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142 items found for "human"
- Molecular targets of psychedelic-induced plasticity
Considering the central role of the serotonin 5-HT2A receptor in the distinct effects of psychedelics in human Here we discuss some of the most recent findings in human studies and contextualize them considering
- Odorant receptors – a bit of smell for drug discovery
Although ORs expression is quite stable, the number of ORs expressed in different human tissues is highly OR4N4 is the most highly expressed OR in human spermatozoa and is an example of a highly and selectively In the human kidney ORs elicit intracellular Ca2+flux in renal proximal tubule cells via adenylyl cyclase In the skin, OR51E2 was shown to play a role in human melanocyte homeostasis (Gelis L. et. al 2016) and the sandalore-activated receptor OR2AT4 shown to promote human keratinocyte proliferation and migration
- G protein-coupled receptor 21 in macrophages: An in vitro study
The aim of this study was to evaluate the role of GPR21 in human macrophages, analyzing (i) its involvement Boyden chamber migration assay, performed on macrophages derived from both the THP-1 cell line and human
- GPCR Signaling and mTORC1 Regulation
The activation of mTOR complex 1 (mTORC1) is typically observed in human disease and continues to be Significance Statement mTORC1 is a master regulator of many cellular processes and is often hyperactivated in human the molecular underpinnings of these pathways will undoubtedly be promising to the mTORC1 field and human
- Arginine 125 Is an Essential Residue for the Function of MRAP2
Results obtained with the MRAP2 mutants R125H and R125C, which are found in human patients with extreme MRAP2, in which arginine 125 is normally replaced by histidine, were compared with those obtained with human
- Novel interaction between neurotrophic factor-α1/carboxypeptidase E and serotonin receptor, 5-HTR1E,
mechanism involving interaction between neurotrophic factor-α1 (NF-α1/carboxypeptidase E, CPE) and human Immunofluorescence studies showed 5-HTR1E and NF-α1/CPE are highly expressed and co-localized on cell surface of human Importantly, knock-down of 5-HTR1E in human primary neurons diminished the NF-α1/CPE-mediated protection
- GPCR Weekly Whirlwind: Top Receptor Highlights from Sep 30 - Oct 6, 2024!
Christopoulos , Christopher Langmead , et al. for their outstanding work on Ligand-directed biased agonism at human of Hypoparathyroidism World first: Australian scientists uncover “plant-like” behavior in important human receptors through auxiliary KCTD proteins accelerates channel gating Ligand-directed biased agonism at human Context, methodology and implications Structural and Molecular Insights into GPCR Function LYCHOS is a human
- 📰 GPCR Weekly News, March 18 to 24, 2024
Miles Thompson, Alexander Hauser, Caroline Gorvin et al. for their research on GPCR gene variants and human from March 18th to 24th, 2024 GPCR Activation and Signaling Calcium-Driven In Silico Inactivation of a Human endosomes and other organelles Reviews, GPCRs, and more G protein-coupled receptor (GPCR) gene variants and human
- Accelerating GPCR Drug Discovery With Conformation-Stabilizing VHHs
based on amino acid sequence similarities, but only four of the classes (A, B, C, and F) are found in humans Despite this high number of GPCR targeted drugs, only a small portion (∼110) of the human GPCRome (consisting
- Pharmacophore-guided Virtual Screening to Identify New β 3 -adrenergic Receptor Agonists
Ligand-based pharmacophore modeling was performed since no 3D structure of human β3 -AR is yet available Out of 35 tested compounds, 4 compounds were active in CHO-K1 cells expressing the human β3 -AR, and
- 📰 GPCR Weekly News, March 25 to March 31, 2024
Caculitan, and Adam W Smith for their research on β2-adrenergic receptor associates with CXCR4 multimers in human neurons GPCR Binders, Drugs, and more In silico identification of a biarylamine acting as agonist at human homeostasis GPCRs in Oncology and Immunology The β2-adrenergic receptor associates with CXCR4 multimers in human receptor class C group 5 member A expression on lipopolysaccharide-induced inflammatory response in human
- FSH and bone: Comparison between males with central versus primary hypogonadism
proposed a direct effect of follicle-stimulating hormone (FSH) on the skeletal metabolism, but results of human
- Design and validation of recombinant protein standards for quantitative Western blot analysis of...
and stable recombinant protein constructs GST-CB1414-472 and GST-CB1414-442 containing much of the human the C-terminal residues 443-473 of the mouse CB1 receptor that corresponds to residues 442-472 in the human
- Positive Recommendation for Use of TAVNEOS™ (avacopan) in ANCA Vasculitis Adopted by European ...
