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John Katzenellenbogen

This is a preview profile on BiomedExperts - the first literature-based scientific social network. It brings the right researchers together and allows them to collaborate online. Collexis and Dell provide the BiomedExperts network of +1.5 Million pre-calculated profiles free of charge to researchers worldwide.

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Waibel Michael; Kieser Karen J; Carlson Kathryn E; Stossi Fabio; Katzenellenbogen Benita S; Katzenellenbogen John A
Phenethyl pyridines with non-polar internal substituents as selective ligands for estrogen receptor beta.
Waibel Michael; De Angelis Meri; Stossi Fabio; Kieser Karen J; Carlson Kathryn E; Katzenellenbogen Benita S; Katzenellenbogen John A
Bibenzyl- and stilbene-core compounds with non-polar linker atom substituents as selective ligands for estrogen receptor beta.
LaFrate Andrew L; Carlson Kathryn E; Katzenellenbogen John A
Steroidal bivalent ligands for the estrogen receptor: design, synthesis, characterization and binding affinities.

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All Publications

2009: Waibel Michael; Kieser Karen J; Carlson Kathryn E; Stossi Fabio; Katzenellenbogen Benita S; Katzenellenbogen John A
Phenethyl pyridines with non-polar internal substituents as selective ligands for estrogen receptor beta.
European journal of medicinal chemistry 2009;44(9):3560-70.
2009: Waibel Michael; De Angelis Meri; Stossi Fabio; Kieser Karen J; Carlson Kathryn E; Katzenellenbogen Benita S; Katzenellenbogen John A
Bibenzyl- and stilbene-core compounds with non-polar linker atom substituents as selective ligands for estrogen receptor beta.
European journal of medicinal chemistry 2009;44(9):3412-24.
2009: LaFrate Andrew L; Carlson Kathryn E; Katzenellenbogen John A
Steroidal bivalent ligands for the estrogen receptor: design, synthesis, characterization and binding affinities.
Bioorganic & medicinal chemistry 2009;17(10):3528-35.
2009: Zhou Dong; Zhou Haibing; Jenks Carl C; Lewis Jason S; Katzenellenbogen John A; Welch Michael J
Bromination from the macroscopic level to the tracer radiochemical level: (76)Br radiolabeling of aromatic compounds via electrophilic substitution.
Bioconjugate chemistry 2009;20(4):808-16.
2009: Jeyakumar M; Katzenellenbogen John A
A dual-acceptor time-resolved Föster resonance energy transfer assay for simultaneous determination of thyroid hormone regulation of corepressor and coactivator binding to the thyroid hormone receptor: Mimicking the cellular context of thyroid hormone action.
Analytical biochemistry 2009;386(1):73-8.
2009: Lee Byung Chul; Dence Carmen S; Zhou Haibing; Parent Ephraim E; Welch Michael J; Katzenellenbogen John A
Fluorine-18 labeling and biodistribution studies on peroxisome proliferator-activated receptor-gamma ligands: potential positron emission tomography imaging agents.
Nuclear medicine and biology 2009;36(2):147-53.
2009: Gunther Jillian R; Du Yuhong; Rhoden Eric; Lewis Iestyn; Revennaugh Brian; Moore Terry W; Kim Sung Hoon; Dingledine Raymond; Fu Haian; Katzenellenbogen John A
A set of time-resolved fluorescence resonance energy transfer assays for the discovery of inhibitors of estrogen receptor-coactivator binding.
Journal of biomolecular screening : the official journal of the Society for Biomolecular Screening 2009;14(2):181-93.
2009: Minutolo Filippo; Bertini Simone; Granchi Carlotta; Marchitiello Teresa; Prota Giovanni; Rapposelli Simona; Tuccinardi Tiziano; Martinelli Adriano; Gunther Jillian R; Carlson Kathryn E; Katzenellenbogen John A; Macchia Marco
Structural evolutions of salicylaldoximes as selective agonists for estrogen receptor beta.
Journal of medicinal chemistry 2009;52(3):858-67.
2009: Dehdashti Farrokh; Mortimer Joanne E; Trinkaus Kathryn; Naughton Michael J; Ellis Matthew; Katzenellenbogen John A; Welch Michael J; Siegel Barry A
PET-based estradiol challenge as a predictive biomarker of response to endocrine therapy in women with estrogen-receptor-positive breast cancer.
Breast cancer research and treatment 2009;113(3):509-17.
2009: Trogden Bridget G; Kim Sung Hoon; Lee Shuyi; Katzenellenbogen John A
Tethered indoles as functionalizable ligands for the estrogen receptor.
Bioorganic & medicinal chemistry letters 2009;19(2):485-8.
2009: Zhou Hai-Bing; Carlson Kathryn E; Stossi Fabio; Katzenellenbogen Benita S; Katzenellenbogen John A
Analogs of methyl-piperidinopyrazole (MPP): antiestrogens with estrogen receptor alpha selective activity.
Bioorganic & medicinal chemistry letters 2009;19(1):108-10.
2008: LaFrate Andrew L; Gunther Jillian R; Carlson Kathryn E; Katzenellenbogen John A
Synthesis and biological evaluation of guanylhydrazone coactivator binding inhibitors for the estrogen receptor.
Bioorganic & medicinal chemistry 2008;16(23):10075-84.
2008: Kim Sung Hoon; Gunther Jillian R; Katzenellenbogen John A
Nonclassical SNAPFL analogue as a Cy5 resonance energy transfer partner.
Organic letters 2008;10(21):4931-4.
2008: Parent Alexander A; Gunther Jillian R; Katzenellenbogen John A
Blocking estrogen signaling after the hormone: pyrimidine-core inhibitors of estrogen receptor-coactivator binding.
Journal of medicinal chemistry 2008;51(20):6512-30.
2008: Madak-Erdogan Zeynep; Kieser Karen J; Kim Sung Hoon; Komm Barry; Katzenellenbogen John A; Katzenellenbogen Benita S
Nuclear and extranuclear pathway inputs in the regulation of global gene expression by estrogen receptors.
Molecular endocrinology (Baltimore, Md.) 2008;22(9):2116-27.
2008: Zhou Dong; Sharp Terry L; Fettig Nicole M; Lee Hsiaoju; Lewis Jason S; Katzenellenbogen John A; Welch Michael J
Evaluation of a bromine-76-labeled progestin 16alpha,17alpha-dioxolane for breast tumor imaging and radiotherapy: in vivo biodistribution and metabolic stability studies.
Nuclear medicine and biology 2008;35(6):655-63.
2008: Alyea Rebecca A; Laurence Stephanie E; Kim Sung H; Katzenellenbogen Benita S; Katzenellenbogen John A; Watson Cheryl S
The roles of membrane estrogen receptor subtypes in modulating dopamine transporters in PC-12 cells.
Journal of neurochemistry 2008;106(4):1525-33.
2008: Jeyakumar M; Webb Paul; Baxter John D; Scanlan Thomas S; Katzenellenbogen John A
Quantification of ligand-regulated nuclear receptor corepressor and coactivator binding, key interactions determining ligand potency and efficacy for the thyroid hormone receptor.
Biochemistry 2008;47(28):7465-76.
2008: Paulmurugan Ramasamy; Tamrazi Anobel; Katzenellenbogen John A; Katzenellenbogen Benita S; Gambhir Sanjiv S
A human estrogen receptor (ER)alpha mutation with differential responsiveness to nonsteroidal ligands: novel approaches for studying mechanism of ER action.
Molecular endocrinology (Baltimore, Md.) 2008;22(7):1552-64.
2008: Parent Ephraim E; Dence Carmen S; Sharp Terry L; Welch Michael J; Katzenellenbogen John A
7alpha-18F-fluoromethyl-dihydrotestosterone and 7alpha-18F-fluoromethyl-nortestosterone: ligands to determine the role of sex hormone-binding globulin for steroidal radiopharmaceuticals.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine 2008;49(6):987-94.
2008: Gunther Jillian R; Moore Terry W; Collins Margaret L; Katzenellenbogen John A
Amphipathic benzenes are designed inhibitors of the estrogen receptor alpha/steroid receptor coactivator interaction.
ACS chemical biology 2008;3(5):282-6.
2008: Chang Edmund C; Charn Tze Howe; Park Sung-Hee; Helferich William G; Komm Barry; Katzenellenbogen John A; Katzenellenbogen Benita S
Estrogen Receptors alpha and beta as determinants of gene expression: influence of ligand, dose, and chromatin binding.
Molecular endocrinology (Baltimore, Md.) 2008;22(5):1032-43.
