Search Results
565 items found for "class C GPCR"
- Structure-Based Discovery of Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5
October 2022 "Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed treatment of psychiatric and neurodegenerative diseases, and several allosteric modulators of this GPCR libraries have complementary advantages and illustrate how access to high-resolution structures of GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews
- Production of human A2AAR in lipid nanodiscs for 19F-NMR and single-molecule fluorescence...
single-molecule fluorescence spectroscopy "We describe production of the human A2A adenosine receptor (A2AAR), a class A G protein-coupled receptor (GPCR) for 19F-NMR and single-molecule fluorescence (SMF) spectroscopy. Read more at the source #DrGPCR #GPCR #IndustryNews
- GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between ...
GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between Health and Disease GPCRs arguably represent the most effective current therapeutic targets for a plethora GPCRs also possess a pivotal role in the regulation of the physiological balance between healthy and changes in organismal tissue complexity and compartmentalization, thus enabling a nuanced GPCR-based GPCRs have been long considered as controllers of communication between tissues and cells.
- Chemical signaling regulates axon regeneration via the GPCR-Gqα pathway in Caenorhabditis elegans
demonstrate that the chemoreceptor genes, srg-36 and srg-37 , which encode G protein-coupled receptors (GPCRs SIGNIFICANCE STATEMENT In C. elegans , axon regeneration is positively regulated by the EGL-30 Gqα-JNK Here, we show that SRG-36 and SRG-37 act as upstream GPCRs that activate EGL-30. SRG-36 and SRG-37 are GPCRs for the dauer-inducing ascaroside, ascr#5. Thus, ascaroside signaling promotes axon regeneration by activating the GPCR-Gqα pathway.
- PH-Binding Motif in PAR4 Oncogene: From Molecular Mechanism to Drug Design
October 2022 "While the role of G-protein-coupled receptors (GPCR) in cancer is acknowledged, their underlying Protease-activated receptors (PAR), a subgroup of GPCRs, form a family of four members (PAR1-4) centrally Point mutations are in the C-tail of PAR4 PH-binding domain; F347 L and D349A, but not E346A, abrogate Read more at the source #DrGPCR #GPCR #IndustryNews
- Identification of GPCRs Modulating Flow-induced Signaling Pathways in Vascular Endothelial Cells
Brian Arey is doing. https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #virtualcafe
- 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. with a prototypical GPCR by nuclear magnetic resonance (NMR) spectroscopy. This plasticity of βarr conformation in complex with GPCRs engaged in different binding modes may explain
- 8th RSC / SCI symposium on GPCRs in Medicinal Chemistry. October 5-7, 2022, Verona, Italy
August 2022 "GPCRs in Medicinal Chemistry Event 8th RSC / SCI symposium on GPCRs in Medicinal Chemistry 6th September 30th September – online registration (card payments)" Read more at the source #DrGPCR #GPCR
- Subscribe to our monthly newsletter for FREE!
Do you hustle around looking for information about your favorite #GPCR? No need for that anymore! GPCR has it for you! 🔔 Subscribe to our monthly newsletter for FREE! ➡️ https://bit.ly/3cCI4em #gpcr #drgpcr
- Sign Up Now!
🌐 🤝 We want to bring closer the #GPCR community! Join the Dr. GPCR Ecosystem as a site member today for FREE and start exploring! Sign up now! ➡️ https://www.ecosystem.drgpcr.com/explore-individuals #gpcr #drgpcr
- New Resources in GPCRdb
GPCR on the 24th of June! This time, the GPCRdb team ( Dr. David Gloriam , Dr. Albert Kooistra & Gáspár Pándy-Szekeres ) will present and demonstrate the newest resources of the GPCRdb Reserve your spot for free at: https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #GPCR #GPCRs #DrGPCR #GPCRdb #VirtualCafe
- Effect Delta-9-tetrahydrocannabinol and cannabidiol on milk proteins and lipid levels in HC11 cells
Read more at the source #DrGPCR #GPCR #IndustryNews
- Adrenal G Protein-Coupled Receptors and the Failing Heart: A Long-distance, Yet Intimate Affair
release of these hormones in the adrenals is tightly regulated by adrenal G protein-coupled receptors (GPCRs 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
- 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
- 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 As a result, there is an ongoing need to develop novel approaches to monitor and to modulate GPCR activation nanobodies have been adopted to elucidate the structure, pharmacology, and signaling of cardiovascular GPCRs 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) Guided Pharmacology of Membrane Proteins (BJP 75th Anniversary). " Read more at the source #DrGPCR #GPCR
- TM5-TM6: structural switches that modulate the coupling of serotonin receptors to Gs or Gi
What is the molecular basis that determines that GPCRs bind selectively or promiscuously to different The discovery of the orthosteric binding pocket is of great importance in GPCRs field as it supports Additionally, structural analysis of the TM5 and TM6 regions of 27 class A GPCRs coupled to Gs or Gi/ A GPCRs. #GPCR #DrGPCR
- Design and validation of recombinant protein standards for quantitative Western blot analysis of...
