Benita S Katzenellenbogen

Summary

Affiliation: University of Illinois
Country: USA

Publications

  1. pmc Tamoxifen downregulation of miR-451 increases 14-3-3ζ and promotes breast cancer cell survival and endocrine resistance
    A Bergamaschi
    Department of Molecular and Integrative Physiology, University of Illinois and College of Medicine at Urbana Champaign, Urbana, IL, USA
    Oncogene 31:39-47. 2012
  2. pmc Estrogen Receptors alpha and beta as determinants of gene expression: influence of ligand, dose, and chromatin binding
    Edmund C Chang
    Department of Molecular, University of Illinois, Urbana, Illinois 61801 3704, USA
    Mol Endocrinol 22:1032-43. 2008
  3. ncbi request reprint William L. McGuire Memorial Lecture. Antiestrogens: mechanisms of action and resistance in breast cancer
    B S Katzenellenbogen
    Department of Molecular and Integrative Physiology, University of Illinois, Urbana, USA
    Breast Cancer Res Treat 44:23-38. 1997
  4. pmc Estrogen receptor transcription and transactivation: Estrogen receptor alpha and estrogen receptor beta: regulation by selective estrogen receptor modulators and importance in breast cancer
    B S Katzenellenbogen
    Department of Molecular and Integrative Physiology, University of Illinois at Urbana Champaign, 407 South Goodwin Avenue, Urbana, IL 61801 3704, USA
    Breast Cancer Res 2:335-44. 2000
  5. ncbi request reprint Molecular mechanisms of estrogen action: selective ligands and receptor pharmacology
    B S Katzenellenbogen
    Department of Molecular and Integrative Physiology, University of Illinois and College of Medicine, 524 Burrill Hall, 407 S Goodwin Avenue, 61801 3704, Urbana, IL, USA
    J Steroid Biochem Mol Biol 74:279-85. 2000
  6. ncbi request reprint Bivalent ligands as probes of estrogen receptor action
    K E Bergmann
    Department of Chemistry, University of Illinois, Urbana
    J Steroid Biochem Mol Biol 49:139-52. 1994
  7. ncbi request reprint The estrogen receptor: a structure-based approach to the design of new specific hormone-receptor combinations
    R Tedesco
    Department of Chemistry, University of Illinois, Urbana 61801, USA
    Chem Biol 8:277-87. 2001
  8. ncbi request reprint Synthesis and biological evaluation of a novel series of furans: ligands selective for estrogen receptor alpha
    D S Mortensen
    Department of Chemistry, University of Illinois, Urbana, Illinois 61801, USA
    J Med Chem 44:3838-48. 2001
  9. ncbi request reprint Structure-function relationships in estrogen receptors and the characterization of novel selective estrogen receptor modulators with unique pharmacological profiles
    B S Katzenellenbogen
    Department of Molecular and Integrative Physiology, University of Illinois and College of Medicine, Urbana 61801, USA
    Ann N Y Acad Sci 949:6-15. 2001
  10. ncbi request reprint Furans with basic side chains: synthesis and biological evaluation of a novel series of antagonists with selectivity for the estrogen receptor alpha
    D S Mortensen
    Department of Chemistry, University of Illinois, Urbana, 61801, USA
    Bioorg Med Chem Lett 11:2521-4. 2001

Research Grants

  1. ANTIESTROGENS--MECHANISM OF ANTAGONIST ACTION
    Benita Katzenellenbogen; Fiscal Year: 2003
  2. ANTIESTROGENS--MECHANISM OF ANTAGONIST ACTION
    Benita Katzenellenbogen; Fiscal Year: 2000
  3. DOMINANT NEGATIVE ESTROGEN RECEPTORS AND BREAST CANCER
    Benita Katzenellenbogen; Fiscal Year: 2000
  4. ANTIESTROGENS--MECHANISM OF ANTAGONIST ACTION
    Benita Katzenellenbogen; Fiscal Year: 2001
  5. DOMINANT NEGATIVE ESTROGEN RECEPTORS AND BREAST CANCER
    Benita Katzenellenbogen; Fiscal Year: 2001
  6. ANTIESTROGENS--MECHANISM OF ANTAGONIST ACTION
    Benita Katzenellenbogen; Fiscal Year: 2002
  7. DOMINANT NEGATIVE ESTROGEN RECEPTORS AND BREAST CANCER
    Benita Katzenellenbogen; Fiscal Year: 2002
  8. ANTIESTROGENS: MECHANISM OF ANTAGONIST ACTION
    Benita Katzenellenbogen; Fiscal Year: 2004
  9. ANTIESTROGENS: MECHANISM OF ANTAGONIST ACTION
    Benita Katzenellenbogen; Fiscal Year: 2005
  10. ANTIESTROGENS: MECHANISM OF ANTAGONIST ACTION
    Benita Katzenellenbogen; Fiscal Year: 2006