2008: Nettles Kendall W; Bruning John B; Gil German; Nowak Jason; Sharma Sanjay K; Hahm Johnnie B; Kulp Kristen; Hochberg Richard B; Zhou Haibing; Katzenellenbogen John A; Katzenellenbogen Benita S; Kim Younchang; Joachmiak Andrzej; Greene Geoffrey L
NFkappaB selectivity of estrogen receptor ligands revealed by comparative crystallographic analyses.
Nature chemical biology 2008;4(4):241-7.
2008: Minutolo Filippo; Bellini Rosalba; Bertini Simone; Carboni Isabella; Lapucci Annalina; Pistolesi Letizia; Prota Giovanni; Rapposelli Simona; Solati Francesca; Tuccinardi Tiziano; Martinelli Adriano; Stossi Fabio; Carlson Kathryn E; Katzenellenbogen Benita S; Katzenellenbogen John A; Macchia Marco
Monoaryl-substituted salicylaldoximes as ligands for estrogen receptor beta.
Journal of medicinal chemistry 2008;51(5):1344-51.
2008: Kim Dong Wook; Jeong Hwan-Jeong; Lim Seok Tae; Sohn Myung-Hee; Katzenellenbogen John A; Chi Dae Yoon
Facile nucleophilic fluorination reactions using tert-alcohols as a reaction medium: significantly enhanced reactivity of alkali metal fluorides and improved selectivity.
The Journal of organic chemistry 2008;73(3):957-62.
2008: Seo Jai Woong; Kim Hee Jun; Lee Byoung Se; Katzenellenbogen John A; Chi Dae Yoon
Convenient one-pot synthesis of 2,2-bis-(4-hydroxyphenyl)-cyclopentanone.
The Journal of organic chemistry 2008;73(2):715-8.
2007: Kim Sung Hoon; Jeyakumar M; Katzenellenbogen John A
Dual-mode fluorophore-doped nickel nitrilotriacetic acid-modified silica nanoparticles combine histidine-tagged protein purification with site-specific fluorophore labeling.
Journal of the American Chemical Society 2007;129(43):13254-64.
2007: LaFrate Andrew L; Katzenellenbogen John A
Improved chemical syntheses of 5,6-dihydro-5-fluorouracil.
The Journal of organic chemistry 2007;72(22):8573-6.
2007: Zhou Hai-Bing; Collins Margaret L; Gunther Jillian R; Comninos John S; Katzenellenbogen John A
Bicyclo[2.2.2]octanes: close structural mimics of the nuclear receptor-binding motif of steroid receptor coactivators.
Bioorganic & medicinal chemistry letters 2007;17(15):4118-22.
2007: Parent Ephraim E; Carlson Kathryn E; Katzenellenbogen John A
Synthesis of 7alpha-(fluoromethyl)dihydrotestosterone and 7alpha-(fluoromethyl)nortestosterone, structurally paired androgens designed to probe the role of sex hormone binding globulin in imaging androgen receptors in prostate tumors by positron emission tomography.
The Journal of organic chemistry 2007;72(15):5546-54.
2007: Zhou Hai-Bing; Nettles Kendall W; Bruning John B; Kim Younchang; Joachimiak Andrzej; Sharma Sanjay; Carlson Kathryn E; Stossi Fabio; Katzenellenbogen Benita S; Greene Geoffrey L; Katzenellenbogen John A
Elemental isomerism: a boron-nitrogen surrogate for a carbon-carbon double bond increases the chemical diversity of estrogen receptor ligands.
Chemistry & biology 2007;14(6):659-69.
2007: Seo Jai Woong; Chi Dae Yoon; Dence Carmen S; Welch Michael J; Katzenellenbogen John A
Synthesis and biodistribution of fluorine-18-labeled fluorocyclofenils for imaging the estrogen receptor.
Nuclear medicine and biology 2007;34(4):383-90.
2007: Parent Ephraim E; Dence Carmen S; Jenks Carl; Sharp Terry L; Welch Michael J; Katzenellenbogen John A
Synthesis and biological evaluation of [18F]bicalutamide, 4-[76Br]bromobicalutamide, and 4-[76Br]bromo-thiobicalutamide as non-steroidal androgens for prostate cancer imaging.
Journal of medicinal chemistry 2007;50(5):1028-40.
2007: Lee Byung Chul; Lee Kyo Chul; Lee Hsiaoju; Mach Robert H; Katzenellenbogen John A
Strategies for the labeling of halogen-substituted peroxisome proliferator-activated receptor gamma ligands: potential positron emission tomography and single photon emission computed tomography imaging agents.
Bioconjugate chemistry 2007;18(2):514-23.
2007: Lee Byung Chul; Lee Kyo Chul; Lee Hsiaoju; Mach Robert H; Katzenellenbogen John A
Synthesis and binding affinity of a fluorine-substituted peroxisome proliferator-activated gamma (PPARgamma) ligand as a potential positron emission tomography (PET) imaging agent.
Bioconjugate chemistry 2007;18(2):507-13.
2007: Zhou Hai-Bing; Sheng Shubin; Compton Dennis R; Kim Younchang; Joachimiak Andrzej; Sharma Sanjay; Carlson Kathryn E; Katzenellenbogen Benita S; Nettles Kendall W; Greene Geoffrey L; Katzenellenbogen John A
Structure-guided optimization of estrogen receptor binding affinity and antagonist potency of pyrazolopyrimidines with basic side chains.
Journal of medicinal chemistry 2007;50(2):399-403.
2006: Likhite Varsha S; Stossi Fabio; Kim Kyuri; Katzenellenbogen Benita S; Katzenellenbogen John A
Kinase-specific phosphorylation of the estrogen receptor changes receptor interactions with ligand, deoxyribonucleic acid, and coregulators associated with alterations in estrogen and tamoxifen activity.
Molecular endocrinology (Baltimore, Md.) 2006;20(12):3120-32.
2006: Kim Sung Hoon; Katzenellenbogen John A
Hormone-PAMAM dendrimer conjugates: polymer dynamics and tether structure affect ligand access to receptors.
Angewandte Chemie (International ed. in English) 2006;45(43):7243-8.
2006: Parent Ephraim E; Jenks Carl; Sharp Terry; Welch Michael J; Katzenellenbogen John A
Synthesis and biological evaluation of a nonsteroidal bromine-76-labeled androgen receptor ligand 3-[76Br]bromo-hydroxyflutamide.
Nuclear medicine and biology 2006;33(6):705-13.
2006: Zhou Dong; Carlson Kathryn E; Katzenellenbogen John A; Welch Michael J
Bromine- and iodine-substituted 16alpha,17alpha-dioxolane progestins for breast tumor imaging and radiotherapy: synthesis and receptor binding affinity.
Journal of medicinal chemistry 2006;49(15):4737-44.
2006: Parent Ephraim E; Dence Carmen S; Sharp Terry L; Welch Michael J; Katzenellenbogen John A
Synthesis and biological evaluation of a fluorine-18-labeled nonsteroidal androgen receptor antagonist, N-(3-[18F]fluoro-4-nitronaphthyl)-cis-5-norbornene-endo-2,3-dicarboxylic imide.
Nuclear medicine and biology 2006;33(5):615-24.
2006: Stossi Fabio; Likhite Varsha S; Katzenellenbogen John A; Katzenellenbogen Benita S
Estrogen-occupied estrogen receptor represses cyclin G2 gene expression and recruits a repressor complex at the cyclin G2 promoter.
The Journal of biological chemistry 2006;281(24):16272-8.
2006: Seo Jai Woong; Comninos John S; Chi Dae Yoon; Kim Dong Wook; Carlson Kathryn E; Katzenellenbogen John A
Fluorine-substituted cyclofenil derivatives as estrogen receptor ligands: synthesis and structure-affinity relationship study of potential positron emission tomography agents for imaging estrogen receptors in breast cancer.
Journal of medicinal chemistry 2006;49(8):2496-511.
2005: De Angelis Meri; Stossi Fabio; Waibel Michael; Katzenellenbogen Benita S; Katzenellenbogen John A
Isocoumarins as estrogen receptor beta selective ligands: Isomers of isoflavone phytoestrogens and their metabolites.
Bioorganic & medicinal chemistry 2005;13(23):6529-42.
2005: Zhou Hai-Bing; Comninos John S; Stossi Fabio; Katzenellenbogen Benita S; Katzenellenbogen John A
Synthesis and evaluation of estrogen receptor ligands with bridged oxabicyclic cores containing a diarylethylene motif: estrogen antagonists of unusual structure.
Journal of medicinal chemistry 2005;48(23):7261-74.
2005: Yoo Jeongsoo; Dence Carmen S; Sharp Terry L; Katzenellenbogen John A; Welch Michael J
Synthesis of an estrogen receptor beta-selective radioligand: 5-[18F]fluoro-(2R,3S)-2,3-bis(4-hydroxyphenyl)pentanenitrile and comparison of in vivo distribution with 16alpha-[18F]fluoro-17beta-estradiol.
Journal of medicinal chemistry 2005;48(20):6366-78.
2005: Katzenellenbogen John A
Designing effective hybrid toxins.
Chemistry & biology 2005;12(7):719-21.
2005: Tamrazi Anobel; Carlson Kathryn E; Rodriguez Alice L; Katzenellenbogen John A
Coactivator proteins as determinants of estrogen receptor structure and function: spectroscopic evidence for a novel coactivator-stabilized receptor conformation.
Molecular endocrinology (Baltimore, Md.) 2005;19(6):1516-28.
2005: Chockalingam Karuppiah; Chen Zhilei; Katzenellenbogen John A; Zhao Huimin
Directed evolution of specific receptor-ligand pairs for use in the creation of gene switches.
Proceedings of the National Academy of Sciences of the United States of America 2005;102(16):5691-6.
2005: Bigott Heather M; Parent Ephraim; Luyt Leonard G; Katzenellenbogen John A; Welch Michael J
Design and synthesis of functionalized cyclopentadienyl tricarbonylmetal complexes for technetium-94m PET imaging of estrogen receptors.
Bioconjugate chemistry 2005;16(2):255-64.
2005: Kim Sung Hoon; Tamrazi Anobel; Carlson Kathryn E; Katzenellenbogen John A
A proteomic microarray approach for exploring ligand-initiated nuclear hormone receptor pharmacology, receptor selectivity, and heterodimer functionality.
Molecular & cellular proteomics : MCP 2005;4(3):267-77.
2005: De Angelis Meri; Stossi Fabio; Carlson Kathryn A; Katzenellenbogen Benita S; Katzenellenbogen John A
Indazole estrogens: highly selective ligands for the estrogen receptor beta.
Journal of medicinal chemistry 2005;48(4):1132-44.
2004: De Angelis Meri; Katzenellenbogen John A
Ring nitrogen-substituted non-steroidal estrogens: pyridine and pyrimidine analogs of the phenol in deoxyhexestrol experience resonance constraints on preferred ligand conformation.
Bioorganic & medicinal chemistry letters 2004;14(23):5835-9.
2004: Compton Dennis R; Sheng Shubin; Carlson Kathryn E; Rebacz Natalie A; Lee In Young; Katzenellenbogen Benita S; Katzenellenbogen John A
Pyrazolo[1,5-a]pyrimidines: estrogen receptor ligands possessing estrogen receptor beta antagonist activity.
Journal of medicinal chemistry 2004;47(24):5872-93.
2004: Compton Dennis R; Carlson Kathryn E; Katzenellenbogen John A
Pyrazolo[1,5-a]pyrimidines as estrogen receptor ligands: defining the orientation of a novel heterocyclic core.
Bioorganic & medicinal chemistry letters 2004;14(22):5681-4.
2004: Selvaraj Vimal; Zakroczymski Melissa A; Naaz Afia; Mukai Motoko; Ju Young H; Doerge Daniel R; Katzenellenbogen John A; Helferich William G; Cooke Paul S
Estrogenicity of the isoflavone metabolite equol on reproductive and non-reproductive organs in mice.
Biology of reproduction 2004;71(3):966-72.
2004: Kim Sung Hoon; Tamrazi Anobel; Carlson Kathryn E; Daniels Jonathan R; Lee In Young; Katzenellenbogen John A
Estrogen receptor microarrays: subtype-selective ligand binding.
Journal of the American Chemical Society 2004;126(15):4754-5.
2004: Muthyala Rajeev S; Ju Young H; Sheng Shubin; Williams Lee D; Doerge Daniel R; Katzenellenbogen Benita S; Helferich William G; Katzenellenbogen John A
Equol, a natural estrogenic metabolite from soy isoflavones: convenient preparation and resolution of R- and S-equols and their differing binding and biological activity through estrogen receptors alpha and beta.
Bioorganic & medicinal chemistry 2004;12(6):1559-67.
2004: Nettles Kendall W; Sun Jun; Radek James T; Sheng Shubin; Rodriguez Alice L; Katzenellenbogen John A; Katzenellenbogen Benita S; Greene Geoffrey L
Allosteric control of ligand selectivity between estrogen receptors alpha and beta: implications for other nuclear receptors.
Molecular cell 2004;13(3):317-27.
2004: Hurth Kyle M; Nilges Mark J; Carlson Kathryn E; Tamrazi Anobel; Belford R Linn; Katzenellenbogen John A
Ligand-induced changes in estrogen receptor conformation as measured by site-directed spin labeling.
Biochemistry 2004;43(7):1891-907.
2004: Rodriguez Alice L; Tamrazi Anobel; Collins Margaret L; Katzenellenbogen John A
Design, synthesis, and in vitro biological evaluation of small molecule inhibitors of estrogen receptor alpha coactivator binding.
Journal of medicinal chemistry 2004;47(3):600-11.
2003: Muthyala Rajeev S; Carlson Kathryn E; Katzenellenbogen John A
Exploration of the bicyclo[3.3.1]nonane system as a template for the development of new ligands for the estrogen receptor.
Bioorganic & medicinal chemistry letters 2003;13(24):4485-8.
2003: Tamrazi Anobel; Carlson Kathryn E; Katzenellenbogen John A
Molecular sensors of estrogen receptor conformations and dynamics.
Molecular endocrinology (Baltimore, Md.) 2003;17(12):2593-602.
2003: Luyt Leonard G; Bigott Heather M; Welch Michael J; Katzenellenbogen John A
7alpha- and 17alpha-substituted estrogens containing tridentate tricarbonyl rhenium/technetium complexes: synthesis of estrogen receptor imaging agents and evaluation using microPET with technetium-94m.
Bioorganic & medicinal chemistry 2003;11(23):4977-89.
2003: Harrington William R; Sheng Shubin; Barnett Daniel H; Petz Larry N; Katzenellenbogen John A; Katzenellenbogen Benita S
Activities of estrogen receptor alpha- and beta-selective ligands at diverse estrogen responsive gene sites mediating transactivation or transrepression.
Molecular and cellular endocrinology 2003;206(1-2):13-22.
2003: Lee Kyo Chul; Moon Byung Seok; Lee Jae Hak; Chung Kyoo-Hyun; Katzenellenbogen John A; Chi Dae Yoon
Synthesis and binding affinities of fluoroalkylated raloxifenes.
Bioorganic & medicinal chemistry 2003;11(17):3649-58.
2003: Vijaykumar Dange; Al-Qahtani Mohammed H; Welch Michael J; Katzenellenbogen John A
Synthesis and biological evaluation of a fluorine-18 labeled estrogen receptor-alpha selective ligand: [18F] propyl pyrazole triol.
Nuclear medicine and biology 2003;30(4):397-404.
2003: Muthyala Rajeev S; Sheng Shubin; Carlson Kathryn E; Katzenellenbogen Benita S; Katzenellenbogen John A
Bridged bicyclic cores containing a 1,1-diarylethylene motif are high-affinity subtype-selective ligands for the estrogen receptor.
Journal of medicinal chemistry 2003;46(9):1589-602.
2003: Wüst Frank; Carlson Kathryn E; Katzenellenbogen John A
Synthesis of novel arylpyrazolo corticosteroids as potential ligands for imaging brain glucocorticoid receptors.
Steroids 2003;68(2):177-91.
2003: Sun Jun; Baudry Jerome; Katzenellenbogen John A; Katzenellenbogen Benita S
Molecular basis for the subtype discrimination of the estrogen receptor-beta-selective ligand, diarylpropionitrile.
Molecular endocrinology (Baltimore, Md.) 2003;17(2):247-58.
2003: Ghosh Usha; Ganessunker Deshanie; Sattigeri Viswajanani J; Carlson Kathryn E; Mortensen Deborah J; Katzenellenbogen Benita S; Katzenellenbogen John A
Estrogenic diazenes: heterocyclic non-steroidal estrogens of unusual structure with selectivity for estrogen receptor subtypes.
Bioorganic & medicinal chemistry 2003;11(4):629-57.
2003: Tamrazi Anobel; Katzenellenbogen John A
Site-specific fluorescent labeling of estrogen receptors and structure-activity relationships of ligands in terms of receptor dimer stability.
