2012
ChemInform Abstract: Synthesis and Evaluation of 17α‐E‐20‐(Heteroaryl)norpregn‐1,3,5 (10),20‐tetraene‐3,17β‐diols [17α‐(Heteroaryl)vinyl Estradiols] as Ligands for the Estrogen Receptor‐α Ligand Binding Domain (ERα‐LBD).
Olmsted S, Tongcharoensirikul P, McCaskill E, Gandiaga K, Labaree D, Hochberg R, Hanson R. ChemInform Abstract: Synthesis and Evaluation of 17α‐E‐20‐(Heteroaryl)norpregn‐1,3,5 (10),20‐tetraene‐3,17β‐diols [17α‐(Heteroaryl)vinyl Estradiols] as Ligands for the Estrogen Receptor‐α Ligand Binding Domain (ERα‐LBD). ChemInform 2012, 43: no-no. DOI: 10.1002/chin.201242199.Peer-Reviewed Original Research
2001
Estradiol-16α-carboxylic Acid Esters as Locally Active Estrogens
Labaree D, Reynolds T, Hochberg R. Estradiol-16α-carboxylic Acid Esters as Locally Active Estrogens. Journal Of Medicinal Chemistry 2001, 44: 1802-1814. PMID: 11356114, DOI: 10.1021/jm000523h.Peer-Reviewed Original ResearchMeSH KeywordsAlkaline PhosphataseAnimalsBinding, CompetitiveEnzyme InductionEstersEstradiolEstradiol CongenersEstrogen Receptor alphaEstrogen Receptor betaFemaleHumansIn Vitro TechniquesMiceMicrosomes, LiverOrgan SizeOvariectomyOxidoreductasesRatsRats, Sprague-DawleyReceptors, EstrogenStructure-Activity RelationshipTumor Cells, CulturedUterusVaginaConceptsEstrogenic actionActive estrogensAnalogues of estradiolRat uterine weightEstrogenic potencyEstrogen receptor bindingSystemic estrogenRat hepatic microsomesUterine weightIshikawa cellsVivo modelEstrogenTherapeutic treatmentHepatic microsomesReceptor bindingFluoroethyl esterSystemic actionER affinityHigh ER affinityEstradiolEsterase hydrolysisPotencyDyspareuniaLocal actionMenopause
1999
Regiospecific Esterification of Estrogens by Lecithin:Cholesterol Acyltransferase1
Kanji S, Kuohung W, Labaree D, Hochberg R. Regiospecific Esterification of Estrogens by Lecithin:Cholesterol Acyltransferase1. The Journal Of Clinical Endocrinology & Metabolism 1999, 84: 2481-2488. PMID: 10404824, DOI: 10.1210/jcem.84.7.5755.Peer-Reviewed Original ResearchConceptsLow-density lipoproteinEsterification of estradiolCholesterol acyltransferasePowerful antioxidant actionD-ring structureDensity lipoproteinEstrogenPolar oestrogensEstradiolEstradiol estersAntioxidant actionSteroidsLCAT substrateBloodDifferent steroidsPowerful antioxidantLCATHuman LCATEstriolTissueCholesterolGroup