2004
Estrogen to Antiestrogen with a Single Methylene Group Resulting in an Unusual Steroidal Selective Estrogen Receptor Modulator
Zhang JX, Labaree DC, Mor G, Hochberg RB. Estrogen to Antiestrogen with a Single Methylene Group Resulting in an Unusual Steroidal Selective Estrogen Receptor Modulator. The Journal Of Clinical Endocrinology & Metabolism 2004, 89: 3527-3535. PMID: 15240642, DOI: 10.1210/jc.2003-032005.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBody WeightBone and BonesCell Line, TumorCholesterolDose-Response Relationship, DrugEstradiolEstrogen AntagonistsEstrogen Receptor alphaEstrogen Receptor betaEstrogensFemaleHumansHydrocarbonsMethaneOrgan SizeRatsRats, Sprague-DawleyReceptors, EstrogenSelective Estrogen Receptor ModulatorsTransfectionUterusConceptsSelective estrogen receptor modulatorsEstrogen receptor modulatorsReceptor modulatorsBreast cancer preventionEstradiol-induced proliferationER affinityHigh ER affinityImportant therapeutic agentsPlasma cholesterolER alphaCancer preventionEstrogen agonistEstrogenic agonistTherapeutic agentsEstradiol analogsHigh estrogenic potencyCell bioassayBone growthEstrogenic activityAntiestrogensEstrogenic potencyAgonistsCritical structuresUnique mechanismGroup
2003
Synthesis and Evaluation of B-, C-, and D-Ring-Substituted Estradiol Carboxylic Acid Esters as Locally Active Estrogens
Labaree DC, Zhang JX, Harris HA, O'Connor C, Reynolds TY, Hochberg RB. Synthesis and Evaluation of B-, C-, and D-Ring-Substituted Estradiol Carboxylic Acid Esters as Locally Active Estrogens. Journal Of Medicinal Chemistry 2003, 46: 1886-1904. PMID: 12723952, DOI: 10.1021/jm0204340.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBinding, CompetitiveEsterasesEstersEstradiolEstradiol CongenersEstrogen Receptor alphaEstrogen Receptor betaFemaleHumansIn Vitro TechniquesKidneyLigandsMiceMicrosomesOrgan SizeOxidoreductasesRatsRats, Sprague-DawleyReceptors, EstrogenStructure-Activity RelationshipTumor Cells, CulturedUterusVaginaConceptsEstrogen receptorHormonal activityReceptor bindingAnalogues of estradiolEstrogen-sensitive genesEstrogen receptor bindingEstrogen-responsive genesEstrogenic actionIshikawa cellsEffective estrogenActive estrogensEstrogenHormonal actionDerivatives of estradiolEstradiolEstrogenic responsesSystemic actionReceptorsEstrogenic activityVivo assaysNonspecific esterasesSteroid nucleusSensitive genesActivitySteroid ring
1998
Biological Esterification of Steroids*
Hochberg R. Biological Esterification of Steroids*. Endocrine Reviews 1998, 19: 331-348. PMID: 9626557, DOI: 10.1210/edrv.19.3.0330.Peer-Reviewed Original Research
1990
A Simple and Sensitive Microtiter Plate Estrogen Bioassay Based on Stimulation of Alkaline Phosphatase in Ishikawa Cells: Estrogenic Action of Δ5 Adrenal Steroids*
Littlefield BA, Gurpide E, Markiewicz L, McKinley B, Hochberg RB. A Simple and Sensitive Microtiter Plate Estrogen Bioassay Based on Stimulation of Alkaline Phosphatase in Ishikawa Cells: Estrogenic Action of Δ5 Adrenal Steroids*. Endocrinology 1990, 127: 2757-2762. PMID: 2249627, DOI: 10.1210/endo-127-6-2757.Peer-Reviewed Original ResearchConceptsEstrogenic actionIshikawa cellsHuman endometrial adenocarcinoma cell lineEndometrial adenocarcinoma cell lineAction of estradiolDelta 5Ishikawa human endometrial adenocarcinoma cell lineType of steroidAdenocarcinoma cell lineAdrenal steroidsEstrogen bioassayAdrenal delta 5Aromatase inhibitorsEstrogenC19 steroidsAlkPEstradiolSteroidsDelta 4StimulationAntiestrogensCell linesDehydrogenase inhibitorAlkaline phosphataseAlkaline phosphatase enzyme activity