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[7α-18F]fluoro-17α-methyl-5α-dihydrotestosterone: a ligand for androgen receptor-mediated imaging of prostate cancer
Garg P, Labaree D, Hoyte R, Hochberg R. [7α-18F]fluoro-17α-methyl-5α-dihydrotestosterone: a ligand for androgen receptor-mediated imaging of prostate cancer. Nuclear Medicine And Biology 2001, 28: 85-90. PMID: 11182568, DOI: 10.1016/s0969-8051(00)00172-4.Peer-Reviewed Original ResearchConceptsProstate cancerAndrogen receptor-dependent mechanismReceptor-mediated imagingReceptor-dependent mechanismProstate of ratsPositron emission tomographySex hormonesAndrogen receptorSteroid receptorsEmission tomographyCancerCarrier-added radiosynthesisReceptorsSteroids bindHigh affinityAndrogensProstateRatsHormoneGlobulin
1999
7α-Iodo and 7α-Fluoro Steroids as Androgen Receptor-Mediated Imaging Agents
Labaree D, Hoyte R, Nazareth L, Weigel N, Hochberg R. 7α-Iodo and 7α-Fluoro Steroids as Androgen Receptor-Mediated Imaging Agents. Journal Of Medicinal Chemistry 1999, 42: 2021-2034. PMID: 10354410, DOI: 10.1021/jm990064o.Peer-Reviewed Original ResearchConceptsAndrogen receptorAndrogen-responsive reporter geneHigh androgenic activityImaging agentReceptor-mediated uptakeDHT 4Rat prostatic cytosolReceptor binding propertiesHigh affinityMale ratsRat prostateAndrogenic activityResponsive reporter geneProstatic cytosolDiagnostic imaging agentsReceptorsHigh binding activitySteroidsIodinated compoundBiological activityDegrees CHigher bindingMetabolic oxidationDHTBiological potency
1998
Iodinated and fluorinated steroid 2′-aryl-[3,2-c] pyrazoles as potential glucocorticoid receptor imaging agents
Hoyte R, Labaree D, Fede J, Harris C, Hochberg R. Iodinated and fluorinated steroid 2′-aryl-[3,2-c] pyrazoles as potential glucocorticoid receptor imaging agents. Steroids 1998, 63: 595-602. PMID: 9830686, DOI: 10.1016/s0039-128x(98)00069-5.Peer-Reviewed Original ResearchConceptsPotent glucocorticoidGlucocorticoid receptorTrihydroxy-16Potential glucocorticoid receptorReceptor imaging agentImaging agentPositron emission tomographyHeLa cell assayGlucocorticoid potencyEmission tomographySteroidsGlucocorticoidsReceptorsCell assayDexamethasoneAlkaline phosphataseSteroids 2PotencyAgentsPara positionBromo analogueBest ligandSide chainsCortivazolFluoro analogue