in ANCA Vasculitis Adopted by European Medicines Agency (EMA) Committee for Medicinal Products for Human CCXI), today announced that the European Medicines Agency’s (EMA) Committee for Medicinal Products for Human
- 📰 GPCR Weekly News, November 6 to November 12, 2023
Larixol is not an inhibitor of Gαi containing G proteins and lacks effect on signaling mediated by human expressed formyl peptide receptors Molecular recognition of niacin and lipid-lowering drugs by the human of hedgehog pathway repression in tissue morphogenesis TIPE proteins control directed migration of human
- Differences across sexes on head-twitch behavior and 5-HT2A receptor signaling in C57BL/6J mice
Current studies focused on the potentially clinical effects of psychedelics on human subjects tend to Here we tested the effects of DOI on head-twitch behavior (HTR) - a mouse behavioral proxy of human psychedelic
- 📰 GPCR Weekly News, February 26 to March 3, 2024
Horn et. al for their for their research on adhesion GPCR transcript variants from publicly available human and structure of adhesion GPCR transcript variants assembled from publicly available deep-sequenced human samples GPCR Activation and Signaling Structure-guided engineering of biased-agonism in the human niacin
- Harnessing Deep Mutational Scanning for Enhanced Drug Discovery
advent of precision medicine by enabling a more detailed understanding of how genetic variation within human systems might not replicate the natural environment or post-translational modifications observed in humans the application of DMS to a wider array of biological systems, including multicellular organisms and human
- GPR125 (ADGRA3) is an autocleavable adhesion GPCR that traffics with Dlg1 to the basolateral...
Here, we show that human GPR125 likely undergoes cis-autoproteolysis when expressed in canine kidney epithelial MDCK cells and human embryonic kidney HEK293 cells.
- 📰 GPCR Weekly News, July 24 to July 30, 2023
Terence Hébert’s work on Comparative study on human iPSC-derived vs. rat neonatal cardiomyocytes. Comparing the signaling and transcriptome profiling landscapes of human iPSC-derived and primary rat Profiling neuronal methylome and hydroxymethylome of opioid use disorder in the human orbitofrontal cortex
- 📰 GPCR Weekly News, September 18 to 24, 2023
secretory phenotype Mesenchymal stromal cell secretory molecules improve the functional survival of human frequent and specific expression of PRL3 in pediatric solid tumors for first-in-child use of PRL3-zumab humanized HTR1E serotonin receptor Structural and Molecular Insights into GPCR Function Cryo-EM structures of human
- Advancements in G protein-coupled receptor biosensors to study GPCR-G protein coupling
Biosensors for monitoring G protein-coupled receptors (GPCRs), the most drugged class of proteins in the human
- GPCR/endocytosis/ERK signaling/S2R is involved in the regulation of the internalization...
involved in the regulation of the internalization, mitochondria-targeting and -activating properties of human salivary histatin 1 "Human salivary histatin 1 (Hst1) exhibits a series of cell-activating properties
- Embark on a GPCR Adventure: Your Weekly Research Expedition! | Oct 21-27, 2024
bass (Micropterus salmoides) The pyruvate-GPR31 axis promotes transepithelial dendrite formation in human intestinal dendritic cells Methods & Updates in GPCR Research Generation of CRISPR/Cas9 modified human
- Genome-wide identification of 216 G protein-coupled receptor (GPCR) genes from the marine water ...
Phylogenetic comparison of GPCRs in D. celebensis to those in humans (Homo sapiens), fruitfly (Drosophila and opsin receptor repertoire, while purinergic and chemokine receptors were highly differentiated in humans
- 📰 GPCR Weekly News, January 15 to 21, 2024
Graham Ladds’ team refines AlphaFold models using binding calculations for human adenosine A3 receptor FR900359 Derived From Unculturable Plant Symbiont Systematic assessment of chemokine ligand bias at the human Design Using Kinetic and Thermodynamic Binding Calculations: A Case Study for the Unresolved Inactive Human
- Specific Functions of Melanocortin 3 Receptor (MC3R)
Despite the drastic effects of the MC3R deficiency in humans and other mammals, its cellular mechanisms
- GRK2 selectively attenuates the neutrophil NADPH-oxidase response triggered by β-arrestin recruiting
GRK2 was shown to be expressed in human neutrophils and analysis of subcellular fractions revealed a