecting duct-specific GPR56 knockout (GPR56CD-KO) mouse model by crossing GPR56flox (Control) with cadherin 16 Cre mice. The deletion of GPR56 in the collecting duct was confirmed by RNAscope ISH. GPR56CD-KO mice were born at predicted Mendelian frequencies, appeared grossly indistinguishable from Con mice, and developed normally. For baseline phenotypic characterization, blood gas analysis showed no differences in blood pH, blood HCO3-, blood Na+, or blood K+ between GPR56CD-KO and control mice. Metabolic cage experiments demonstrated no differences in fluid intake, urine volume, urinary pH or urine osmolality between genotypes in baseline. 24hr water deprivation experiment showed that GPR56CD-KO mice can concentrate urine as effectively as control mice. In conclusion, we successfully generated collecting duct-specific GPR56 knockout mouse and found no defective urine concentrating ability in GPR56CD-KO mice. This mouse model will be useful to delineate the collecting duct-specific role of GPR56 for renal function, including acid-base regulation." Authors & Affiliations "Hailey Steichen, Krystin Eaton, Teagan Yan, and Nathan Zaidman; Department of Biochemistry and Molecular Biology, University of New Mexico" About Jianxiang Xue "I am a postdoctoral researcher working in the Department of Biochemistry and Molecular Biology, University of New Mexico. I earned my PhD degree in Biomedical Sciences from the University of South Florida. During my graduate studies, using various transgenic mouse models and expertise in intestinal and renal physiology, I systematically characterized the function of sodium/hydrogen exchanger 3 in the intestine and kidneys for fluid and electrolyte homeostasis and acid-base balance. My predoctoral work was supported by an American Heart Association fellowship. Since staring my postdoctoral training, I have continued to develop my expertise to answer fundamental questions on adhesion GPCR in renal physiology and pathology. In my free time, I enjoy reading, workouts, and hiking." Jianxiang Xue on the web Zaidman Physiology Lab Anti-Tumorigenic Role of Brain Angiogenesis Inhibitor 3 (BAI3) in WNT-Activated Medulloblastomas Virginea de Araujo Farias Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Van Meir, Erwin G. University of Alabama at Birmingham" About Virginea de Araujo Farias "Brain Angiogenesis Inhibitor (BAI) proteins are members of group VII of the adhesion G protein-coupled receptor (aGPCR) family. BAI1-3 are highly expressed in the brain, where they participate in synaptogenesis and synapse maintenance. In cancers, BAI1-3 expression can be lost through epigenetic silencing, copy number loss or truncating mutations. In medulloblastomas (MB), BAI3 (ADGRB3) expression is specifically reduced in the WNT-activated group (WNT-MB), but not in the other three molecular groups. WNT pathway activation in WNT-MB is driven by mutations of the CTNNB1 gene, activating ß-catenin-dependent signaling; however, no interactions between BAI3 and the WNT signaling pathway have been described so far. MAGI3, a PDZ-containing scaffolding protein is known to downregulate WNT signaling by interacting with ß-catenin in gliomas, but it is unknown whether this involves BAI3. To explore a possible connection between BAI3 and ß-catenin signaling through MAGI3 in WNT-MB, we probed for potential protein-protein interactions using co-IP experiments. We found an interaction between BAI3 and MAGI3 in mouse brain lysates. Therefore, we hypothesize that re-expression of BAI3 in WNT-MB cells will restrain ß-catenin activity through the formation of a BAI3/MAGI3/ß-catenin complex, reducing their tumorigenic properties. To test this hypothesis, we created WNT-like MB cell lines stably expressing tet-on wild-type BAI3 or a BAI3 lacking the C-terminal PDZ-binding motif (PBM). We will present the effects of BAI3 re-expression on WNT-MB cells oncogenic properties and signaling." Virginea de Araujo Farias on the web Google Scholar Conformational And Functional Coupling Between Extracellular and Transmembrane Regions of a Holo-Adhesion GPCR Szymon P. Kordon Abstract "Adhesion G Protein-Coupled Receptors (aGPCRs) are key cell-adhesion molecules involved in numerous physiological functions. aGPCRs have large multi-domain extracellular regions (ECR) that mediate cell adhesion and play roles in transmitting extracellular signals to the inside of the cell. Ligand binding and mechanical force applied on the ECR regulate receptor function. However, how the ECR communicates with the seven-pass transmembrane domain (7TM) remains elusive, because the relative orientation and dynamics of the ECR and 7TM within a holoreceptor is unclear. Here, we describe the cryo-EM reconstruction of an aGPCR, Latrophilin3/ADGRL3, and reveal that the conserved GAIN domain, that directly precedes 7TM, adopts a parallel orientation to the membrane and has constrained movement. Single-molecule FRET experiments unveil three slow-exchanging FRET states of the ECR relative to the 7TM within the holoreceptor. GAIN-targeted antibodies, and cancer-associated mutations at the GAIN-7TM interface, alter holoreceptor conformations, and modulate downstream receptor signaling. Altogether, this data demonstrates conformational and functional coupling between the ECR and 7TM, suggesting an ECR-mediated mechanism for aGPCR activation." Authors & Affiliations "Cechova Kristina (3), Bandekar Sumit J.