Search results for "PPARs"
showing 3 items of 3 documents
Anticancer properties of 4-thiazolidinone derivatives depend on peroxisome proliferator-activated receptor gamma (PPARγ)
2017
Peroxisome proliferator-activated receptors (PPARs) play an important role in numerous chronic diseases such as diabetes, obesity, atherosclerosis and cancer, and PPAR modulators are among the approved drugs and drug-candidates for their treatment. The aim of this study was to elucidate the involvement of PPARs in the mechanism of cytotoxic and pro-apoptotic action of novel anticancer 4-thiazolidinone derivatives (Les-2194, Les-3377, Les-3640) and approved 4-thiazolidinones (Rosiglitazone, Pioglitazone) towards the human squamous carcinoma (SCC-15) cell line. Experiments with 4-thiazaolidinone derivatives and PPAR-specific siRNA were conducted and PPARα, PPARβ and PPARγ mRNA expression was …
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…
Crescere/Svilupparsi. Teorie e rappresentazioni fra mondo antico e scienze della vita contemporanee
2020
Il volume raccoglie i contributi scientifici di diversi autori, la maggior parte dei quali avevano presentato le loro relazioni già nell'ambito del Convegno di studi intitolato "Memoria scientiae 2019. Crescere/Svilupparsi" (Palermo, 21-23 febbraio 2019) sulle teorie e rappresentazioni della crescita umana e degli altri organismi viventi nel mondo antico (in particolare greco e romano) e nelle moderne scienze della vita. The volume collects the scientific contributions of various authors, most of whom had presented their reports already in the context of the study conference entitled "Memoria scientiae 2019. Grow / Develop" (Palermo, February 21-23, 2019) on theories and representations of …