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Results found for "GPCR Drug Design"

  • AlphaFold2 versus experimental structures: evaluation on G protein-coupled receptors

    August 2022 "As important drug targets, G protein-coupled receptors (GPCRs) play pivotal roles in a wide Extensive efforts of structural biology have been made on the study of GPCRs. differences impeded the use of predicted structure models in the functional study and structure-based drug design of GPCRs, which required reliable high-resolution structural information." Read more at the source #DrGPCR #GPCR #IndustryNews

  • High-Content Screening for GPCR Programs: Overcoming Assay Limitations with Fluorescent Ligands

    High-content screening (HCS) has become a cornerstone in GPCR and phenotypic drug discovery, enabling Overcoming them requires careful assay design and strategic use of the right fluorescent probes. In this blog, you’ll learn:  How HCS works and why it is increasingly central to GPCR-based drug discovery Assay Design and Pilot Optimization Successful HCS begins with a clearly defined biological question Conclusion High-content screening continues to reshape GPCR drug discovery, offering richer biological

  • Diversity and specificity in location-based signaling outputs of neuronal GPCRs

    August 2022 "The common mechanisms by which members of the G protein-coupled receptor (GPCR) family respond However, it is becoming increasingly clear that GPCRs show great diversity in their intracellular location Here we will discuss recent studies on the diversity of location, effectors, and signaling of GPCRs, and how these could interact to generate specific spatiotemporal patterns of GPCR signaling in cells. Read more at the source #DrGPCR #GPCR #IndustryNews

  • Multifunctional role of GPCR signaling in epithelial tube formation

    Rho1 signaling is activated by G-protein-coupled receptor (GPCR) signaling at the cell surface. During Drosophila embryonic salivary gland (SG) invagination, the GPCR ligand Folded gastrulation (Fog Here, we reveal that the Smog GPCR transduces Fog signal to regulate Rho kinase accumulation and myosin Read more at the source #DrGPCR #GPCR #IndustryNews

  • Dr. Mark Connor - Dr. GPCR Podcast

    GPCR podcast is now available! Our guest is Dr. Mark Connor! Learn more about #GPCRs and life as an academic wearing different hats. Listen nowhere you get your podcasts. https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ #gpcr #drgpcr

  • Immerse yourself in the Dr. GPCR Ecosystem!

    GPCR Ecosystem with a paid membership for extra benefits. Catch up with the latest #GPCR news, our monthly Virtual Cafe, and much more! Join the #GPCR movement today! ➡️ https://bit.ly/3SUkB8D

  • Dr. Marta Filizola - Dr. GPCR Podcast

    GPCR Podcast, we have none other than Dr. Marta Filizola! https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ #gpcr #drgpcr #podcast

  • Multifunctional role of GPCR signaling in epithelial tube formation

    Rho1 signaling is activated by G-protein-coupled receptor (GPCR) signaling at the cell surface. During Drosophila embryonic salivary gland (SG) invagination, the GPCR ligand Folded gastrulation (Fog Here, we reveal that the Smog GPCR transduces Fog signal to regulate Rho kinase accumulation and myosin Read more at the source #DrGPCR #GPCR #IndustryNews

  • Time is your enemy, GPCRs are your friend

    Stuart Maudsley on how an aging physiological context affects #GPCR signaling #drgpcr. Register here (FREE) https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #virtualcafe

  • Subscribe to Dr. GPCR Newsletter Today!

    Did you know that each month we collect the most recent #GPCR publications and the newest Biotech/Pharma GPCR-related news? GPCR monthly newsletter for FREE! ➡️ https://bit.ly/3cCI4em #gpcr #drgpcr

  • Dr. Juan José Fung - Dr. GPCR Podcast

    GPCR Podcast is back this week with a brand new episode. Our guest is none other than Dr. Juan Jose Fung, Principal Scientist, at GPCR Therapeutics. https://buff.ly/32fzGbO #gpcr #drgpcr #podcast

  • Dr. Ben Myers - Dr. GPCR Podcast

    GPCR podcast is now available! Our guest is Dr. Ben Myers! studying sensory #ionchannels to the group leader at the University of Utah investigating Class F #GPCRs Listen nowhere you get your podcasts https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ #gpcr #drgpcr

  • Integrating Fluorescent Ligands into Flow Cytometry: Enhancing GPCR Analysis Beyond Traditional Antibody Staining

    In order to expand its role in GPCRs, which antibodies tend to have more trouble binding to. How Fluorescent Ligands Transform Flow Cytometry in GPCR Analysis GPCRs are a tough target in traditional At Celtarys, we support this transition by offering optimized fluorescent ligands specifically designed for GPCR targets , including CELT-240 for hD2/D3 dopamine receptors and CELT-483 for the hσ1/σ2 sigma Illuminating the life of GPCRs.

  • Learn about Dr. GPCR Ecosystem!