(1, 2), Leon Katherine (1, 2), Dutka Przemysław (1, 4), Siffer Gracie (3), Kossiakoff Anthony A. (1), Vafabakhsh Reza (3), Araç Demet (1, 2) 1. Department of Biochemistry and Molecular Biology, The University of Chicago, Chicago, IL, USA; 2. Neuroscience Institute, Institute for Biophysical Dynamics, and Center for Mechanical Excitability, The University of Chicago, Chicago, IL, USA; 3. Department of Molecular Biosciences, Northwestern University, Evanston, IL, USA; 4. Current affiliation: Department of Structural Biology, Genentech, South San Francisco, CA, USA" About Szymon P. Kordon "I am a postdoctoral scholar in the Araç Lab at The University of Chicago, studying the structure and function of aGPCRs. Utilizing synthetic antibody fragments, I aim to understand better the structural basis of the aGPCRs activation and signaling and to characterize ECR-mediated signal transduction at the molecular level." Szymon P. Kordon on the web Araç Laboratory at UChicago Deorphanization Of The Adhesion GPCRs GPR110 and GPR116 Tingzhen Shen Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Frank E. Kwarcinski, Gregory G. Tall (University of Michigan, Ann Arbor)" About Tingzhen Shen "A graduate student from Tall Lab, department of Pharmacology, University of Michigan, Ann Arbor." Tingzhen Shen on the web University of Michigan Self-Cleavage of GPR110 SEA Domain and Its Impact on GAIN Domain Autoproteolysis Bill Huang Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Hee-Yong Kim, Laboratory of Molecular Signaling, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Rockville, MD, USA" About Bill Huang "Researcher" Bill Huang on the web LinkedIn Tethered Agonist Dependent ADGRL3 Signaling Activity In The G12/13 Pathway Júlia Rosell Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Regmi, Rajesh (1), Perry-Hauser, Nicole A. (2), Javitch, Jonathan A. (2), Mathiasen, Signe (1) (1) Department of Biomedical Sciences, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark. (2) Department of Psychiatry and Molecular Pharmacology and Therapeutics, Columbia University Vagelos College of Physicians and Surgeons, New York, USA; Division of Molecular Therapeutics, New York State Psychiatric Institute, New York, USA" About Júlia Rosell "I am a first-year PhD student with two years of experience in the adhesion GPCR field. I completed my Master’s thesis on ADGRL3, where I conducted research involving mammalian cell cultures and techniques such as BRET assays and gene expression assays. Currently, my research focuses on the intracellular signaling of ADGRL3 from a single-molecule perspective and investigating how the binding of extracellular transsynaptic ligands modulates ADGRL3 activity, aiming to elucidate their interplay." Júlia Rosell on the web LinkedIn Endocytic Cues Determine the Signaling Profile of Adhesion GPCR ADGRL1 / Latrophilin-1 Sheila Ribalta-Mena Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations " Hernández-Aranda Judith 2, Correoso-Braña Kerlys 1, Vialou Vincent 3, Leduc Richard 4, Olivares-Reyes Jesús Alberto 2, Boucard Antony A1. 1 Department of Cell Biology, Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional (Cinvestav-IPN), México City, México. 2 Department of Biochemistry, Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional (Cinvestav-IPN), México City, México. 3 Sorbonne Université, Inserm, CNRS, Neurosciences Paris Seine, Paris, France. 