0000000000329477

AUTHOR

Vittorio Colantuoni

showing 2 related works from this author

Everolimus as first line therapy for pancreatic neuroendocrine tumours: current knowledge and future perspectives

2017

urpose Everolimus has been shown to be effective for advanced pancreatic neuroendocrine tumours (pNETs), but its positioning in the therapeutic algorithm for pNETs is matter of debate. Methods With the aim to shed light on this point, we performed an up-to-date critical review taking into account the results of both retrospective and prospective published studies, and the recommendations of international guidelines. In addition, we performed an extensive search on the Clinical Trial Registries databases worldwide, to gather information on the ongoing clinical trials related to this specific topic. Results We identified eight retrospective published studies, two prospective published studies…

0301 basic medicinemTOR inhibitorsCancer Researchmedicine.medical_specialtyPathologymTOR inhibitorEverolimus; mTOR inhibitors; Neuroendocrine tumours; Therapy; Antineoplastic Agents; Everolimus; Humans; Neuroendocrine Tumors; Pancreatic Neoplasms; Oncology; Cancer ResearchTherapeutic algorithmEverolimus; mTOR inhibitors; neuroendocrine tumours; therapy; antineoplastic agents; everolimus; humans; neuroendocrine tumours; pancreatic neoplasms; oncology; cancer researchEndocrine SyndromeNeuroendocrine tumorsAntineoplastic Agent03 medical and health sciences0302 clinical medicineFirst line therapyNeuroendocrine tumourantineoplastic agentsmedicinehumansIntensive care medicinetherapyEverolimusbusiness.industryPancreatic Neoplasmpancreatic neoplasmsGeneral Medicineeverolimusmedicine.diseaseDiscovery and development of mTOR inhibitorsClinical trialEverolimuNeuroendocrine Tumors030104 developmental biologyOncology030220 oncology & carcinogenesisneuroendocrine tumoursNeuroendocrine TumorbusinessEverolimus; mTOR inhibitors; Neuroendocrine tumours; Therapy; Antineoplastic Agents; Everolimus; Humans; Neuroendocrine Tumors; Pancreatic NeoplasmsHumanmedicine.drugJournal of Cancer Research and Clinical Oncology
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A compound-based proteomic approach discloses 15-ketoatractyligenin methyl ester as a new PPARγ partial agonist with anti-proliferative ability

2017

AbstractProteomics based approaches are emerging as useful tools to identify the targets of bioactive compounds and elucidate their molecular mechanisms of action. Here, we applied a chemical proteomic strategy to identify the peroxisome proliferator-activated receptor γ (PPARγ) as a molecular target of the pro-apoptotic agent 15-ketoatractyligenin methyl ester (compound 1). We demonstrated that compound 1 interacts with PPARγ, forms a covalent bond with the thiol group of C285 and occupies the sub-pocket between helix H3 and the β-sheet of the ligand-binding domain (LBD) of the receptor by Surface Plasmon Resonance (SPR), mass spectrometry-based studies and docking experiments. 1 displayed…

Transcriptional Activation0301 basic medicinenatural productTime FactorsPeroxisome proliferator-activated receptorApoptosisLigandsPartial agonistArticleRosiglitazonePPAR_gammaJurkat Cells03 medical and health sciencesTransactivation0302 clinical medicineproteomicsHumansBinding siteReceptorMode of actionPI3K/AKT/mTOR pathwayCell Proliferationchemistry.chemical_classificationBinding SitesMultidisciplinaryProtein StabilityProtein Proliferator-Activated-Receptor PPARs Ligand-Binding Domain Chemical Proteomics Accurate Docking Pi3k/Akt Pathway Drug Discovery Anticancer compoundsReproducibility of ResultsEstersSurface Plasmon ResonanceMolecular Docking SimulationPPAR gammaKineticsHEK293 Cells030104 developmental biologychemistryBiochemistryDocking (molecular)030220 oncology & carcinogenesisThermodynamicsThiazolidinedionesproteomics PPAR_gamma natural productDiterpenes KauraneHT29 CellsScientific Reports
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