Methods in enzymology 2003;364():37-53.
2002: Tamrazi Anobel; Carlson Kathryn E; Daniels Jonathan R; Hurth Kyle M; Katzenellenbogen John A
Estrogen receptor dimerization: ligand binding regulates dimer affinity and dimer dissociation rate.
Molecular endocrinology (Baltimore, Md.) 2002;16(12):2706-19.
2002: Luyt Leonard G; Katzenellenbogen John A
A trithiolate tripodal bifunctional ligand for the radiolabeling of peptides with gallium(III).
Bioconjugate chemistry 2002;13(5):1140-5.
2002: Vijaykumar Dange; Mao Wang; Kirschbaum Karen S; Katzenellenbogen John A
An efficient route for the preparation of a 21-fluoro progestin-16 alpha,17 alpha-dioxolane, a high-affinity ligand for PET imaging of the progesterone receptor.
The Journal of organic chemistry 2002;67(14):4904-10.
2002: Shiau Andrew K; Barstad Danielle; Radek James T; Meyers Marvin J; Nettles Kendall W; Katzenellenbogen Benita S; Katzenellenbogen John A; Agard David A; Greene Geoffrey L
Structural characterization of a subtype-selective ligand reveals a novel mode of estrogen receptor antagonism.
Nature structural biology 2002;9(5):359-64.
2002: Mull Eric S; Sattigeri Viswajanani J; Rodriguez Alice L; Katzenellenbogen John A
Aryl cyclopentadienyl tricarbonyl rhenium complexes: novel ligands for the estrogen receptor with potential use as estrogen radiopharmaceuticals.
Bioorganic & medicinal chemistry 2002;10(5):1381-98.
2002: Nishiguchi Gisele A; Rodriguez Alice L; Katzenellenbogen John A
Diaryl-dialkyl-substituted pyrazoles: regioselective synthesis and binding affinity for the estrogen receptor.
Bioorganic & medicinal chemistry letters 2002;12(6):947-50.
2002: Katzenellenbogen Benita S; Katzenellenbogen John A
Biomedicine. Defining the "S" in SERMs.
Science (New York, N.Y.) 2002;295(5564):2380-1.
2002: Sun Jun; Huang Ying R; Harrington William R; Sheng Shubin; Katzenellenbogen John A; Katzenellenbogen Benita S
Antagonists selective for estrogen receptor alpha.
Endocrinology 2002;143(3):941-7.
2002: Cesati Richard R; Tamagnan Gilles; Baldwin Ronald M; Zoghbi Sami S; Innis Robert B; Kula Nora S; Baldessarini Ross J; Katzenellenbogen John A
Synthesis of cyclopentadienyltricarbonyl rhenium phenyltropanes by double ligand transfer: organometallic ligands for the dopamine transporter.
Bioconjugate chemistry 2002;13(1):29-39.
2001: Katzenellenbogen B S; Sun J; Harrington W R; Kraichely D M; Ganessunker D; Katzenellenbogen J A
Structure-function relationships in estrogen receptors and the characterization of novel selective estrogen receptor modulators with unique pharmacological profiles.
Annals of the New York Academy of Sciences 2001;949():6-15.
2001: Meyers M J; Sun J; Carlson K E; Marriner G A; Katzenellenbogen B S; Katzenellenbogen J A
Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues.
Journal of medicinal chemistry 2001;44(24):4230-51.
2001: Mortensen D S; Rodriguez A L; Carlson K E; Sun J; Katzenellenbogen B S; Katzenellenbogen J A
Synthesis and biological evaluation of a novel series of furans: ligands selective for estrogen receptor alpha.
Journal of medicinal chemistry 2001;44(23):3838-48.
2001: Mortensen D S; Rodriguez A L; Sun J; Katzenellenbogen B S; Katzenellenbogen J A
Furans with basic side chains: synthesis and biological evaluation of a novel series of antagonists with selectivity for the estrogen receptor alpha.
Bioorganic & medicinal chemistry letters 2001;11(18):2521-4.
2001: Tedesco R; Youngman M K; Wilson S R; Katzenellenbogen J A
Synthesis and evaluation of hexahydrochrysene and tetrahydrobenzofluorene ligands for the estrogen receptor.
Bioorganic & medicinal chemistry letters 2001;11(10):1281-4.
2001: Kim S H; Jonson S D; Welch M J; Katzenellenbogen J A
Fluorine-substituted ligands for the peroxisome proliferator-activated receptor gamma (PPARgamma): potential imaging agents for metastatic tumors.
Bioconjugate chemistry 2001;12(3):439-50.
2001: Tedesco R; Thomas J A; Katzenellenbogen B S; Katzenellenbogen J A
The estrogen receptor: a structure-based approach to the design of new specific hormone-receptor combinations.
Chemistry & biology 2001;8(3):277-87.
2001: Stauffer S R; Huang Y R; Aron Z D; Coletta C J; Sun J; Katzenellenbogen B S; Katzenellenbogen J A
Triarylpyrazoles with basic side chains: development of pyrazole-based estrogen receptor antagonists.
Bioorganic & medicinal chemistry 2001;9(1):151-61.
2001: Stauffer S R; Huang Y; Coletta C J; Tedesco R; Katzenellenbogen J A
Estrogen pyrazoles: defining the pyrazole core structure and the orientation of substituents in the ligand binding pocket of the estrogen receptor.
Bioorganic & medicinal chemistry 2001;9(1):141-50.
2000: Stauffer S R; Coletta C J; Tedesco R; Nishiguchi G; Carlson K; Sun J; Katzenellenbogen B S; Katzenellenbogen J A
Pyrazole ligands: structure-affinity/activity relationships and estrogen receptor-alpha-selective agonists.
Journal of medicinal chemistry 2000;43(26):4934-47.
2000: Katzenellenbogen B S; Choi I; Delage-Mourroux R; Ediger T R; Martini P G; Montano M; Sun J; Weis K; Katzenellenbogen J A
Molecular mechanisms of estrogen action: selective ligands and receptor pharmacology.
The Journal of steroid biochemistry and molecular biology 2000;74(5):279-85.
2000: Cesati R R; Katzenellenbogen J A
Preparation of hexahydrobenzo[f]isoquinolines using a vinylogous pictet-spengler cyclization.
Organic letters 2000;2(23):3635-8.
2000: Ju Y H; Carlson K E; Sun J; Pathak D; Katzenellenbogen B S; Katzenellenbogen J A; Helferich W G
Estrogenic effects of extracts from cabbage, fermented cabbage, and acidified brussels sprouts on growth and gene expression of estrogen-dependent human breast cancer (MCF-7) cells.
Journal of agricultural and food chemistry 2000;48(10):4628-34.
2000: Kraichely D M; Sun J; Katzenellenbogen J A; Katzenellenbogen B S
Conformational changes and coactivator recruitment by novel ligands for estrogen receptor-alpha and estrogen receptor-beta: correlations with biological character and distinct differences among SRC coactivator family members.
Endocrinology 2000;141(10):3534-45.
2000: Huang Y R; Katzenellenbogen J A
Regioselective synthesis of 1,3,5-triaryl-4-alkylpyrazoles: novel ligands for the estrogen receptor.
Organic letters 2000;2(18):2833-6.
2000: Stauffer S R; Katzenellenbogen J A
Solid-phase synthesis of tetrasubstituted pyrazoles, novel ligands for the estrogen receptor.
Journal of combinatorial chemistry 2000;2(4):318-29.
2000: Stauffer S R; Sun J; Katzenellenbogen B S; Katzenellenbogen J A
Acyclic amides as estrogen receptor ligands: synthesis, binding, activity and receptor interaction.
Bioorganic & medicinal chemistry 2000;8(6):1293-316.
2000: Skaddan M B; Wüst F R; Jonson S; Syhre R; Welch M J; Spies H; Katzenellenbogen J A
Radiochemical synthesis and tissue distribution of Tc-99m-labeled 7alpha-substituted estradiol complexes.
Nuclear medicine and biology 2000;27(3):269-78.
2000: Kim S H; Katzenellenbogen J A
Triarylethylene bisphenols with a novel cycle are ligands for the estrogen receptor.
Bioorganic & medicinal chemistry 2000;8(4):785-93.
2000: Katzenellenbogen B S; Katzenellenbogen J A
Estrogen receptor transcription and transactivation: Estrogen receptor alpha and estrogen receptor beta: regulation by selective estrogen receptor modulators and importance in breast cancer.
Breast cancer research : BCR 2000;2(5):335-44.