4 Department of Physiology and Pharmacology, Université de Sherbrooke, Sherbrooke, Canada " About Sheila Ribalta-Mena " Cell Biology PhD student " Sheila Ribalta-Mena on the web CINVESTAV ResearchGate LinkedIn GPR110 modulates anxiety-like behaviors and memory function in mice potentially through neuronal and neuroimmune alterations during neurodevelopment Mariam Melkumyan Abstract "GPR110, an adhesion G protein coupled receptor (GPCR), is widely expressed in developing brains but diminishes in adult stage except in the hippocampus, a region involved in learning and memory. Ligand-induced GPR110 signaling stimulates neurogenesis and synaptogenesis during development, and the absence of the ligand-induced signaling causes object recognition and spatial memory deficits in adulthood and increased neuroinflammatory responses. Nevertheless, the role of GPR110 signaling in behavioral consequences has not been fully explored. This study aimed to understand the effects of GPR110 on mouse behaviors in relation to neurodevelopmental and neuroimmune gene and protein expression. Anxiety and memory function were tested using both male and female mice at 5-6 month of age. GPR110 knockout (KO) mice displayed trends for increased anxiety-like behaviors in the elevated plus maze test and in the open field test. Memory tests, including the novel object test and the radial 8-arm maze showed worsened spatial and reference memory in the GPR110 KO mice compared to wildtype mice. The y-maze showed a significant sex by genotype interactions with GPR110 KO male mice having increased number of correct alterations and errors, while the GPR110 KO females had fewer correct alterations and errors. RNAseq data indicated significantly impaired developmental gene expression for neuronal differentiation, axonogenesis, and synaptogenesis, as well as altered neuroinflammatory marker expression in GPR110 KO mouse brains. Further studies exploring the protein expression and neural activity of these mouse brain will give insight on the mechanism underlying the behavioral consequences associated with the GPR110 receptor. " Authors & Affiliations "Joel Toro, Bill Huang, Hee-Yong Kim Laboratory of Molecular Signaling, National Institute of Alcohol Abuse and Alcoholism, NIH" About Mariam Melkumyan "Mariam Melkumyan is a postdoctoral fellow at the Laboratory of Molecular Signaling studying the role of GPR110 in neurotransmission and neuroimmune activity involved in learning and memory, anxiety, and alcohol use. Mariam, originally from Armenia, completed her bachelor's degree in Neuroscience at American University in Washington, DC and her dual-title PhD in Neuroscience and Clinical and Translational Sciences at Penn State College of Medicine in Hershey, PA. Mariam started her postdoctoral training in February 2024 and is hoping to become an academic professor and mentor the next generation of scientists." Mariam Melkumyan on the web LinkedIn Google Scholar < Previous Session Next Session >

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 Abhishek Kumar Singh Adgrg6/Gpr126 is Required for Myocardial Notch Activity and N-cadherin Localization to Attain Trabecular Identity Andrew Dates Heterogeneity of Tethered Agonist Signaling in Adhesion G Protein-Coupled Receptors Cheng-Chih Hsiao ADGRG1/GPR56 regulates survival of terminally differentiated CD8+ T cells Erwin G. Van Meir Adhesion GPCR BAI1/ADGRB1 can block IGF1R-mediated growth signalling, increase radiosensitivity and augment survival in medulloblastoma. Gavin Zhang NovoiSMART - A new platform for GPCR antibody drug discovery Jinpeng Sun Identification and Functional Characterization of Adhesion GPCRs As Steroid Hormone Receptors and Hearing and Balance Receptors Mariam Melkumyan GPR110 modulates anxiety-like behaviors and memory function in mice potentially through neuronal and neuroimmune alterations during neurodevelopment Rashed Rezwan Parag Novel isoforms of adhesion G protein coupled receptor B1 (ADGRB1/BAI1) generated from an alternative promoter in intron 17 Sumit Bandekar Structural studies of the CELSR1 extracellular region reveal a compact multidomain module of fourteen domains which regulates signaling Vasiliki Karagiannakou A single cell GPCR map of thermogenic fat Alain Garcia De Las Bayonas The Adhesion GPCR Cupidon Regulates Mating In The Closest Relatives Of Animals Anne Bormann Intricacies Of Complex Assembly And Ligand Interaction In The Adhesion GPCR Latrophilin/Cirl 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 Fabian Pohl Structural Determinants Of GAIN Domain Autoproteolysis And Cleavage Resistance Of Adhesion G Protein-Coupled Receptors Hailey Steichen Identification of Differentially Expressed Gpr116 (Adgrf5) Transcript Variants in Mouse Kidney Joseph Duman BAI1/ADGRB1-mediated Regulation of Mitochondrial Morphology in Axons Monserrat Avila Zozaya The ADGRF5/GPR116 receptor is a key regulator of lymphatic endothelial cell identity and function Sheila Ribalta-Mena Endocytic Cues Determine the Signaling Profile of Adhesion GPCR ADGRL1 / Latrophilin-1 Szymon P. Kordon Conformational And Functional Coupling Between Extracellular and Transmembrane Regions of a Holo-Adhesion GPCR Virginea de Araujo Farias Anti-Tumorigenic Role of Brain Angiogenesis Inhibitor 3 (BAI3) in WNT-Activated Medulloblastomas Alex Torrelli-Diljohn Investigating The Role of ADGRB3 Loss of Expression in Brain Tumor Formation in Li-Fraumeni Syndrome