Search results for "ERα"

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Dibutyl Phthalate (DBP)-Induced Apoptosis and Neurotoxicity are Mediated via the Aryl Hydrocarbon Receptor (AhR) but not by Estrogen Receptor Alpha (…

2016

Dibutyl phthalate (di-n-butyl phthalate, DBP) is one of the most commonly used phthalate esters. DBP is widely used as a plasticizer in a variety of household industries and consumer products. Because phthalates are not chemically bound to products, they can easily leak out to enter the environment. DBP can pass through the placental and blood–brain barriers due to its chemical structure, but little is known about its mechanism of action in neuronal cells. This study demonstrated the toxic and apoptotic effects of DBP in mouse neocortical neurons in primary cultures. DBP stimulated caspase-3 and LDH activities as well as ROS formation in a concentration (10 nM–100 µM) and time-dependent (3–…

0301 basic medicineTime Factorsgenetic structuresPPARγPeroxisome proliferator-activated receptorApoptosis010501 environmental sciencesToxicology01 natural sciencesDBPMicechemistry.chemical_compoundERβReceptorCells CulturedERαCerebral CortexNeuronschemistry.chemical_classificationbiologyCaspase 3General NeurosciencePhthalateDibutyl PhthalatePhthalateOriginal ArticleSignal transductioncirculatory and respiratory physiologymedicine.medical_specialtyCell SurvivalDibutyl phthalateNeuroscience(all)03 medical and health sciencesInternal medicinemedicineAnimalsEstrogen Receptor betaRNA Messengercardiovascular diseasesEstrogen receptor beta0105 earth and related environmental sciencesDose-Response Relationship DrugAhREstrogen Receptor alphaNeuronAryl hydrocarbon receptorPPAR gamma030104 developmental biologyEndocrinologyReceptors Aryl Hydrocarbonchemistrybiology.proteinReactive Oxygen SpeciesEstrogen receptor alphaNeurotoxicity Research
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Switching from Aromatase Inhibitors to Dual Targeting Flavonoid-Based Compounds for Breast Cancer Treatment

2023

Despite the significant outcomes attained by scientific research, breast cancer (BC) still represents the second leading cause of death in women. Estrogen receptor-positive (ER+) BC accounts for the majority of diagnosed BCs, highlighting the disruption of estrogenic signalling as target for first-line treatment. This goal is presently pursued by inhibiting aromatase (AR) enzyme or by modulating Estrogen Receptor (ER) α. An appealing strategy for fighting BC and reducing side effects and resistance issues may lie in the design of multifunctional compounds able to simultaneously target AR and ER. In this paper, previously reported flavonoid-related potent AR inhibitors were suitably modified…

homoisoflavones; aromatase inhibitors; ERα ligands; multitarget; molecular dynamicsOrganic ChemistryPharmaceutical ScienceERα ligandshomoisoflavonesmolecular dynamicsaromatase inhibitorsAnalytical ChemistrySettore CHIM/03 - Chimica Generale E InorganicaChemistry (miscellaneous)Drug DiscoveryMolecular MedicinemultitargetPhysical and Theoretical ChemistryMolecules
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