2000: Katzenellenbogen B S; Montano M M; Ediger T R; Sun J; Ekena K; Lazennec G; Martini P G; McInerney E M; Delage-Mourroux R; Weis K; Katzenellenbogen J A
Estrogen receptors: selective ligands, partners, and distinctive pharmacology.
Recent progress in hormone research 2000;55():163-93; discussion 194-5.
1999: Gee A C; Carlson K E; Martini P G; Katzenellenbogen B S; Katzenellenbogen J A
Coactivator peptides have a differential stabilizing effect on the binding of estrogens and antiestrogens with the estrogen receptor.
Molecular endocrinology (Baltimore, Md.) 1999;13(11):1912-23.
1999: Wüst F; Skaddan M B; Leibnitz P; Spies H; Katzenellenbogen J A; Johannsen B
Synthesis of novel progestin-rhenium conjugates as potential ligands for the progesterone receptor.
Bioorganic & medicinal chemistry 1999;7(9):1827-35.
1999: Meyers M J; Sun J; Carlson K E; Katzenellenbogen B S; Katzenellenbogen J A
Estrogen receptor subtype-selective ligands: asymmetric synthesis and biological evaluation of cis- and trans-5,11-dialkyl- 5,6,11, 12-tetrahydrochrysenes.
Journal of medicinal chemistry 1999;42(13):2456-68.
1999: Fink B E; Mortensen D S; Stauffer S R; Aron Z D; Katzenellenbogen J A
Novel structural templates for estrogen-receptor ligands and prospects for combinatorial synthesis of estrogens.
Chemistry & biology 1999;6(4):205-19.
1999: Sun J; Meyers M J; Fink B E; Rajendran R; Katzenellenbogen J A; Katzenellenbogen B S
Novel ligands that function as selective estrogens or antiestrogens for estrogen receptor-alpha or estrogen receptor-beta.
Endocrinology 1999;140(2):800-4.
1999: Jonson S D; Bonasera T A; Dehdashti F; Cristel M E; Katzenellenbogen J A; Welch M J
Comparative breast tumor imaging and comparative in vitro metabolism of 16alpha-[18F]fluoroestradiol-17beta and 16beta-[18F]fluoromoxestrol in isolated hepatocytes.
Nuclear medicine and biology 1999;26(1):123-30.
1999: Spradau T W; Edwards W B; Anderson C J; Welch M J; Katzenellenbogen J A
Synthesis and biological evaluation of Tc-99m-cyclopentadienyltricarbonyltechnetium-labeled octreotide.
Nuclear medicine and biology 1999;26(1):1-7.
1999: Skaddan M B; Katzenellenbogen J A
Integrated "3+1" oxorhenium(V) complexes as estrogen mimics.
Bioconjugate chemistry 1999;10(1):119-29.
1998: Meyers M J; Carlson K E; Katzenellenbogen J A
Facile synthesis of high affinity styrylpyridine systems as inherently fluorescent ligands for the estrogen receptor.
Bioorganic & medicinal chemistry letters 1998;8(24):3589-94.
1998: Wüst F; Carlson K E; Katzenellenbogen J A; Spies H; Johannsen B
Synthesis and binding affinities of new 17 alpha-substituted estradiol-rhenium "n + 1" mixed-ligand and thioether-carbonyl complexes.
Steroids 1998;63(12):665-71.
1998: Spradau T W; Katzenellenbogen J A
Ligands for the estrogen receptor, containing cyclopentadienyltricarbonylrhenium units.
Bioorganic & medicinal chemistry letters 1998;8(22):3235-40.
1998: Spradau T W; Katzenellenbogen J A
Protein and peptide labeling with (cyclopentadienyl)tricarbonyl rhenium and technetium.
Bioconjugate chemistry 1998;9(6):765-72.
1998: Jonson S D; d'Avignon D A; Katzenellenbogen J A; Welch M J
Methyl hypofluorite in the synthesis of 16-methoxyestradiol stereoisomers.
Steroids 1998;63(9):470-8.
1998: Ekena K; Katzenellenbogen J A; Katzenellenbogen B S
Determinants of ligand specificity of estrogen receptor-alpha: estrogen versus androgen discrimination.
The Journal of biological chemistry 1998;273(2):693-9.
1997: Carlson K E; Choi I; Gee A; Katzenellenbogen B S; Katzenellenbogen J A
Altered ligand binding properties and enhanced stability of a constitutively active estrogen receptor: evidence that an open pocket conformation is required for ligand interaction.
Biochemistry 1997;36(48):14897-905.
1997: Hom R K; Katzenellenbogen J A
Technetium-99m-labeled receptor-specific small-molecule radiopharmaceuticals: recent developments and encouraging results.
Nuclear medicine and biology 1997;24(6):485-98.
1997: Katzenellenbogen J A; Welch M J; Dehdashti F
The development of estrogen and progestin radiopharmaceuticals for imaging breast cancer.
Anticancer research 1997;17(3B):1573-6.
1997: Bonasera T A; Jonson S D; Pajeau T S; Katzenellenbogen J A; Welch M J
Retardation of 17-oxidation of 16 alpha-[18F]fluoroestradiol-17 beta by substitution of deuterium for hydrogen in the 17 alpha position(6).
Nuclear medicine and biology 1997;24(3):239-49.
1997: Scribner A W; Jonson S D; Welch M J; Katzenellenbogen J A
Synthesis, estrogen receptor binding, and tissue distribution of [18F]fluorodoisynolic acids.
Nuclear medicine and biology 1997;24(3):209-24.
1997: Ekena K; Weis K E; Katzenellenbogen J A; Katzenellenbogen B S
Different residues of the human estrogen receptor are involved in the recognition of structurally diverse estrogens and antiestrogens.
The Journal of biological chemistry 1997;272(8):5069-75.
1996: Kym P R; Hummert K L; Nilsson A G; Lubin M; Katzenellenbogen J A
Bisphenolic compounds that enhance cell cation transport are found in commercial phenol red.
Journal of medicinal chemistry 1996;39(25):4897-904.
1996: Ekena K; Weis K E; Katzenellenbogen J A; Katzenellenbogen B S
Identification of amino acids in the hormone binding domain of the human estrogen receptor important in estrogen binding.
The Journal of biological chemistry 1996;271(33):20053-9.
1996: Mortimer J E; Dehdashti F; Siegel B A; Katzenellenbogen J A; Fracasso P; Welch M J
Positron emission tomography with 2-[18F]Fluoro-2-deoxy-D-glucose and 16alpha-[18F]fluoro-17beta-estradiol in breast cancer: correlation with estrogen receptor status and response to systemic therapy.
Clinical cancer research : an official journal of the American Association for Cancer Research 1996;2(6):933-9.
1996: Bonasera T A; O'Neil J P; Xu M; Dobkin J A; Cutler P D; Lich L L; Choe Y S; Katzenellenbogen J A; Welch M J
Preclinical evaluation of fluorine-18-labeled androgen receptor ligands in baboons.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine 1996;37(6):1009-15.
1996: Dence C S; Napolitano E; Katzenellenbogen J A; Welch M J
Carbon-11-labeled estrogens as potential imaging agents for breast tumors.
Nuclear medicine and biology 1996;23(4):491-6.
1996: Katzenellenbogen J A; O'Malley B W; Katzenellenbogen B S
Tripartite steroid hormone receptor pharmacology: interaction with multiple effector sites as a basis for the cell- and promoter-specific action of these hormones.
Molecular endocrinology (Baltimore, Md.) 1996;10(2):119-31.
1995: Dehdashti F; Mortimer J E; Siegel B A; Griffeth L K; Bonasera T J; Fusselman M J; Detert D D; Cutler P D; Katzenellenbogen J A; Welch M J
Positron tomographic assessment of estrogen receptors in breast cancer: comparison with FDG-PET and in vitro receptor assays.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine 1995;36(10):1766-74.
1995: Seielstad D A; Carlson K E; Kushner P J; Greene G L; Katzenellenbogen J A
Analysis of the structural core of the human estrogen receptor ligand binding domain by selective proteolysis/mass spectrometric analysis.
Biochemistry 1995;34(39):12605-15.
1995: Katzenellenbogen J A; Coleman R E; Hawkins R A; Krohn K A; Larson S M; Mendelsohn J; Osborne C K; Piwnica-Worms D; Reba R C; Siegel B A
Tumor receptor imaging: proceedings of the National Cancer Institute workshop, review of current work, and prospective for further investigations.
Clinical cancer research : an official journal of the American Association for Cancer Research 1995;1(8):921-32.