Collaborators

Detail Information

Publications80

  1. pmc Tamoxifen downregulation of miR-451 increases 14-3-3ζ and promotes breast cancer cell survival and endocrine resistance
    A Bergamaschi
    Department of Molecular and Integrative Physiology, University of Illinois and College of Medicine at Urbana Champaign, Urbana, IL, USA
    Oncogene 31:39-47. 2012
    ....
  2. pmc Estrogen Receptors alpha and beta as determinants of gene expression: influence of ligand, dose, and chromatin binding
    Edmund C Chang
    Department of Molecular, University of Illinois, Urbana, Illinois 61801 3704, USA
    Mol Endocrinol 22:1032-43. 2008
    ....
  3. ncbi request reprint William L. McGuire Memorial Lecture. Antiestrogens: mechanisms of action and resistance in breast cancer
    B S Katzenellenbogen
    Department of Molecular and Integrative Physiology, University of Illinois, Urbana, USA
    Breast Cancer Res Treat 44:23-38. 1997
    ..In addition, antiestrogens which work through somewhat different mechanisms of interaction with the ER should prove useful in treatment of some breast cancers that become resistant to a different category of antiestrogens...
  4. pmc Estrogen receptor transcription and transactivation: Estrogen receptor alpha and estrogen receptor beta: regulation by selective estrogen receptor modulators and importance in breast cancer
    B S Katzenellenbogen
    Department of Molecular and Integrative Physiology, University of Illinois at Urbana Champaign, 407 South Goodwin Avenue, Urbana, IL 61801 3704, USA
    Breast Cancer Res 2:335-44. 2000
    ..As these critical components are becoming increasingly well defined, they provide a sound basis for the development of novel SERMs with optimal profiles of tissue selectivity as medical therapeutic agents...
  5. ncbi request reprint Molecular mechanisms of estrogen action: selective ligands and receptor pharmacology
    B S Katzenellenbogen
    Department of Molecular and Integrative Physiology, University of Illinois and College of Medicine, 524 Burrill Hall, 407 S Goodwin Avenue, 61801 3704, Urbana, IL, USA
    J Steroid Biochem Mol Biol 74:279-85. 2000
    ....
  6. ncbi request reprint Bivalent ligands as probes of estrogen receptor action
    K E Bergmann
    Department of Chemistry, University of Illinois, Urbana
    J Steroid Biochem Mol Biol 49:139-52. 1994
    ....
  7. ncbi request reprint The estrogen receptor: a structure-based approach to the design of new specific hormone-receptor combinations
    R Tedesco
    Department of Chemistry, University of Illinois, Urbana 61801, USA
    Chem Biol 8:277-87. 2001
    ..Conclusions: In best cases, the new interaction is sufficiently favorable and orthogonal so as to represent the creation of a new hormone specificity, which might be useful in the regulation of transgene activity...
  8. ncbi request reprint Synthesis and biological evaluation of a novel series of furans: ligands selective for estrogen receptor alpha
    D S Mortensen
    Department of Chemistry, University of Illinois, Urbana, Illinois 61801, USA
    J Med Chem 44:3838-48. 2001
    ..These ligands should be useful in studying the biological roles of both ER alpha and ER beta, and they might form the basis for the development of novel estrogen pharmaceuticals...
  9. ncbi request reprint Structure-function relationships in estrogen receptors and the characterization of novel selective estrogen receptor modulators with unique pharmacological profiles
    B S Katzenellenbogen
    Department of Molecular and Integrative Physiology, University of Illinois and College of Medicine, Urbana 61801, USA
    Ann N Y Acad Sci 949:6-15. 2001
    ....
  10. ncbi request reprint Furans with basic side chains: synthesis and biological evaluation of a novel series of antagonists with selectivity for the estrogen receptor alpha
    D S Mortensen
    Department of Chemistry, University of Illinois, Urbana, 61801, USA
    Bioorg Med Chem Lett 11:2521-4. 2001
