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Results found for "Druggable GPCR"
- Pharmacophore-guided Virtual Screening to Identify New β 3 -adrenergic Receptor Agonists
Read more at the source #DrGPCR #GPCR #IndustryNews
- Actions of Parathyroid Hormone Ligand Analogues in Humanized PTH1R Knockin Mice
Read more at the source #DrGPCR #GPCR #IndustryNews
- Therapeutic validation of an orphan G protein-coupled receptor: The case of GPR84
August 2022 "Despite the importance of members of the GPCR superfamily as targets of a broad range of effective medicines many GPCRs remain poorly characterised. pharmacological tool compounds to study its broader role and biology. " Read more at the source #DrGPCR #GPCR
- Asking Better Questions in Science: A Practical Guide for Emerging Researchers
In his collaboration with David Hodson, every major leap—from early ligand design to GPCR visualization Throughout his own journey—from organic chemistry to chemical biology to GPCR imaging—every pivotal step 🎧 Listen to the full episode https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/chemical-probes-for-gpcr-imaging-and-internalization
- Chemical Drug Matter : Rethinking the Molecules We Choose to Develop In Drug Discovery
outcomes An understanding of new chemical sources beyond natural agonist analogs Awareness of how GPCR Allostery and Biased Signaling Change the Game The most profound change in GPCR drug discovery is our GPCRs are not simple on/off switches. Peptide GPCR therapies now address obesity, diabetes, cancer, neuroendocrine disorders, inflammatory GPCR innovation is accelerating.
- Biphasic activation of β-arrestin 1 upon interaction with a GPCR revealed by methyl-TROSY NMR
β-arrestins (βarrs) play multifaceted roles in the function of G protein-coupled receptors (GPCRs). βarrs typically interact with phosphorylated C-terminal tail (C tail) and transmembrane core (TM core) of GPCRs changes for βarr activation upon the C tail- and TM core-mediated interactions with a prototypical GPCR This plasticity of βarr conformation in complex with GPCRs engaged in different binding modes may explain
- C5aR Fluorescent Ligands: Need for new Research Tools
GPCRs are one of the most important families of therapeutic targets in the pharmaceutical industry oncological, degenerative, metabolic, immunological… around a third of the drugs in clinical use are GPCR the C5a anaphylatoxin chemotactic receptor 1 (also known as CD88), is part of the rhodopsin family of GPCRs Trends in GPCR Drug Discovery: New Agents, Targets and Indications. Identification of A2BAR as a Potential Target in Colorectal Cancer Using Novel Fluorescent GPCR Ligands
- GBCRdb for beginners
Join us for a fantastic introduction to GPCRdb with Dr. David Gloriam and Dr. Albert Kooistra. Register today: https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #virtualcafe
- Orion and Peptilogics are pursuing AI-driven drug discovery to explore new functional chemical ...
and precision-engineer therapeutics with enhanced potency and tailored signaling against an undrugged GPCR #ai #drugdiscovery #gpcr" Read more at the source #DrGPCR #GPCR #IndustryNews
- All About Addgene: More Open and Reproducible Science with Materials Sharing
GPCR Virtual Cafe? Register today! Addgene's Dr. Joanne Kamens is our guest. research or you want to share your materials, this is the place to go. https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe / #gpcr #drgpcr #virtualcafe #addgene
- Location bias contributes to functionally selective responses of biased CXCR3 agonists
November 2022 "Some G protein-coupled receptor (GPCR) ligands act as "biased agonists" that preferentially Although GPCRs are primarily found at the plasma membrane, GPCRs can traffic to and signal from many subcellular signaling contributes to the biased signaling generated by three endogenous ligands of the GPCR observed at CXCR3, which has important implications for drugs targeting chemokine receptors and other GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE
- Molecular basis for variations in the sensitivity of pathogenic rhodopsin variants to 9-cis-retinal
Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Newsletter HERE
- G-protein-coupled receptors as therapeutic targets for glioblastoma
In this review, we focus on recent advances in G-protein-coupled receptor (GPCR) targets.