1995: Napolitano E; Fiaschi R; Carlson K E; Katzenellenbogen J A
11 beta-substituted estradiol derivatives. 2. Potential carbon-11- and iodine-labeled probes for the estrogen receptor.
Journal of medicinal chemistry 1995;38(14):2774-9.
1995: Choe Y S; Bonasera T A; Chi D Y; Welch M J; Katzenellenbogen J A
6 alpha-[18F]fluoroprogesterone: synthesis via halofluorination-oxidation, receptor binding and tissue distribution.
Nuclear medicine and biology 1995;22(5):635-42.
1995: Seielstad D A; Carlson K E; Katzenellenbogen J A; Kushner P J; Greene G L
Molecular characterization by mass spectrometry of the human estrogen receptor ligand-binding domain expressed in Escherichia coli.
Molecular endocrinology (Baltimore, Md.) 1995;9(6):647-58.
1995: Katzenellenbogen J A
Designing steroid receptor-based radiotracers to image breast and prostate tumors.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine 1995;36(6 Suppl):8S-13S.
1995: Choe Y S; Katzenellenbogen J A
Synthesis of C-6 fluoroandrogens: evaluation of ligands for tumor receptor imaging.
Steroids 1995;60(5):414-22.
1995: Miksicek R J; Carlson K E; Hwang K J; Katzenellenbogen J A
Studies using fluorescent tetrahydrochrysene estrogens for in situ visualization of the estrogen receptor in living cells.
Molecular endocrinology (Baltimore, Md.) 1995;9(5):592-604.
1995: Choe Y S; Lidström P J; Chi D Y; Bonasera T A; Welch M J; Katzenellenbogen J A
Synthesis of 11 beta-[18F]fluoro-5 alpha-dihydrotestosterone and 11 beta-[18F]fluoro-19-nor-5 alpha-dihydrotestosterone: preparation via halofluorination-reduction, receptor binding, and tissue distribution.
Journal of medicinal chemistry 1995;38(5):816-25.
1995: Chi D Y; Wilson S R; Katzenellenbogen J A
Crystal structure of doisynolic acid and the structure of other products formed during its synthesis.
Steroids 1995;60(3):261-4.
1995: Napolitano E; Fiaschi R; Carlson K E; Katzenellenbogen J A
11 beta-Substituted estradiol derivatives, potential high-affinity carbon-11-labeled probes for the estrogen receptor: a structure-affinity relationship study.
Journal of medicinal chemistry 1995;38(3):429-34.
1995: Buckman B O; Bonasera T A; Kirschbaum K S; Welch M J; Katzenellenbogen J A
Fluorine-18-labeled progestin 16 alpha, 17 alpha-dioxolanes: development of high-affinity ligands for the progesterone receptor with high in vivo target site selectivity.
Journal of medicinal chemistry 1995;38(2):328-37.
1995: Kym P R; Carlson K E; Katzenellenbogen J A
Evaluation of a highly efficient aryl azide photoaffinity labeling reagent for the progesterone receptor.
Bioconjugate chemistry 1995;6(1):115-22.
1994: Buckman B O; VanBrocklin H F; Dence C S; Bergmann S R; Welch M J; Katzenellenbogen J A
Synthesis and tissue biodistribution of [omega-11C]palmitic acid. A novel PET imaging agent for cardiac fatty acid metabolism.
Journal of medicinal chemistry 1994;37(15):2481-5.
1994: Bergmann K E; Wooge C H; Carlson K E; Katzenellenbogen B S; Katzenellenbogen J A
Bivalent ligands as probes of estrogen receptor action.
The Journal of steroid biochemistry and molecular biology 1994;49(2-3):139-52.
1994: O'Neil J P; Carlson K E; Anderson C J; Welch M J; Katzenellenbogen J A
Progestin radiopharmaceuticals labeled with technetium and rhenium: synthesis, binding affinity, and in vivo distribution of a new progestin N2S2-metal conjugate.
Bioconjugate chemistry 1994;5(3):182-93.
1994: Chi D Y; O'Neil J P; Anderson C J; Welch M J; Katzenellenbogen J A
Homodimeric and heterodimeric bis(amino thiol) oxometal complexes with rhenium(V) and technetium(V). Control of heterodimeric complex formation and an approach to metal complexes that mimic steroid hormones.
Journal of medicinal chemistry 1994;37(7):928-37.
1994: Bergmann K E; Carlson K E; Katzenellenbogen J A
Hexestrol diazirine photoaffinity labeling reagent for the estrogen receptor.
Bioconjugate chemistry 1994;5(2):141-50.
1994: Bergmann K E; Landvatter S W; Rocque P G; Carlson K E; Welch M J; Katzenellenbogen J A
Oxohexestrol derivatives labeled with fluorine-18. Synthesis, receptor binding and in vivo distribution of two non-steroidal estrogens as potential breast tumor imaging agents.
Nuclear medicine and biology 1994;21(1):25-39.
1994: VanBrocklin H F; Liu A; Welch M J; O'Neil J P; Katzenellenbogen J A
The synthesis of 7 alpha-methyl-substituted estrogens labeled with fluorine-18: potential breast tumor imaging agents.
Steroids 1994;59(1):34-45.
1993: Anstead G M; Carlson K E; Kym P R; Hwang K J; Katzenellenbogen J A
The effect of acceptor group variation on the solvatochromism of donor-acceptor fluorophores.
Photochemistry and photobiology 1993;58(6):785-94.
1993: Kym P R; Anstead G M; Pinney K G; Wilson S R; Katzenellenbogen J A
Molecular structures, conformational analysis, and preferential modes of binding of 3-aroyl-2-arylbenzo[b]thiophene estrogen receptor ligands: LY117018 and aryl azide photoaffinity labeling analogs.
Journal of medicinal chemistry 1993;36(24):3910-22.
1993: Katzenellenbogen J A; Mathias C J; VanBrocklin H F; Brodack J W; Welch M J
Titration of the in vivo uptake of 16 alpha-[18F]fluoroestradiol by target tissues in the rat: competition by tamoxifen, and implications for quantitating estrogen receptors in vivo and the use of animal models in receptor-binding radiopharmaceutical development.
Nuclear medicine and biology 1993;20(6):735-45.
1993: VanBrocklin H F; Carlson K E; Katzenellenbogen J A; Welch M J
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
Journal of medicinal chemistry 1993;36(11):1619-29.
1993: Anstead G M; Hwang K J; Katzenellenbogen J A
Characterization of the spectroscopic properties of a tetrahydrochrysene system containing a rigidified hydroxynitrostilbene chromophore: an inherently fluorescent ligand designed for the estrogen receptor.
Photochemistry and photobiology 1993;57(4):616-28.
1993: French A N; Wilson S R; Welch M J; Katzenellenbogen J A
A synthesis of 7 alpha-substituted estradiols: synthesis and biological evaluation of a 7 alpha-pentyl-substituted BODIPY fluorescent conjugate and a fluorine-18-labeled 7 alpha-pentylestradiol analog.
Steroids 1993;58(4):157-69.
1993: Kochanny M J; VanBrocklin H F; Kym P R; Carlson K E; O'Neil J P; Bonasera T A; Welch M J; Katzenellenbogen J A
Fluorine-18-labeled progestin ketals: synthesis and target tissue uptake selectivity of potential imaging agents for receptor-positive breast tumors.
Journal of medicinal chemistry 1993;36(9):1120-7.
1993: Kym P R; Carlson K E; Katzenellenbogen J A
Progestin 16 alpha, 17 alpha-dioxolane ketals as molecular probes for the progesterone receptor: synthesis, binding affinity, and photochemical evaluation.
Journal of medicinal chemistry 1993;36(9):1111-9.
1993: French A N; Napolitano E; VanBrocklin H F; Hanson R N; Welch M J; Katzenellenbogen J A
Synthesis, radiolabeling and tissue distribution of 11 beta-fluoroalkyl- and 11 beta-fluoroalkoxy-substituted estrogens: target tissue uptake selectivity and defluorination of a homologous series of fluorine-18-labeled estrogens.
Nuclear medicine and biology 1993;20(1):31-47.
1993: VanBrocklin H F; Rocque P A; Lee H V; Carlson K E; Katzenellenbogen J A; Welch M J
16 beta-[18F]fluoromoxestrol: a potent, metabolically stable positron emission tomography imaging agent for estrogen receptor positive human breast tumors.
Life sciences 1993;53(10):811-9.
1992: Rai R; Katzenellenbogen J A
Effect of conformational mobility and hydrogen-bonding interactions on the selectivity of some guanidinoaryl-substituted mechanism-based inhibitors of trypsin-like serine proteases.