antibody-antigen interaction-based approaches for quantitative analysis of G protein-coupled receptor (GPCR GPCRs in general and cannabinoid CB1 receptor in particular show a progressive tendency to aggregate This renders full-length recombinant GPCRs useless for analytical purposes, a problem that can be overcome To this end we used three different antibodies, all raised against a peptide comprising the C-terminal Read more at the source #DrGPCR #GPCR #IndustryNews
- Structural landscape of the Chemokine Receptor system
Chemokine receptors (CKRs) belong to a subfamily of G-protein-coupled receptors (GPCRs) and play a crucial A GPCR family. Activation in Class A GPCRs Ligand binding in the orthosteric site leads to diverse activation mechanisms In class A GPCRs, the inactive conformation is stabilized by the inactive configuration of the D3.49R3.50Y3.51motif In addition, it has a glutamate residue at position 3.45, which is not found in human class A GPCRs,
- β-arrestin1 promotes tauopathy by transducing GPCR signaling, disrupting microtubules and autophagy
G protein-coupled receptors (GPCRs) have been shown to play integral roles in Alzheimer's disease pathogenesis However, it is unclear how diverse GPCRs similarly affect Aβ and tau pathogenesis. GPCRs share a common mechanism of action via the β-arrestin scaffolding signaling complexes, which not only serve to desensitize GPCRs by internalization, but also mediate multiple downstream signaling events As signaling via the GPCRs, β2-adrenergic receptor (β2AR), and metabotropic glutamate receptor 2 (mGluR2
- Mechanistic Understanding of the Palmitoylation of Go Protein in the Allosteric Regulation of...
)-a major family of GPCRs-play critical roles in the regulation of tissue development and cancer progression The orphan receptor GPR97, activated by glucocorticoid stress hormones, is a prototypical aGPCR. Although it has been established that the palmitoylation of the C-terminal Go protein is essential for of the Go protein, and offers guidance for future drug design of aGPCRs." Read more at the source #DrGPCR #GPCR #IndustryNews
- Activation of the human chemokine receptor CX3CR1 regulated by cholesterol
A much smaller conformational change of helix VI upon activation than previously solved class A GPCR-Gi Thus, our data deepen the understanding of cholesterol modulation in GPCR (G protein-coupled receptor Read more at the source #DrGPCR #GPCR #IndustryNews
- Successful prednisolone or calcimimetic treatment of acquired hypocalciuric hypercalcemia caused...
hypercalcemia caused by biased allosteric CaSR autoantibodies "Biased agonism is a frontier field in GPCR with the 2 cases we previously reported as follows: (a) elderly (74-87 years at diagnosis), (b) male, (c) insights into the phenotype and characteristics of AHH and the mechanisms by which the biased agonism of GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews
- Label-free LC-MS based assay to characterize small molecule compound binding to cells
This assay was applied to various target classes, with particular emphasis on those for which protein-based In one example, to study a G protein coupled receptor (GPCR), we used one antagonist as probe and multiple Read more at the source #DrGPCR #GPCR #IndustryNews
- Enhanced membrane binding of oncogenic G protein αqQ209L confers resistance to inhibitor YM-254890
October 2022 "Heterotrimeric G proteins couple activated G protein-coupled receptors (GPCR) to intracellular They can also function independently of GPCR activation upon acquiring mutations that prevent GTPase YM-254890 (YM) can inhibit signaling by both GPCR-activated wild type αq and GPCR-independent αqQ209L GPCR-dependent signaling by PM-restricted wild type αq is strongly inhibited by YM, demonstrating that Read more at the source #DrGPCR #GPCR #IndustryNews
- Dimerization of β2-adrenergic receptor is responsible for the constitutive activity subjected to inv
Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE
- 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
- Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell...
Originally, β-arrestins were identified for their contribution to GPCR desensitization to agonist-mediated However, current investigations have now recognized that in addition to GPCR arresting (hence the name Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE