Search Results - "Sepe, Valentina"
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Hijacking SARS-CoV-2/ACE2 Receptor Interaction by Natural and Semi-synthetic Steroidal Agents Acting on Functional Pockets on the Receptor Binding Domain
Published in Frontiers in chemistry (23-10-2020)“…The coronavirus disease 2019 (COVID-19) is a respiratory tract infection caused by the severe acute respiratory syndrome coronavirus (SARS)-CoV-2. In light of…”
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Development of dual GPBAR1 agonist and RORγt inverse agonist for the treatment of inflammatory bowel diseases
Published in Pharmacological research (01-10-2024)“…Inflammatory bowel diseases (IBD), including Crohn's disease and ulcerative colitis, are chronic disorders characterized by dysregulated immune response and…”
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Design, Synthesis, and Biological Evaluation of Potent Dual Agonists of Nuclear and Membrane Bile Acid Receptors
Published in Journal of medicinal chemistry (13-02-2014)“…Bile acids exert genomic and nongenomic effects by interacting with membrane G-protein-coupled receptors, including the bile acid receptor GP-BAR1, and nuclear…”
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Impaired Itching Perception in Murine Models of Cholestasis Is Supported by Dysregulation of GPBAR1 Signaling
Published in PloS one (15-07-2015)“…In cholestatic syndromes, body accumulation of bile acids is thought to cause itching. However, the mechanisms supporting this effect remain elusive. Recently,…”
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Analysis of Gastric Cancer Transcriptome Allows the Identification of Histotype Specific Molecular Signatures With Prognostic Potential
Published in Frontiers in oncology (03-05-2021)“…Gastric cancer is the fifth most common malignancy but the third leading cause of cancer-associated mortality worldwide. Therapy for gastric cancer remain…”
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Insights on FXR selective modulation. Speculation on bile acid chemical space in the discovery of potent and selective agonists
Published in Scientific reports (07-01-2016)“…Bile acids are the endogenous modulators of the nuclear receptor FXR and the membrane receptor GPBAR1. FXR represents a promising pharmacological target for…”
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Discovery of BAR502, as potent steroidal antagonist of leukemia inhibitory factor receptor for the treatment of pancreatic adenocarcinoma
Published in Frontiers in oncology (14-03-2023)“…The leukemia inhibitory factor (LIF), is a cytokine belonging to IL-6 family, whose overexpression correlate with poor prognosis in cancer patients, including…”
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Structure-based drug design targeting the cell membrane receptor GPBAR1: exploiting the bile acid scaffold towards selective agonism
Published in Scientific reports (16-11-2015)“…Bile acids can regulate nutrient metabolism through the activation of the cell membrane receptor GPBAR1 and the nuclear receptor FXR. Developing an exogenous…”
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Discovery that theonellasterol a marine sponge sterol is a highly selective FXR antagonist that protects against liver injury in cholestasis
Published in PloS one (23-01-2012)“…The farnesoid-x-receptor (FXR) is a bile acid sensor expressed in the liver and gastrointestinal tract. Despite FXR ligands are under investigation for…”
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Discovery of a Potent and Orally Active Dual GPBAR1/CysLT1R Modulator for the Treatment of Metabolic Fatty Liver Disease
Published in Frontiers in pharmacology (25-04-2022)“…Nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH) are two highly prevalent human diseases caused by excessive fat deposition in…”
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The leukemia inhibitory factor regulates fibroblast growth factor receptor 4 transcription in gastric cancer
Published in Cellular oncology (Dordrecht) (01-04-2024)“…Purpose The gastric adenocarcinoma (GC) represents the third cause of cancer-related mortality worldwide, and available therapeutic options remain sub-optimal…”
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Introduction of Nonacidic Side Chains on 6-Ethylcholane Scaffolds in the Identification of Potent Bile Acid Receptor Agonists with Improved Pharmacokinetic Properties
Published in Molecules (Basel, Switzerland) (16-03-2019)“…As a cellular bile acid sensor, farnesoid X receptor (FXR) and the membrane G-coupled receptor (GPBAR1) participate in maintaining bile acid, lipid, and…”
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Natural ligands for nuclear receptors: biology and potential therapeutic applications
Published in Current topics in medicinal chemistry (01-03-2012)“…Nuclear receptors are key regulators of various processes including reproduction, development, and metabolism of xeno- and endobiotics. Research in the last…”
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Repositioning Mifepristone as a Leukaemia Inhibitory Factor Receptor Antagonist for the Treatment of Pancreatic Adenocarcinoma
Published in Cells (Basel, Switzerland) (03-11-2022)“…Pancreatic cancer is a leading cause of cancer mortality and is projected to become the second-most common cause of cancer mortality in the next decade. While…”
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Correction to “Discovery of a Novel Class of Dual GPBAR1 Agonists–RORγt Inverse Agonists for the Treatment of IL-17-Mediated Disorders”
Published in ACS omega (28-11-2023)“…[This corrects the article DOI: 10.1021/acsomega.2c07907.]…”
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Navigation in bile acid chemical space: discovery of novel FXR and GPBAR1 ligands
Published in Scientific reports (06-07-2016)“…Bile acids are signaling molecules interacting with nuclear receptors and membrane G-protein-coupled receptors. Among these receptors, the farnesoid X receptor…”
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Thiazolidin-4-one-based compounds interfere with the eicosanoid biosynthesis pathways by mPGES-1/sEH/5-LO multi-target inhibition
Published in European journal of medicinal chemistry reports (01-08-2022)“…Here we report the application of a multi-disciplinary protocol for investigating thiazolidin-4-one-based compounds as new promising anti-inflammatory agents…”
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Targeting Bile Acid Receptors: Discovery of a Potent and Selective Farnesoid X Receptor Agonist as a New Lead in the Pharmacological Approach to Liver Diseases
Published in Frontiers in pharmacology (30-03-2017)“…Bile acid (BA) receptors represent well-defined targets for the development of novel therapeutic approaches to metabolic and inflammatory diseases. In the…”
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Homophymine A, an Anti-HIV Cyclodepsipeptide from the Sponge Homophymia sp
Published in Journal of organic chemistry (18-07-2008)“…A new anti-HIV cyclodepsipeptide, homophymine A, was isolated from a New Caledonian collection of the marine sponge Homophymia sp. The structure of homophymine…”
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Insights on pregnane-X-receptor modulation. Natural and semisynthetic steroids from Theonella marine sponges
Published in European journal of medicinal chemistry (12-02-2014)“…Pregnane-X-receptor (PXR) is a member of nuclear receptors superfamily that activates gene transcription by binding to responsive elements in the promoter of…”
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