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Results found for "GPCR Pharmacology"

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

    Human cells express over 800 G-protein-coupled receptors (GPCRs) to facilitate communication with the Capturing the dynamics of GPCR activation has always been a challenge because G protein activation in With this high-resolution, dynamic view of GPCR activation, scientists can better tackle diseases by Beyond GPCRs, the methods and insights from this study can be applied to other fast, transient biological Time-resolved cryo-EM of G-protein activation by a GPCR. Nature (2024).

  • 📰 GPCR Weekly News, January 29 to February 4, 2024

    GPCR Symposia Our upcoming symposium on March 15th is about GPCR activation and signaling. GPCR University This week marks the beginning of our first Dr.GPCR University course, 'Applying Pharmacology Webinars February 11 - 14, 2024 | 2024 BPS Annual Meeting February 20, 2024 | Career Opportunities in Pharmacology World Congress of Basic and Clinical Pharmacology 2026 GPCR Jobs NEW Postdoctoral Fellowship- Mechanistic GPCR Ecosystem

  • 📰 GPCR Weekly News, September 4 to 10, 2023

    GPCR Symposium on ''GPCRs as Therapeutic Modalities' Share your project with a 1-minute abstract video GPCR Newsletter for more insights! Program Acquired by Vertex Call for GPCR Papers opnMe GPCR Route 66+ project. Jobs NEW Senior Research Associate, In Vitro Pharmacology - Crinetics Pharmaceuticals NEW Postdoc In GPCR Ecosystem

  • PI(4,5)P 2-stimulated positive feedback drives the recruitment of Dishevelled to Frizzled in Wnt-β-c

    that the affinity of Fzd for Dvl was not affected by Wnt ligands, in contrast to other members of the GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

  • Why “Displacement” Misleads You: Allosteric Binding Demystified

    If your project involves GPCRs , functional selectivity , or non-traditional ligands , this session is Function: Two Different Worlds One of the most common—and dangerous—mistakes in allosteric pharmacology When a PAM increases radioligand binding but suppresses functional response, it’s not broken pharmacology—it The takeaway:  what looks like pharmacology failure may be a systems problem . Terry Kenakin An always-growing library of on-demand pharmacology insights The ability to vote on or

  • Septerna emerges with $100M to spark 'second golden age' of prolific drug target GPCR with ...

    February 2022 Septerna emerges with $100M to spark 'second golden age' of prolific drug target GPCR with Better known as GPCR, the fruitful research space has led to more than 700 approved drugs over previous The company's co-founder, GPCR pioneer and Nobel laureate Robert Lefkowitz, M.D., has 50 years of experience Read more at the source #DrGPCR #GPCR #IndustryNews

  • 📰 GPCR Weekly News, August 14 to 20, 2023

    Congrats to the GPCR Therapeutics team for their recent paper in the American College of Clinical Pharmacology GPCR Symposium on 'GPCRs as Therapeutic Modalities'. ' latest science paper was published by the American College of Clinical Pharmacology Sosei and Cancer Postdoc Research Associate Director, Regulatory Affairs Research Scientist/Senior Scientist I - Molecular Pharmacology GPCR Ecosystem

  • Nanobodies as Probes and Modulators of Cardiovascular G Protein-Coupled Receptors

    October 2022 "Understanding the activation of G protein-coupled receptors (GPCRs) is of paramount importance Although many cardiovascular GPCRs have been extensively studied as model receptors for decades, new Here, we review how nanobodies have been adopted to elucidate the structure, pharmacology, and signaling of cardiovascular GPCRs, resolving long-standing mysteries and revealing unexpected mechanisms. Read more at the source #DrGPCR #GPCR #IndustryNews

  • Adrenal G Protein-Coupled Receptors and the Failing Heart: A Long-distance, Yet Intimate Affair

    Despite considerable advances in pharmacological treatment, HF represents a severe clinical and social In this review, we discuss important aspects of adrenal GPCR signaling and regulation, as they pertain modulation of cardiac function in the context of chronic HF, by focusing on the 2 best studied adrenal GPCR the β-arrestins in the adrenals, 2 protein families that regulate the signaling and functioning of GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews

  • Pepducin-mediated G Protein-Coupled Receptor Signaling in the Cardiovascular System

    are small-lipidated peptides designed from the intracellular loops of G protein-coupled receptors (GPCRs ) that act in an allosteric manner to modulate the activity of GPCRs. Over the past 2 decades, pepducins have progressed initially from pharmacologic tools used to manipulate GPCR activity in an orthosteric site-independent manner to compounds with therapeutic potential that Read more at the source #DrGPCR #GPCR #IndustryNews

  • 📰 GPCR Weekly News, August 7 to 13, 2023

    Hello GPCR enthusiasts! Check out the latest advancements in GPCR studies. Save the date! GPCR Symposium on 'GPCRs as Therapeutic Modalities'. Want to share your project in a casual way? GPCR Newsletter! Postdoc Research Associate Director, Regulatory Affairs Research Scientist/Senior Scientist I - Molecular Pharmacology GPCR Ecosystem

  • 📰 GPCR Weekly News, July 10 to 16, 2023

    Welcome, GPCR enthusiasts! This week's GPCR papers feature a publication by Dr. Robert J Lefkowitz. GPCR Symposium on Structural and Molecular Insights on GPCR Activation! GPCR Newsletter for updates! Postdoctoral Fellow, Caron Lab Clinical Trial Associate Research Scientist/Senior Scientist I - Molecular Pharmacology GPCR Ecosystem

  • 📰 GPCR Weekly News, July 3 to 9, 2023

    Hello GPCR enthusiasts! We're here to share the latest GPCR news with you. Congratulations to Dr. GPCR Newsletter for updates! /Senior Scientist I - Molecular Pharmacology Vice President, Medical Affairs Associate Director / Director , Clinical Operations Professor in Cardiovascular Pharmacology Explore Dr. GPCR Ecosystem

  • Sosei Heptares and Kallyope Enter Collaboration to Identify and Validate Novel Gastrointestinal GPCR

    2022 Sosei Heptares and Kallyope Enter Collaboration to Identify and Validate Novel Gastrointestinal GPCR the Sosei Heptares compound library for its industry-leading biology platform to identify potential GPCR entered a strategic research collaboration to identify and validate novel G protein-coupled receptor (GPCR drug discovery programs in the area of gastrointestinal diseases. " Read more at the source #DrGPCR #GPCR

  • Glucagon receptor-mediated regulation of gluconeogenic gene transcription is endocytosis-dependent..

    transcription is endocytosis-dependent in primary hepatocytes "A number of G protein-coupled receptors (GPCRs activation by glucagon within 5 min and transit via EEA1-marked endosomes shown previously to be sites of GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

  • Molecular basis for ligand modulation of the cannabinoid CB 1 receptor

    August 2022 "The cannabinoid CB1 receptor is the most abundant G protein coupled receptor (GPCR) in LINKED ARTICLES: This article is part of a themed issue on Structure Guided Pharmacology of Membrane Proteins (BJP 75th Anniversary). " Read more at the source #DrGPCR #GPCR #IndustryNews

  • 📰 GPCR Weekly News, June 19 to 25, 2023

    Welcome, GPCR buffs! Join us for our weekly round-up of GPCR News. Congratulations to our Dr. GPCR Symposium on Structural and Molecular Insights on GPCR Activation. Signalling (June 30 - July 1, 2023) 19th World Congress of Basic & Clinical Pharmacology 2023. - 29, 2024) GPCR Jobs Professor in Cardiovascular Pharmacology Scientist I / Scientist II DOE (Native GPCR Ecosystem

  • 📰 GPCR Weekly News, June 12 to 18, 2023

    Greetings GPCR enthusiasts! Join us to explore the fascinating world of GPCRs. GPCR Symposium on Structural and Molecular Insights on GPCR Activation. Signalling (June 30 - July 1, 2023) 19th World Congress of Basic & Clinical Pharmacology 2023. (March 24 - 29, 2024) GPCR Jobs NEW Professor in Cardiovascular Pharmacology Scientist I / Scientist GPCR Ecosystem

