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280 results for “nuclear receptors”
Chemogenomics for NR1 nuclear hormone receptors
<p>Compound information sheets for our chemogenomic library (CGL) for the NR1 family of nuclear hormone receptors.</p> <p>The information sheets contain general information about the substances, the biological activity for the NR main targets and NR off-targets, as well as information about identity and purity.</p>
Phosphorylation regulated conformational diversity and topological dynamics of an intrinsically disordered nuclear receptor
<p>Molecular dynamics simulations of AF1c region of human glucocorticoid receptor and its phosphovariants as described in the below paper: </p> <p>Phosphorylation regulated conformational diversity and topological dynamics of an intrinsically disordered nuclear receptor</p> <p>Vasily Akulov, Alba Jiménez Panizo, Eva Estébanez-Perpiñá, John van Noort, Alireza Mashaghi</p> <p> </p> <p>The data related to this project has been deposited in two repositories. This repository contains the second part of the data; the first part can be found at DOI: 10.5281/zenodo.13820169</p>
The nuclear import receptor Kapβ2 modifies neurotoxicity mediated by poly(GR) in C9orf72-linked ALS/FTD
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NUclear Receptor Activity (NURA) dataset
<p><strong>Dataset information</strong></p> <p>NURA (NUclear Receptor Activity) dataset collects curated information on small molecules that modulate nuclear receptors (NRs), to be intended for both pharmacological and toxicological applications. NURA contains bioactivity annotations for 15,247 molecules and 11 selected NRs, and it was obtained by integrating and curating data from toxicological and pharmacological databases (<em>i.e.,</em> Tox21, ChEMBL, NR-DBIND and BindingDB). NURA dataset is a useful tool to bridge the gap between toxicology- and medicinal-chemistry-related databases, as it is enriched in terms of number of molecules, structural diversity and covered atomic scaffolds compared to the single sources. To the best of our knowledge, NURA dataset is the most exhaustive collection of small molecules annotated for their modulation of the chosen nuclear receptors. NURA dataset is intended to support decision-making in pharmacology and toxicology, as well as to contribute to data-driven applications, such as machine learning. </p> <p><strong>Content</strong></p> <p>Three files are provided:</p> <ol> <li>"Nura_v1.0.0.csv" [datafile] dataset containing activity labels for each molecule (rows, identified by a unique ID and the canonical SMILES string) and each nuclear receptor endpoint (columns).</li> <li>"Nura_v1.0.0_details" [datafile], containing information on the individual records used to generate the dataset.</li> <li>"curation_pipeline.zip" [software], containing the data curation pipeline in KNIME ("NURA_Dataset.knwf") as well as a help file ('help.pdf').</li> </ol> <p>Additional details on the content and curation pipeline can be found in the uploaded, non peer-reviewed, preprint ("NURApreprint.pdf").</p> <p><strong>Version information</strong></p> <ul> <li>v1.0.1: data curation pipeline uploaded.</li> <li>v.1.0.0: initial upload.</li> </ul> <p><strong>Contact</strong></p> <p>If you have any question, contact us! (Francesca Grisoni, francesca.grisoni@pharma.ethz.ch; Davide Ballabio, davide.ballabio@unimib.it)</p>
Cellular uptake of silica and gold nanoparticles induces early activation of nuclear receptor NR4A1
<p>The approval of new nanomedicines requires a deeper understanding of the interaction between cells and nanoparticles (NPs). Silica (SiO<sub>2</sub>) and gold (Au) NPs have shown great potential in biomedical applications, such as the delivery of therapeutic agents, diagnostics, and biosensors. NP-cell interaction and internalization can trigger several cellular responses, including gene expression regulation. The identification of differentially expressed genes in response to NP uptake contributes to a better understanding of the cellular processes involved, including potential side effects. We investigated gene regulation in human macrophages and lung epithelial cells after acute exposure to spherical 60 nm SiO<sub>2</sub> NPs. SiO<sub>2</sub> NPs uptake did not considerably affect gene expression in epithelial cells, whereas five genes were up-regulated in macrophages. These genes are principally related to inflammation, chemotaxis, and cell adhesion. NR4A1, an important modulator of inflammation in macrophages, was found to be up-regulated. The expression of this gene was increased upon 1 h of macrophage exposure to spherical 50 nm AuNPs and 200 nm spherical SiO<sub>2</sub> NPs. NR4A1 can thus be an important immediate regulator of inflammation provoked by NP uptake in macrophages.</p>