Journal of medicinal chemistry 1992;35(23):4297-305.
1992: Hwang K J; Carlson K E; Anstead G M; Katzenellenbogen J A
Donor-acceptor tetrahydrochrysenes, inherently fluorescent, high-affinity ligands for the estrogen receptor: binding and fluorescence characteristics and fluorometric assay of receptor.
Biochemistry 1992;31(46):11536-45.
1992: Rai R; Katzenellenbogen J A
Guanidinophenyl-substituted enol lactones as selective, mechanism-based inhibitors of trypsin-like serine proteases.
Journal of medicinal chemistry 1992;35(22):4150-9.
1992: DiZio J P; Carlson K E; Bannochie C J; Welch M J; Von Angerer E; Katzenellenbogen J A
Estrogen platinum-diamine complexes: preparation of a non-steroidal estrogen platinum-diamine complex labeled with platinum-191 and a study of its binding to the estrogen receptor in vitro and its tissue distribution in vivo.
The Journal of steroid biochemistry and molecular biology 1992;42(3-4):363-73.
1992: Liu A; Carlson K E; Katzenellenbogen J A
Synthesis of high affinity fluorine-substituted ligands for the androgen receptor. Potential agents for imaging prostatic cancer by positron emission tomography.
Journal of medicinal chemistry 1992;35(11):2113-29.
1992: Liu A; Dence C S; Welch M J; Katzenellenbogen J A
Fluorine-18-labeled androgens: radiochemical synthesis and tissue distribution studies on six fluorine-substituted androgens, potential imaging agents for prostatic cancer.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine 1992;33(5):724-34.
1992: Pomper M G; Kochanny M J; Thieme A M; Carlson K E; VanBrocklin H F; Mathias C J; Welch M J; Katzenellenbogen J A
Fluorine-substituted corticosteroids: synthesis and evaluation as potential receptor-based imaging agents for positron emission tomography of the brain.
International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology 1992;19(4):461-80.
1992: Pinney K G; Carlson K E; Katzenellenbogen J A
Nonsteroidal estrogens bearing acyl azide functions: potential electrophilic and photoaffinity labeling agents for the estrogen receptor.
Steroids 1992;57(5):222-32.
1992: VanBrocklin H F; Pomper M G; Carlson K E; Welch M J; Katzenellenbogen J A
Preparation and evaluation of 17-ethynyl-substituted 16 alpha-[18F]fluoroestradiols: selective receptor-based PET imaging agents.
International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology 1992;19(3):363-74.
1992: DiZio J P; Anderson C J; Davison A; Ehrhardt G J; Carlson K E; Welch M J; Katzenellenbogen J A
Technetium- and rhenium-labeled progestins: synthesis, receptor binding and in vivo distribution of an 11 beta-substituted progestin labeled with technetium-99 and rhenium-186.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine 1992;33(4):558-69.
1991: DiZio J P; Fiaschi R; Davison A; Jones A G; Katzenellenbogen J A
Progestin-rhenium complexes: metal-labeled steroids with high receptor binding affinity, potential receptor-directed agents for diagnostic imaging or therapy.
Bioconjugate chemistry 1991;2(5):353-66.
1991: Baek D J; Katzenellenbogen J A
Halo enol lactone inhibitors of chymotrypsin: burst kinetics and enantioselectivity of inactivation.
Biochemical and biophysical research communications 1991;178(3):1335-42.
1991: Dehdashti F; McGuire A H; Van Brocklin H F; Siegel B A; Andriole D P; Griffeth L K; Pomper M G; Katzenellenbogen J A; Welch M J
Assessment of 21-[18F]fluoro-16 alpha-ethyl-19-norprogesterone as a positron-emitting radiopharmaceutical for the detection of progestin receptors in human breast carcinomas.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine 1991;32(8):1532-7.
1991: McGuire A H; Dehdashti F; Siegel B A; Lyss A P; Brodack J W; Mathias C J; Mintun M A; Katzenellenbogen J A; Welch M J
Positron tomographic assessment of 16 alpha-[18F] fluoro-17 beta-estradiol uptake in metastatic breast carcinoma.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine 1991;32(8):1526-31.
1991: Reed P E; Katzenellenbogen J A
Beta-substituted beta-phenylpropionyl chymotrypsins. Structural and stereochemical features in stable acyl enzymes.
Journal of medicinal chemistry 1991;34(3):1162-76.
1991: Pinney K G; Carlson K E; Katzenellenbogen B S; Katzenellenbogen J A
Efficient and selective photoaffinity labeling of the estrogen receptor using two nonsteroidal ligands that embody aryl azide or tetrafluoroaryl azide photoreactive functions.
Biochemistry 1991;30(9):2421-31.
1991: Liu A J; Katzenellenbogen J A; VanBrocklin H F; Mathias C J; Welch M J
20-[18F]fluoromibolerone, a positron-emitting radiotracer for androgen receptors: synthesis and tissue distribution studies.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine 1991;32(1):81-8.
1991: Reed P E; Katzenellenbogen J A
Proline-valine pseudo peptide enol lactones. Effective and selective inhibitors of chymotrypsin and human leukocyte elastase.
The Journal of biological chemistry 1991;266(1):13-21.
1990: Pomper M G; VanBrocklin H; Thieme A M; Thomas R D; Kiesewetter D O; Carlson K E; Mathias C J; Welch M J; Katzenellenbogen J A
11 beta-methoxy-, 11 beta-ethyl- and 17 alpha-ethynyl-substituted 16 alpha-fluoroestradiols: receptor-based imaging agents with enhanced uptake efficiency and selectivity.
Journal of medicinal chemistry 1990;33(12):3143-55.
1990: Anstead G M; Peterson C S; Pinney K G; Wilson S R; Katzenellenbogen J A
Torsionally and hydrophobically modified 2,3-diarylindenes as estrogen receptor ligands.
Journal of medicinal chemistry 1990;33(10):2726-34.
1990: Carlson K E; Katzenellenbogen J A
A comparative study of the selectivity and efficiency of target tissue uptake of five tritium-labeled androgens in the rat.
Journal of steroid biochemistry 1990;36(6):549-61.
1990: Pochapsky S S; VanBrocklin H F; Welch M J; Katzenellenbogen J A
Synthesis and tissue distribution of fluorine-18 labeled trifluorohexadecanoic acids. Considerations in the development of metabolically blocked myocardial imaging agents.
Bioconjugate chemistry 1990;1(4):231-44.
1990: Baek D J; Reed P E; Daniels S B; Katzenellenbogen J A
Alternate substrate inhibitors of an alpha-chymotrypsin: enantioselective interaction of aryl-substituted enol lactones.
Biochemistry 1990;29(18):4305-11.
1990: Pinney K G; Carlson K E; Katzenellenbogen J A
[3H]DU41165: a high affinity ligand and novel photoaffinity labeling reagent for the progesterone receptor.
Journal of steroid biochemistry 1990;35(2):179-89.
1990: Pomper M G; Pinney K G; Carlson K E; van Brocklin H; Mathias C J; Welch M J; Katzenellenbogen J A
Target tissue uptake selectivity of three fluorine-substituted progestins: potential imaging agents for receptor-positive breast tumors.
International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology 1990;17(3):309-19.
1990: VanBrocklin H F; Brodack J W; Mathias C J; Welch M J; Katzenellenbogen J A; Keenan J F; Mizejewski G J
Binding of 16 alpha-[18F]fluoro-17 beta-estradiol to alphafetoprotein in Sprague-Dawley female rats affects blood levels.
International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology 1990;17(8):769-73.
1989: Anstead G M; Peterson C S; Katzenellenbogen J A
Hydroxylated 2,3-diarylindenes: synthesis, estrogen receptor binding affinity, and binding orientation considerations.
Journal of steroid biochemistry 1989;33(5):877-87.
1989: Anstead G M; Wilson S R; Katzenellenbogen J A
2-Arylindenes and 2-arylindenones: molecular structures and considerations in the binding orientation of unsymmetrical nonsteroidal ligands to the estrogen receptor.
Journal of medicinal chemistry 1989;32(9):2163-71.
1989: Carlson K E; Coppey M; Magdelenat H; Katzenellenbogen J A
Receptor binding of NBD-labeled fluorescent estrogens and progestins in whole cells and cell-free preparations.
Journal of steroid biochemistry 1989;32(3):345-55.
1988: Mintun M A; Welch M J; Siegel B A; Mathias C J; Brodack J W; McGuire A H; Katzenellenbogen J A
Breast cancer: PET imaging of estrogen receptors.
