0000000000141464

AUTHOR

Yves Jacquot

0000-0002-4046-9829

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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Structure elucidation of benzopyran-2-ol in solution and in solid state following the reduction of coumarin by DIBAL-H

2001

Lactols are compounds of increasing interest in the synthesis of active pharmaceutical derivatives. Nevertheless, the product obtained by the reduction of the carbonyl group of coumarin has been described only twice, and without definition of its precise chemical structure. Since these studies, doubts have been raised about the existence of a monomeric or dimeric form. Our study has led us to conclude definitely that the single dimeric form exists and to precisely define the spectral properties of the two diastereoisomers.

chemistry.chemical_classificationchemistry.chemical_compoundchemistryBicyclic moleculeLactolStereochemistryChemical structureAcetalDiastereomerGeneral ChemistryChemical synthesisLactoneBenzopyranComptes Rendus de l'Académie des Sciences - Series IIC - Chemistry
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