Phosphorylation regulated conformational diversity and topological dynamics of an intrinsically disordered nuclear receptor
<p>Molecular dynamics simulations of AF1c region of human glucocorticoid receptor and its phosphovariants as described in the below paper: </p> <p><strong>Phosphorylation regulated conformational diversity and topological dynamics of an intrinsically disordered nuclear receptor</strong></p> <p>Vasily Akulov, Alba Jiménez Panizo, Eva Estébanez-Perpiñá, John van Noort, Alireza Mashaghi</p> <p> </p> <p>The data related to this project has been deposited in two repositories. This repository contains the first part of the data; the second part can be found at the DOI: 10.5281/zenodo.13822438</p>
Nuclear receptor E75 regulates molting and ovarian development in <em>Nilaparvata lugens</em>
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Dataset for: A structural signature motif enlightens the origin and diversification of nuclear receptors
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Systematic Gene Expression Mapping Clusters Nuclear Receptors According to Their Function in the Brain - Website save
<p>This is a copy of the website that was related to mousepat.ics-mci.fr</p>
Impact of the Rapid Normalization of Chronic Hyperglycemia and the Practice of Moderate Physical Activity on the "Receptor Activator of Nuclear Factor-kappa B Ligand / Osteoprotégérine (RANKL / OPG) S
ClinicalTrials.gov study NCT04893135. IPD Sharing: NO. Countries: 1. Publications: 0.
Data from: The Drosophila HNF4 nuclear receptor promotes glucose-stimulated insulin secretion and mitochondrial function in adults
Although mutations in HNF4A were identified as the cause of Maturity Onset Diabetes of the Young 1 (MODY1) two decades ago, the mechanisms by which this nuclear receptor regulates glucose homeostasis remain unclear. Here we report that loss of Drosophila HNF4 recapitulates hallmark symptoms of MODY1, including adult-onset hyperglycemia, glucose intolerance and impaired glucose-stimulated insulin secretion (GSIS). These defects are linked to a role for dHNF4 in promoting mitochondrial function as well as the expression of Hex-C, a homolog of the MODY2 gene Glucokinase. dHNF4 is required in the fat body and insulin-producing cells to maintain glucose homeostasis by supporting a developmental switch toward oxidative phosphorylation and GSIS at the transition to adulthood. These findings establish an animal model for MODY1 and define a developmental reprogramming of metabolism to support the energetic needs of the mature animal.
Data from: Hepatic Aryl hydrocarbon Receptor Nuclear Translocator (ARNT) regulates metabolism in mice
Background & Aims: Aryl hydrocarbon Receptor Nuclear Translocator (ARNT) and its partners hypoxia-inducible factors (HIF)-1α and HIF-2α are candidate factors for the well-known link between the liver, metabolic dysfunction and elevation in circulating lipids and glucose. Methods: Hepatocyte-specific ARNT-null (LARNT), HIF-1α-null (LHIF1α) and HIF-2α-null (LHIF2α) mice were created. Results: LARNT mice had increased fasting glucose, impaired glucose tolerance, increased glucose production, raised post-prandial serum triglycerides (TG) and markedly lower hepatic ATP versus littermate controls. There was increased expression of G6Pase, Chrebp, Fas and Scd-1 mRNAs in LARNT animals. Surprisingly, LHIF1α and LHIF2α mice exhibited no alterations in any metabolic parameter assessed. Conclusions: These results provide convincing evidence that reduced hepatic ARNT can contribute to inappropriate hepatic glucose production and post-prandial dyslipidaemia. Hepatic ARNT may be a novel therapeutic target for improving post-prandial hypertriglyceridemia and glucose homeostasis.