Radiology 1988;169(1):45-8.
1988: Bindal R D; Katzenellenbogen J A
Bis(4-hydroxyphenyl)[2-(phenoxysulfonyl)phenyl]methane: isolation and structure elucidation of a novel estrogen from commercial preparations of phenol red (phenolsulfonphthalein)
Journal of medicinal chemistry 1988;31(10):1978-83.
1988: Bindal R D; Carlson K E; Katzenellenbogen B S; Katzenellenbogen J A
Lipophilic impurities, not phenolsulfonphthalein, account for the estrogenic activity in commercial preparations of phenol red.
Journal of steroid biochemistry 1988;31(3):287-93.
1988: Anstead G M; Katzenellenbogen J A
Optimizing of 2,3-diarylindenes as fluorescent estrogens: variation of the acceptor group, ortho substitution of the 2-ring, and C-1 methylation.
Journal of medicinal chemistry 1988;31(9):1754-61.
1988: Anstead G M; Altenbach R J; Wilson S R; Katzenellenbogen J A
2,3-Diarylindenes and 2,3-diarylindenones: synthesis, molecular structure, photochemistry, estrogen receptor binding affinity, and comparisons with related triarylethylenes.
Journal of medicinal chemistry 1988;31(7):1316-26.
1988: Pomper M G; Katzenellenbogen J A; Welch M J; Brodack J W; Mathias C J
21-[18F]fluoro-16 alpha-ethyl-19-norprogesterone: synthesis and target tissue selective uptake of a progestin receptor based radiotracer for positron emission tomography.
Journal of medicinal chemistry 1988;31(7):1360-3.
1988: Fevig T L; Mao M K; Katzenellenbogen J A
Estrogen receptor binding tolerance of 16 alpha-substituted estradiol derivatives.
Steroids 1988;51(5-6):471-97.
1988: Brandes S J; Katzenellenbogen J A
Fundamental considerations in the design of fluorine-18 labeled progestins and androgens as imaging agents for receptor-positive tumors of the breast and prostate.
International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology 1988;15(1):53-67.
1988: Welch M J; Katzenellenbogen J A; Mathias C J; Brodack J W; Carlson K E; Chi D Y; Dence C S; Kilbourn M R; Perlmutter J S; Raichle M E
N-(3-[18F]fluoropropyl)-spiperone: the preferred 18F labeled spiperone analog for positron emission tomographic studies of the dopamine receptor.
International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology 1988;15(1):83-97.
1988: Carlson K E; Brandes S J; Pomper M G; Katzenellenbogen J A
Uptake of three [3H]progestins by target tissues in vivo: implications for the design of diagnostic imaging agents.
International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology 1988;15(4):403-8.
1987: Bindal R D; Carlson K E; Reiner G C; Katzenellenbogen J A
11 beta-chloromethyl-[3H]estradiol-17 beta: a very high affinity, reversible ligand for the estrogen receptor.
Journal of steroid biochemistry 1987;28(4):361-70.
1987: Simpson D M; Elliston J F; Katzenellenbogen J A
Desmethylnafoxidine aziridine: an electrophilic affinity label for the estrogen receptor with high efficiency and selectivity.
Journal of steroid biochemistry 1987;28(3):233-45.
1987: Brandes S J; Katzenellenbogen J A
Fluorinated androgens and progestins: molecular probes for androgen and progesterone receptors with potential use in positron emission tomography.
Molecular pharmacology 1987;32(3):391-403.
1987: Mathias C J; Welch M J; Katzenellenbogen J A; Brodack J W; Kilbourn M R; Carlson K E; Kiesewetter D O
Characterization of the uptake of 16 alpha-([18F]fluoro)-17 beta-estradiol in DMBA-induced mammary tumors.
International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology 1987;14(1):15-25.
1986: Salituro F G; Carlson K E; Elliston J F; Katzenellenbogen B S; Katzenellenbogen J A
[125I]iododesethyl tamoxifen aziridine: synthesis and covalent labeling of the estrogen receptor with an iodine-labeled affinity label.
Steroids 1986;48(5-6):287-313.
1986: Welch M J; Chi D Y; Mathias C J; Kilbourn M R; Brodack J W; Katzenellenbogen J A
Biodistribution of N-alkyl and N-fluoroalkyl derivatives of spiroperidol; radiopharmaceuticals for PET studies of dopamine receptors.
International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology 1986;13(5):523-6.
1986: Chi D Y; Kilbourn M R; Katzenellenbogen J A; Brodack J W; Welch M J
Synthesis of no-carrier-added N-([18F]fluoroalkyl)spiperone derivatives.
International journal of radiation applications and instrumentation. Part A, Applied radiation and isotopes 1986;37(12):1173-80.
1984: Reiner G C; Katzenellenbogen B S; Bindal R D; Katzenellenbogen J A
Biological activity and receptor binding of a strongly interacting estrogen in human breast cancer cells.
Cancer research 1984;44(6):2302-8.
1983: McElvany K D; Carlson K E; Katzenellenbogen J A; Welch M J
Factors affecting the target site uptake selectivity of estrogen radiopharmaceuticals: serum binding and endogenous estrogens.
Journal of steroid biochemistry 1983;18(6):635-41.
1983: Katzenellenbogen J A; Carlson K E; Heiman D F; Robertson D W; Wei L L; Katzenellenbogen B S
Efficient and highly selective covalent labeling of the estrogen receptor with [3H]tamoxifen aziridine.
The Journal of biological chemistry 1983;258(6):3487-95.
1982: Landvatter S W; Katzenellenbogen J A; McElvany K D; Welch M J
(2R*,3S*)-1-[125I]Iodo-2,3-bis(4-hydroxyphenyl)pentane ([125I]iodonorhexestrol) and (2R*,3S*)-1-[77Br]Bromo-2,3-bis(4-hydroxyphenyl)pentane ([77Br]bromonorhexestrol), two gamma-emitting estrogens that show receptor-mediated uptake by target tissues in vivo.
Journal of medicinal chemistry 1982;25(11):1307-12.
1982: Senderoff S G; McElvany K D; Carlson K E; Heiman D F; Katzenellenbogen J A; Welch M J
Methodology for the synthesis and specific activity determination of 16 alpha-[77Br]-bromoestradiol-17 beta and 16 alpha-[77Br]-11 beta-methoxyestradiol-17 beta, two estrogen receptor-binding radiopharmaceuticals.
The International journal of applied radiation and isotopes 1982;33(7):545-51.
1982: McElvany K D; Katzenellenbogen J A; Shafer K E; Siegel B A; Senderoff S G; Welch M J
16 alpha-[77Br]bromoestradiol: dosimetry and preliminary clinical studies.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine 1982;23(5):425-30.
1982: McElvany K D; Carlson K E; Welch M J; Senderoff S G; Katzenellenbogen J A
In vivo comparison of 16 alpha[77Br]bromoestradiol-17 beta and 16 alpha-[125I]iodoestradiol-17 beta.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine 1982;23(5):420-4.
1982: Katzenellenbogen J A; McElvany K D; Senderoff S G; Carlson K E; Landvatter S W; Welch M J
16 alpha-[77Br]bromo-11 beta-methoxyestradiol-17 beta: a gamma-emitting estrogen imaging agent with high uptake and retention by target organs.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine 1982;23(5):411-9.
1981: Katzenellenbogen J A; Senderoff S G; McElvany K D; O'Brien H A; Welch M J
16 alpha-[77Br]bromoestradiol-17 beta: a high specific-activity, gamma-emitting tracer with uptake in rat uterus and uterus and induced mammary tumors.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine 1981;22(1):42-7.
1980: Heiman D F; Senderoff S G; Katzenellenbogen J A; Neeley R J
Estrogen receptor based imaging agents. 1. Synthesis and receptor binding affinity of some aromatic and D-ring halogenated estrogens.
Journal of medicinal chemistry 1980;23(9):994-1002.
1980: Goswami R; Harsy S G; Heiman D F; Katzenellenbogen J A
Estrogen receptor based imaging agents. 2. Synthesis and receptor binding affinity of side-chain halogenated hexestrol derivatives.
Journal of medicinal chemistry 1980;23(9):1002-8.
1980: Katzenellenbogen J A; Carlson K E; Heiman D F; Goswami R
Receptor-binding radiopharmaceuticals for imaging breast tumors: estrogen-receptor interactions and selectivity of tissue uptake of halogenated estrogen analogs.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine 1980;21(6):550-8.

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