  • 📰 GPCR Weekly News, November 6 to November 12, 2023

    This week, we've curated 12 GPCR papers. GPCR Symposium for the year, which will focus on GPCRs in Immunology and Oncology. in Medicinal Chemistry NEW July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology Antibody Discovery Staff Scientist (AC-TAP) in Database Development at Department of Drug Design and Pharmacology GPCR Ecosystem

  • 📰 GPCR Weekly News, June 5 to 11, 2023

    Hi there GPCR enthusiasts! Join us this week for a deep dive into the world of GPCRs. GPCR Symposium on Structural and Molecular Insights on GPCR Activation. Berchiche is at the Molecular Pharmacology GRC, if you are also on-site, please stop by and say hi. 1, 2023) 19th World Congress of Basic & Clinical Pharmacology 2023. GPCR Ecosystem

  • 📰 GPCR Weekly News, October 30 to November 4, 2023

    Good day, GPCR folks! Take advantage of our GPCR highlights of the week. Dr. GPCR Symposium for the year on GPCRs in Immunology and Oncology! Antibody Discovery Staff Scientist (AC-TAP) in Database Development at Department of Drug Design and Pharmacology Medical Sciences Octant Apprentice Head of Human Resource Business Partners Senior Scientist, In vitro pharmacology - Crinetics Pharmaceuticals Senior Director, In vitro pharmacology - Crinetics Pharmaceuticals Explore

  • A NanoBRET-Based H 3 R Conformational Biosensor to Study Real-Time H 3 Receptor Pharmacology in...

    August 2022 A NanoBRET-Based H 3 R Conformational Biosensor to Study Real-Time H 3 Receptor Pharmacology monitor the activation state of G protein-coupled receptors are a useful addition to the molecular pharmacology Read more at the source #DrGPCR #GPCR #IndustryNews

  • Extracellular signal-regulated kinases – a potential pathway for GPCR-targeted drug discovery

    Notably, G-protein-coupled receptors (GPCRs), representing the biggest drug target, have been revealed Historically, drug discovery efforts targeting GPCRs focused on G-protein-dependent signaling pathways In summary, targeting GPCR-activated ERK pathways represents a promising strategy for developing new Minireview: targeting GPCR activated ERK pathways for drug discovery. Pharmacological Reviews, 71(2), 267-315. Lu, N., & Malemud, C. J. (2019).

  • β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling to the...

    β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling to the same GPCR cells "β-arrestins mediate regulatory processes for over 800 different G protein-coupled receptors (GPCRs ) by adopting specific conformations that result from the geometry of the GPCR-β-arrestin complex. However, whether β-arrestin1 and 2 respond differently for binding to the same GPCR is still unknown. Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter

  • 📰 GPCR Weekly News, May 22 to 28, 2023

    Hi GPCR lovers👋, Ready for exciting news in the GPCR world? Read them below! GPCRs in Cardiology, Endocrinology, and Taste Pathophysiology and pharmacology of G protein-coupled receptors (June 4 - 8, 2023). 2023 Molecular Pharmacology (GRS) Seminar GRC. (June 10 - 11, 2023). 1, 2023) 19th World Congress of Basic & Clinical Pharmacology 2023. GPCR Ecosystem

  • Conservation of Allosteric Ligand Binding Sites in G-Protein Coupled Receptors

    November 2022 "Despite the growing number of G protein-coupled receptor (GPCR) structures, only 39 structures The method has found druggable sites overlapping with the cocrystallized allosteric ligands in 21 GPCR We then mapped the 394 GPCR X-ray structures available at the time of the analysis (September 2020). Results show that for each of the 21 structures with bound ligands there exist many other GPCRs that Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE

  • 📰 GPCR Weekly News, May 15 to 21, 2023

    Hi GPCR buffs 👋! This week's GPCR papers feature a publication from Dr. Marta Filizola. GPCR Symposium on GPCR Activation and Signaling was a great success. (June 4 - 8, 2023). 2023 Molecular Pharmacology (GRS) Seminar GRC. (June 10 - 11, 2023). 1, 2023) 19th World Congress of Basic & Clinical Pharmacology 2023. GPCR Ecosystem

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