Data from: TAF4, a subunit of transcription factor II D, directs promoter occupancy of nuclear receptor HNF4A during post-natal hepatocyte differentiation
The functions of the TAF subunits of mammalian TFIID in physiological processes remain poorly characterised. Here we describe a novel function of TAFs in directing genomic occupancy of a transcriptional activator. Using liver-specific inactivation in mice, we show that the TAF4 subunit of TFIID is required for post-natal hepatocyte maturation. TAF4 promotes pre-initiation complex (PIC) formation at post-natal expressed liver function genes and down-regulates a subset of embryonic expressed genes by increased RNA polymerase II pausing. The TAF4-TAF12 heterodimer interacts directly with HNF4A and in vivo TAF4 is necessary to maintain HNF4A-directed embryonic gene expression at post-natal stages and promotes HNF4A occupancy of functional cis-regulatory elements adjacent to the transcription start sites of post-natal expressed genes. Stable HNF4A occupancy of these regulatory elements requires TAF4-dependent PIC formation highlighting that these are mutually dependent events. Local promoter-proximal HNF4A-TFIID interactions therefore act as instructive signals for post-natal hepatocyte differentiation.
Data from: Functional divergence of the nuclear receptor NR2C1 as a modulator of pluripotentiality during hominid evolution
Genes encoding nuclear receptors (NRs) are attractive as candidates for investigating the evolution of gene regulation because they (1) have a direct effect on gene expression and (2) modulate many cellular processes that underlie development. We employed a three-phase investigation linking NR molecular evolution among primates with direct experimental assessment of NR function. Phase 1 was an analysis of NR domain evolution and the results were used to guide the design of phase 2, a codon-model-based survey for alterations of natural selection within the hominids. By using a series of reliability and robustness analyses we selected a single gene, NR2C1, as the best candidate for experimental assessment. We carried out assays to determine whether changes between the ancestral and extant NR2C1s could have impacted stem cell pluripotency (phase 3). We evaluated human, chimpanzee, and ancestral NR2C1 for transcriptional modulation of Oct4 and Nanog (key regulators of pluripotency and cell lineage commitment), promoter activity for Pepck (a proxy for differentiation in numerous cell types), and average size of embryological stem cell colonies (a proxy for the self-renewal capacity of pluripotent cells). Results supported the signal for alteration of natural selection identified in phase 2. We suggest that adaptive evolution of gene regulation has impacted several aspects of pluripotentiality within primates. Our study illustrates that the combination of targeted evolutionary surveys and experimental analysis is an effective strategy for investigating the evolution of gene regulation with respect to developmental phenotypes.
Development and Validation of in Vitro Cell-based Bioassays for Nuclear Receptor Activation
ClinicalTrials.gov study NCT02434562. IPD Sharing: Not stated. Countries: 0. Publications: 1.
Data from: A new method to localize and test the significance of incongruence: detecting domain shuffling in the nuclear receptor superfamily
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Data from: TAF4, a subunit of transcription factor II D, directs promoter occupancy of nuclear receptor HNF4A during post-natal hepatocyte differentiation
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Data from: The Drosophila HNF4 nuclear receptor promotes glucose-stimulated insulin secretion and mitochondrial function in adults
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Data from: Functional divergence of the nuclear receptor NR2C1 as a modulator of pluripotentiality during hominid evolution
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Data from: Widespread epigenetic changes to the enhancer landscape of mouse liver induced by a specific xenobiotic agonist ligand of the nuclear receptor CAR
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Allen Brain Atlas
Allen Brain Atlas is an Allen Institute collection of brain map atlases, datasets, APIs, and analysis tools covering mouse, human, and non-human primate brain resources.
Annotated Behaviour and Observability Dataset (ABODe)
ABODe is a University of Edinburgh DataShare dataset for behavior classification in group-housed mice using home-cage video, identities, bounding boxes, ground-plate positions, and annotator labels.
DANDI Archive for NWB datasets
DANDI is a BRAIN Initiative archive for publishing and sharing neurophysiology data, including electrophysiology, optophysiology, and behavioral data packaged as NWB and related standards.
International Brain Laboratory public data
The International Brain Laboratory public data releases expose standardized mouse decision-making experiments, including Neuropixels recordings, widefield calcium imaging, behavior, and session metadata accessed through the ONE API.
OpenNeuro
OpenNeuro is a free, open platform for sharing neuroimaging datasets, with public search, dataset pages, and download paths for web, S3, DataLad, and the OpenNeuro CLI.