Beatriz Blanco Redondo Uncovering the signaling pathway of the ADGRA homolog Remoulade in Drosophila Dimitris Placantonakis Antibody-drug conjugates targeting CD97 in glioblastoma Florian Seufert Unveiling the GPS Cleavage Mechanism in ADGRL1 with QM/MM Hee-Yong Kim Characterization of Phenotypes Associated with GPR110 Deletion Júlia Rosell Tethered Agonist Dependent ADGRL3 Signaling Activity In The G12/13 Pathway Nicole Perry-Hauser Adhesion G protein-coupled receptor latrophilin-3 (ADGRL3) modulation of dopaminergic neurotransmission Signe Mathiasen Signaling Properties of ADGRL3 Tingzhen Shen Deorphanization Of The Adhesion GPCRs GPR110 and GPR116 Willem Berend Post The Adhesion GPCR Latrophilin Interacts With The Notch Pathway To Control Germ Cell Proliferation Ana Lilia Moreno Salinas Characterizing hADGRE5/CD97 Activation and Signaling: A Mechanical Stimulation BRET-Based Approach (MS-BRET) Bill Huang Self-Cleavage of GPR110 SEA Domain and Its Impact on GAIN Domain Autoproteolysis Douglas Tilley ADGRF5-mediated regulation of cardiac health and disease 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 Jesse Stillwell Next Generation MBD2 inhibitors for Brain Cancer Therapy Lara-Sophie Brodmerkel GAIN Domain Dynamics And Its Relevance For Adhesion GPCR Signaling In Vivo Pal Kasturi Site Specific N-Glycosylation Of The N-Terminal Fragment Of ADGRG6 Drives Proteolytic Processing, Trafficking And Signalling Simeon R. Mihaylov Bai1 Is A Novel Neuronal Substrate Of The Psychiatric Risk Kinase TNIK Tobias Langenhan The CELSR/ADGRC Homolog Flamingo Is Not Autoproteolytically Processed By The GAIN Domain Yimin Zou ADGRCs in glutamatergic synapse formation, maintenance and degeneration Anastasia Georgiadi Adhesion GPCR GPR116/Adgrf5 controls a lineage of anti-thermogenic adipocytes with implications for adaptive thermogenesis during prolonged cold exposure Caroline Formstone Interrogating The Role Of CELSR1 (ADGRC1) In Breast Cancer Emmanouil Kyrloglou GPR124 Mediates Adhesion Of Leukemic Stem Cells To Their Niche And Leads To Myeloid Skewing Gabriela Aust Critical role for CD97/ADGRE5 in the induction of allergic airway inflammation Jianxiang Xue Generation and characterization of collecting duct specific GPR56 knockout mice Laurent Sabbagh bioSens-All: A Multiparametric BRET-Based Platform for Comprehensive Profiling of adhesion GPCR Signaling and Pharmacology-Enabling Drug Discovery Peng Xiao Tethered Peptide Activation Mechanism of Adhesion GPCRs Stephanie Häfner The NTF Release Sensor Approach for Drug Discovery for Human Adhesion GPCRs Tyler Bernadyn Elucidating The Role Of GPR97/ADGRG3 In Neutrophil Biology Yuling Feng Localization of putative ligands for adhesion G protein-coupled receptors in mouse tissues.

< GPCR News < GPCRs in Oncology and Immunology Characterization, expressional and evolutionary analysis of five fish-specific CCRs (CCR4La, CCR4Lc, CCR12a1, CCR12a2, and CCR12b) in largemouth bass (Micropterus salmoides) Published date October 24, 2024 Abstract "CC chemokine receptors (CCRs), the numbers of the G protein-coupled receptor (GPCR) superfamily, had crucial roles in treating infection, inflammation, and tissue damage by binding to their ligands. In this study, five fish-specific CCRs, namely CCR4La, CCR4Lc, CCR12a1, CCR12a2, and CCR12b, were identified in largemouth bass (Micropterus salmoides). The correction of nomenclatures of these CCRs were confirmed by phylogenetic analysis, structural analysis and genomic synteny analysis. Following 1×106 CFU/mL and 1×107 CFU/mL Edwardsiella piscicida infection, these five CCRs were significantly induced in spleen of largemouth bass, indicating their important roles in the immune response against bacterial infection. Selection pressure analysis revealed that CCR4La, CCR4Lc, CCR12a1, and CCR12a2 underwent negative selection pressure, whereas CCR12b experienced positive selection pressure. Robust selection site detection methods identified that positive selected sites of CCR4La, CCR4Lc, CCR12a1, and CCR12a2 mainly distributed in their extracellular regions, which involved in ligand binding and pathogen interaction. Similarly, the positive selected sites of CCR12b were also located in its extracellular regions. The accuracy of the pressure selected sites were also validated by molecular docking analysis. The potential ligands for these five CCRs were identified by molecular docking analysis, with finding that CCL3 and CCL5 might be the ligands of largemouth bass CCR4La/Lc, and CCL5, CCL8, CCL7, CCL13 and CCL26 might be that of largemouth bass CCR12a1/a2/b. Our results provided basis for elucidating the functions of chemokine-receptor complex in largemouth bass." Authors Tags 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 >