    GPCR is much more than a podcast? Come check out the brand new Dr. GPCR Ecosystem and explore its benefits! We have #GPCR News, Learning Center, Events, and more to discover! Learn More HERE ➡️ https://www.ecosystem.drgpcr.com/learning-center #gpcr #drgpcr

  • Innovative Data-Driven Solutions: The pHSense Revolution

    Instead of creating another black-box assay, they designed pHSense around rare-earth europium probes. The Chemistry That Almost Didn’t Work Designing pH-sensitive rare-earth complexes was not an obvious Just a plate reader, an agonist, and an endogenous GPCR. GPCR   Dr. GPCR X Revvity Collaboration ⸻ Want more like this? 👉 Join the Dr. GPCR Premium Ecosystem for behind-the-scenes access to GPCR innovators, exclusive deep-dives, and practical

  • Dr. Tim De Groof - Dr. GPCR Podcast

    GPCR podcast is now available! Our guest is Dr. Tim De Groof! It’s not often when you get the best of both worlds - nano-bodies and #GPCRs. Listen where you get your podcasts https://www.ecosystem.drgpcr.com/dr-gpcr-podcast #gpcr #drgpcr #podcast

  • The Perils and Guardrails of Modifying Signalling Proteins in Bioassays

    biosensors involves the use of mini-G proteins, which are genetically engineered portions of Gα subunits designed Allosteric Modulator Discovery: From Serendipity to Structure-Based Design. Allosteric modulation of GPCRs: From structural insights to in silico drug discovery. Rational design of allosteric modulators: Challenges and successes. Biased Allosteric Modulators: New Frontiers in GPCR Drug Discovery.

  • Dr. JoAnn Trejo - Dr. GPCR Podcast

    GPCR podcast is now available! Our guest is Dr. JoAnn Trejo! Listen where you get your podcasts https://www.ecosystem.drgpcr.com/dr-gpcr-podcast #gpcr #drgpcr #podcast

  • Drug Discovery Picks Up the Pace, Stays on Target

    However, in drug discovery projects, perfection can’t be attained soon enough. A project to develop a perfect drug, or a drug that is as safe and effective as possible, may never begin If only Voltaire were here today to see how drug discovery is being accelerated by new technologies. receptors (GPCRs) to enable the discovery of agonistic biologics; and automated instrumentation that Read more at the source #DrGPCR #GPCR #IndustryNews

  • Structural basis of GPCR coupling to distinct signal transducers: implications for biased signaling

    August 2022 "Three classes of G-protein-coupled receptor (GPCR) partners - G proteins, GPCR kinases, and arrestins - preferentially bind active GPCRs. Our analysis suggests that the structures of GPCRs bound to these interaction partners available today do not reveal a clear conformational basis for signaling bias, which would have enabled the rational design Read more at the source #DrGPCR #GPCR #IndustryNews

  • Dr. Nicola J. Smith - Dr. GPCR Podcast

    GPCR Podcast, we have Dr. https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ #gpcr #drgpcr #podcast

  • Structural basis of adhesion GPCR GPR110 activation by stalk peptide and G-proteins coupling

    However, the detailed mechanism of aGPCR activation remains elusive. The structures also unveil the rarely explored GPCR/G12 and GPCR/G13 engagements. Taken together, our study fills the missing information of GPCR/G-protein engagement and provides a framework for understanding aGPCR activation and GPR110 signaling." Read more at the source #DrGPCR #GPCR #IndustryNews

  • Ode to GPCRs

    The first Nobel prize that can be attributed to work related to GPCR-mediated signaling was the 1947 , Sir James Whyte Black, and Gertrude Belle Elion for their discoveries of important principles for drug treatment.[24–30] Black was particularly interested in developing drugs that targeted GPCRs and was These odorant receptors (ORs) now account for about 60% of all identified human GPCRs. GPCR signaling, and location bias.[68–70] Further, our understanding of cross-talk between GPCR-mediated

  • Membrane Lipids Are an Integral Part of Transmembrane Allosteric Sites in GPCRs: A Case Study of...

    October 2022 Membrane Lipids Are an Integral Part of Transmembrane Allosteric Sites in GPCRs: A Case Negative Allosteric Modulator, ORG27569, and Analogs "A growing number of G-protein-coupled receptor (GPCR transmembrane sites for accurate characterization, binding-affinity calculations, and lead optimization in drug Read more at the source #DrGPCR #GPCR #IndustryNews

  • Dr. Thomas P. Sakmar - Dr. GPCR Podcast

    GPCR podcast! Give it a listen to hear from Dr. Thomas P. Sakmar on how the molecular studies of rhodopsin paved the way to understanding #GPCRs Be sure to subscribe https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ #drgpcr #gpcr #podcast

  • Dr. GPCR Virtual Cafe - Postponed

    GPCR Virtual Cafe with Matthew Eddy scheduled for tomorrow (Sep 29th, 2022) due to Hurricane Ian that #gpcr #drgpcr

  • Dr. Peter Robert Banks - Dr. GPCR Podcast

    GPCR podcast is now available! Our guest is Dr. Listen where you get your podcasts. https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ #gpcr #drgpcr #

  • Lysosomal GPCR-like protein LYCHOS signals cholesterol sufficiency to mTORC1

    Read more at the source #DrGPCR #GPCR #IndustryNews

  • Automated micro-plate-based methods for quantifying GPCR activation

    Joe Clayton from BioTek Instruments talk about automated micro-plate-based methods for quantifying #GPCR activation. https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #drgpcr #gpcr #virtualcafe

  • From DNA day to GPCR genomics

    What does DNA Day have to do with GPCRs? GPCR biology, the development of GPCR-targeted drugs, and the exploration of GPCRs as key regulators in the total count of GPCR genes in the human genome. Furthermore, computational genomics approaches, such as structural bioinformatics analysis, have facilitated drug discovery and design targeting GPCRs, leading to the development of novel therapeutics.

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