0000000000141466

AUTHOR

Guy Laurent

showing 2 related works from this author

ERa dimerization: a key factor for the weak estrogenic activity of an ERa modulator unable to compete with estradiol in binding assays

2016

PMID: 27400858; International audience; AbstractEstrothiazine (ESTZ) is a weak estrogen sharing structural similarities with coumestrol. ESTZ failed to compete with [3H]17β-estradiol ([3H]17β-E2) for binding to the estrogen receptor α (ERα), questioning its ability to interact with the receptor. However, detection by atomic force spectroscopy (AFS) of an ESTZ-induced ERα dimerization has eliminated any remaining doubts. The effect of the compound on the proliferation of ERα-positive and negative breast cancer cells confirmed the requirement of the receptor. The efficiency of ESTZ in MCF-7 cells was weak without any potency to modify the proliferation profile of estradiol and coumestrol. Gro…

0301 basic medicinemedicine.medical_specialtyTranscription Geneticmedicine.drug_class[SDV]Life Sciences [q-bio]ThiazinesEstrogen receptorBreast NeoplasmsPhytoestrogensCoumestrol[ CHIM ] Chemical SciencesBiochemistry[SPI.MAT]Engineering Sciences [physics]/Materials03 medical and health scienceschemistry.chemical_compound0302 clinical medicineInternal medicinemedicineHumans[CHIM]Chemical SciencesBinding site[SPI.NANO]Engineering Sciences [physics]/Micro and nanotechnologies/MicroelectronicsReceptorMolecular BiologyEstrogen receptor beta[SPI.ACOU]Engineering Sciences [physics]/Acoustics [physics.class-ph]Binding Sites[ SDV ] Life Sciences [q-bio]EstradiolSpectrophotometry AtomicEstrogen Receptor alphaCell BiologyCell biologyTranscription Factor AP-1030104 developmental biologyEndocrinologychemistryMechanism of actionEstrogen030220 oncology & carcinogenesisMCF-7 CellsFemalemedicine.symptomDimerizationEstrogen receptor alphaProtein Binding
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Redistribution of CD95, DR4 and DR5 in rafts accounts for the synergistic toxicity of resveratrol and death receptor ligands in colon carcinoma cells.

2004

The natural phytoalexin resveratrol (3, 5, 4'-trihydroxystilbene) exhibits both chemopreventive and antitumor activities through a variety of mechanisms. We have shown previously that resveratrol-induced apoptosis of a human colon cancer cell line involved the redistribution of CD95 (Fas/Apo-1) into lipid rafts. Here, we show that, in colon cancer cells that resist to resveratrol-induced apoptosis, the polyphenol also induces a redistribution of death receptors into lipid rafts. This effect sensitizes these tumor cells to death receptor-mediated apoptosis. In resveratrol-treated cells, tumor necrosis factor (TNF), anti-CD95 antibodies and TNF-related apoptosis-inducing ligand (TRAIL) activa…

Cancer ResearchNystatinTime FactorsApoptosisResveratrolmedicine.disease_causeLigandsReceptors Tumor Necrosis FactorTNF-Related Apoptosis-Inducing Ligandchemistry.chemical_compoundStilbenesReceptorLipid raftCaspaseMembrane GlycoproteinsbiologyFas receptorFlow CytometryLipidsMitochondriaProto-Oncogene Proteins c-bcl-2CaspasesColonic Neoplasmslipids (amino acids peptides and proteins)Tumor necrosis factor alphaSignal Transductionmedicine.medical_specialtyBlotting WesternTransfectionMembrane MicrodomainsInternal medicineCell Line TumorGeneticsmedicineHumansfas ReceptorMolecular BiologyTumor Necrosis Factor-alphaCarcinomaLipid MetabolismAntineoplastic Agents PhytogenicReceptors TNF-Related Apoptosis-Inducing LigandEndocrinologychemistryApoptosisResveratrolCancer researchbiology.proteinCarcinogenesisApoptosis Regulatory ProteinsOncogene
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