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
1995
Long-lived testosterone esters in the rat.
Borg W, Shackleton CH, Pahuja SL, Hochberg RB. Long-lived testosterone esters in the rat. Proceedings Of The National Academy Of Sciences Of The United States Of America 1995, 92: 1545-1549. PMID: 7878017, PMCID: PMC42556, DOI: 10.1073/pnas.92.5.1545.Peer-Reviewed Original ResearchConceptsTestosterone estersPresence of testosteronePotent therapeutic agentLong-term castratesFemale ratsMale ratsTestosterone levelsMeasurable fallEster fractionIntact malesSteroid hormonesTherapeutic agentsRatsHormonal potencyTarget tissuesImportant physiological impactAndrogensFatTestosteroneMost tissuesCastrationTissueFatty acidsTestosterone equivalentsPhysiological impactDistribution of occupied and unoccupied estrogen receptors in the rat brain: effects of physiological gonadal steroid exposure
Yuan H, Bowlby D, Brown T, Hochberg R, MacLusky N. Distribution of occupied and unoccupied estrogen receptors in the rat brain: effects of physiological gonadal steroid exposure. Endocrinology 1995, 136: 96-105. DOI: 10.1210/en.136.1.96.Peer-Reviewed Original ResearchGonadal steroid exposureUnoccupied estrogen receptorEstrogen receptorER occupancySteroid exposureLevels of circulating estradiolBed nucleus of the stria terminalisIn vitro autoradiographic methodOccupied estrogen receptorsBrain regionsTreatment of intact malesHypothalamic arcuate nucleusHypothalamic ventromedial nucleusTissue sectionsEndogenous gonadal steroidsPreovulatory estrogen surgeMessenger RNA levelsER binding capacityArcuate nucleusMale ratsBed nucleusVentromedial nucleusCirculating estradiolLabeled estrogenStria terminalis
1992
Estrogen receptors colocalize with low-affinity nerve growth factor receptors in cholinergic neurons of the basal forebrain.
Toran-Allerand CD, Miranda RC, Bentham WD, Sohrabji F, Brown TJ, Hochberg RB, MacLusky NJ. Estrogen receptors colocalize with low-affinity nerve growth factor receptors in cholinergic neurons of the basal forebrain. Proceedings Of The National Academy Of Sciences Of The United States Of America 1992, 89: 4668-4672. PMID: 1316615, PMCID: PMC49144, DOI: 10.1073/pnas.89.10.4668.Peer-Reviewed Original ResearchConceptsLow-affinity nerve growth factor receptorNerve growth factor receptorGrowth factor receptorBasal forebrainCholinergic neuronsSame neuronsFactor receptorCholinergic marker enzyme choline acetyltransferaseGonadal steroid hormone estrogenBrain-derived neurotrophic factorPrimate basal forebrainRodent basal forebrainSteroid hormone estrogenEnzyme choline acetyltransferaseNerve growth factorSitu hybridization histochemistryEstrogen deficiencyNeurotrophic factorNeurotrophin-3Cholinergic functionCholine acetyltransferaseNeuronal survivalHormone estrogenEstrogen receptorClinical conditions
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
1989
The synthesis of 11 beta-methoxy-[16 alpha-123I] iodoestradiol and its interaction with the estrogen receptor in vivo and in vitro.
Zielinski JE, Larner JM, Hoffer PB, Hochberg RB. The synthesis of 11 beta-methoxy-[16 alpha-123I] iodoestradiol and its interaction with the estrogen receptor in vivo and in vitro. Journal Of Nuclear Medicine 1989, 30: 209-15. PMID: 2738649.Peer-Reviewed Original Research
1982
Estradiol fatty acid esters. The isolation and identification of the lipoidal derivative of estradiol synthesized in the bovine uterus.
Mellon-Nussbaum SH, Ponticorvo L, Schatz F, Hochberg RB. Estradiol fatty acid esters. The isolation and identification of the lipoidal derivative of estradiol synthesized in the bovine uterus. Journal Of Biological Chemistry 1982, 257: 5678-5684. PMID: 7068614, DOI: 10.1016/s0021-9258(19)83831-0.Peer-Reviewed Original Research