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539 items found for "GPCR Drug Design"

  • 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

  • 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

  • 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

  • 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

  • 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

  • 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. Nicola J. Smith - Dr. GPCR Podcast

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

  • 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 #

  • 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

  • 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

  • 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

  • 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. GPCR Summit 2022 is coming!

    GPCR Summit 2022 held between October 10th and 16th. Dr. GPCR Summit is FREE for all Ecosystem site members! Become a member today, it's also free! ➡️ https://bit.ly/3wKZmfR #gpcr #drgpcr

  • Dr. GPCR Summit 2022 is coming!

    GPCR Summit is between October 10th to the 16th! ➡️ https://www.ecosystem.drgpcr.com/dr-gpcr-summit-2022 #gpcr #drgpcr

  • 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

  • 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

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

    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

  • The complicated lives of GPCRs in cardiac fibroblasts

    October 2022 "The role of different G protein-coupled receptors (GPCRs) in the cardiovascular system In VSMCs, stimulation of GPCRs also modulates contractile and cell growth phenotypes. Here, we will focus on the relatively less well-studied effects of GPCRs in cardiac fibroblasts, focusing We discuss how such events may be distinct depending on where the GPCRs and their associated signaling Read more at the source #DrGPCR #GPCR #IndustryNews

  • Function and structure of bradykinin receptor 2 for drug discovery

    October 2022 "Type 2 bradykinin receptor (B2R) is an essential G protein-coupled receptor (GPCR) that provided molecular insights into the functions and regulation of B2R, which shed light on structure-based drug design for the treatment of B2R-related diseases. In this review, we summarize the structure and function of B2R in relation to drug discovery and discuss Read more at the source #DrGPCR #GPCR #IndustryNews

  • A cryptic mode of GPCR regulation revealed

    2022 "Over three decades of research have provided thorough insights into G protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

  • Mechanistic basis of GPCR activation explored by ensemble refinement of crystallographic structures

    October 2022 "G protein-coupled receptors (GPCRs) are important drug targets characterized by a canonical Recent advances in X-ray crystallography and cryo-EM have resulted in a wealth of GPCR structures that have been used in drug design and formed the basis for mechanistic activation hypotheses. adrenergic receptor (β2 AR) and A2A adenosine receptor (A2A AR). " Read more at the source #DrGPCR #GPCR

  • Dimerization of GPCRs: Novel insight into the role of FLNA and SSAs regulating SST2 and SST5...

    September 2022 Dimerization of GPCRs: Novel insight into the role of FLNA and SSAs regulating SST2 and SST5 homo- and hetero-dimer formation "The process of GPCR dimerization can have profound effects on GPCR activation, signaling, and intracellular trafficking. Somatostatin receptors (SSTs) are class A GPCRs abundantly expressed in pituitary tumors where they represent Read more at the source #DrGPCR #GPCR #IndustryNews

  • Odorant receptors – a bit of smell for drug discovery

    function and expression landscape Odorant receptors (ORs) belong to the G protein-coupled receptor (GPCR compounds, there has been a growing interest from the scientific community to target this class of GPCRs (for drug repurposing) and endogenous ligands. design. Check the original article at https://pubmed.ncbi.nlm.nih.gov/35999088/ #GPCR #DrGPCR#Ecosystem

  • 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.

  • GPR125 (ADGRA3) is an autocleavable adhesion GPCR that traffics with Dlg1 to the basolateral...

    October 2022 GPR125 (ADGRA3) is an autocleavable adhesion GPCR that traffics with Dlg1 to the basolateral membrane and regulates epithelial apicobasal polarity "The adhesion family of G protein-coupled receptors (GPCRs GPR125 (ADGRA3), an orphan adhesion GPCR, has been shown to modulate planar cell polarity in gastrulating Thus, the basolateral protein GPR125, an autocleavable adhesion GPCR, appears to play a crucial role Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the newsletter HERE

  • 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

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