- High hedgehog signaling is transduced by a multikinase-dependent switch controlling the...
signaling is transduced by a multikinase-dependent switch controlling the apico-basal distribution of the GPCR smoothened "The oncogenic G-protein-coupled receptor (GPCR) Smoothened (SMO) is a key transducer of of HH to the apico-basal distribution of SMO and provide a novel mechanism for the regulation of a GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Increased Anxiety-like Behaviors in Adgra1-/- Male But Not Female Mice are Attributable to...
Pathways "Adhesion G protein-coupled receptor A1 (ADGRA1) belongs to the G protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Case Report of a Juvenile Patient with Autism Spectrum Disorder with a Novel Combination of Copy...
Read more at the source #DrGPCR #GPCR #IndustryNews
- Recurrent hypoglycemia increases hepatic gluconeogenesis without affecting glycogen metabolism or sy
hypoglycemia, we first checked expression of counterregulatory hormone G-protein coupled receptors (GPCRs regulators and downstream enzymes catalyzing glycogen metabolism, gluconeogenesis and lipolysis by qPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- ADGRL3 genomic variation implicated in neurogenesis and ADHD links functional effects to the...
harbored in the ADGLR3-hormone receptor domain (HRM, a common extracellular domain of the secretin-like GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews
- Production of human A2AAR in lipid nanodiscs for 19F-NMR and single-molecule fluorescence...
describe production of the human A2A adenosine receptor (A2AAR), a class A G protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Use of CRISPR/Cas9-edited HEK293 cells reveals that both conventional and novel protein kinase C...
are involved in mGlu5a receptor internalization "The internalization of G protein-coupled receptors (GPCRs Additionally, using the Gαq/11 inhibitor YM-254890, GPCR kinase 2 and 3 (GRK2 and GRK3) KO cells, and Our PKC KO cell lines expand the repertoire of KO HEK293A cell lines available to research GPCR pharmacology 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 Read more at the source #DrGPCR #GPCR #IndustryNews
- Specific Functions of Melanocortin 3 Receptor (MC3R)
October 2022 "Melanocortin 3 receptor (MC3R) is a G-protein coupled receptor (GPCR) that is defined Read more at the source #DrGPCR #GPCR #IndustryNews
- GPR15 expressed in T lymphocytes from RA patients is involved in leukocyte chemotaxis to the...
GPR15 is a G protein-coupled receptor (GPCR) located on chromosome 3 and has similarity in its sequence The expression of GPR15 and c10orf99/gpr15l mRNA was analyzed by RT-qPCR. Read more at the source #DrGPCR #GPCR #IndustryNews
- Network pharmacological investigation into the mechanism of Kaixinsan powder for the treatment of...
indicated that the mechanism of KXS in treating depression was involved in the biological process of GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- G protein-coupled receptor signaling: transducers and effectors
October 2022 "G protein-coupled receptors (GPCRs) are of considerable interest due to their importance dynamic structures, and physiological relevance in the cardiovascular system of the three most important GPCR signaling effectors: heterotrimeric G proteins, GPCR kinases (GRKs), and β-arrestins. As new technologies are developed and applied to studying GPCR structure and their downstream effectors Read more at the source #DrGPCR #GPCR #IndustryNews
- Pharmacological targeting of cGAS/STING-YAP axis suppresses pathological angiogenesis and...
STING-YAP signaling by both a small-molecule STING agonist, SR-717, and a G protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Protein Uncoupling as an Innovative Practice in Diabetes Mellitus Treatment: A Metabolic Disorder
Read more at the source #DrGPCR #GPCR #IndustryNews
- Although the cannabinoid type-2 receptor (CB2) is highly expressed in the immune system, emerging...
Read more at the source #DrGPCR #GPCR #IndustryNews
- Synthesis and characterization of an orally bioavailable small molecule agonist of the apelin recept
pentan-3-yl)-1-cyclopentyl-5-(2,6-dimethoxyphenyl)-1H-pyrazole-3-carboxamide hydrochloride) of this GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Fluorescent Ligands Targeting Intracellular Allosteric Binding Site of the Chemokine Receptor CCR2
"Fluorescently labeled ligands are versatile molecular tools to study G protein-coupled receptors (GPCRs targeting the intracellular allosteric binding site (IABS) of the CC chemokine receptor 2 (CCR2), a class A GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