    ..3-alkyl-2,4,5-triarylfurans with basic side-chain substituents were prepared as ligands for the estrogen receptor. Those analogues having the basic side chain on the C(4) phenol were high-affinity, ERalpha-selective antagonists...
  11. ncbi request reprint Regulation of prothymosin alpha gene expression by estrogen in estrogen receptor-containing breast cancer cells via upstream half-palindromic estrogen response element motifs
    P G Martini
    Department of Molecular and Integrative Physiology, University of Illinois and College of Medicine, Urbana, Illinois 61801, USA
    Endocrinology 142:3493-501. 2001
    ....
  12. ncbi request reprint Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues
    M J Meyers
    Department of Chemistry, University of Illinois, Urbana, Illinois 61801, USA
    J Med Chem 44:4230-51. 2001
    ..These ERbeta-selective compounds may prove to be valuable tools in understanding the differences in structure and biological function of ERalpha and ERbeta...
  13. pmc An estrogen receptor-selective coregulator that potentiates the effectiveness of antiestrogens and represses the activity of estrogens
    M M Montano
    Department of Molecular and Integrative Physiology, University of Illinois and College of Medicine, Urbana, IL 61801 3704, USA
    Proc Natl Acad Sci U S A 96:6947-52. 1999
    ....
  14. ncbi request reprint Human estrogen receptor beta-specific monoclonal antibodies: characterization and use in studies of estrogen receptor beta protein expression in reproductive tissues
    I Choi
    Department of Molecular and Integrative Physiology, University of Illinois College of Medicine, 524 Burrill Hall, 407 South Goodwin Avenue, Urbana, IL, USA
    Mol Cell Endocrinol 181:139-50. 2001
    ....
  15. ncbi request reprint Involvement of cyclic AMP response element binding protein (CREB) and estrogen receptor phosphorylation in the synergistic activation of the estrogen receptor by estradiol and protein kinase activators
    G Lazennec
    Department of Molecular and Integrative Physiology, University of Illinois at Urbana-Champaign, 524 Burrill Hall, 407 South Goodwin Ave, Urbana, IL 61801, USA
    J Steroid Biochem Mol Biol 77:193-203. 2001
    ....
  16. pmc Prothymosin alpha selectively enhances estrogen receptor transcriptional activity by interacting with a repressor of estrogen receptor activity
    P G Martini
    Departments of Molecular and Integrative Physiology and Cell and Structural Biology, University of Illinois and College of Medicine, Urbana, Illinois 61801, USA
    Mol Cell Biol 20:6224-32. 2000
    ..Proteins such as PTalpha represent an additional regulatory component that defines a novel paradigm enabling receptor-selective enhancement of transcriptional activity by coactivators...
  17. ncbi request reprint Mechanistic aspects of estrogen receptor activation probed with constitutively active estrogen receptors: correlations with DNA and coregulator interactions and receptor conformational changes
    G Lazennec
    Department of Molecular and Integrative Physiology, University of Illinois, Urbana 61801, USA
    Mol Endocrinol 11:1375-86. 1997
    ....
  18. pmc Estrogen action and male fertility: roles of the sodium/hydrogen exchanger-3 and fluid reabsorption in reproductive tract function
    Q Zhou
    Department of Veterinary Biosciences, University of Illinois, Urbana, IL 61802, USA
    Proc Natl Acad Sci U S A 98:14132-7. 2001
    ..Finally, these data raise the possibility of targeting ER alpha in developing a contraceptive for the male...
  19. ncbi request reprint A transcriptionally active estrogen receptor mutant is a novel type of dominant negative inhibitor of estrogen action
    E M McInerney
    Department of Molecular and Integrative Physiology, University of Illinois and College of Medicine, Urbana 61801, USA
    Mol Endocrinol 10:1519-26. 1996
    ....
  20. pmc The estrogen-regulated transcription factor PITX1 coordinates gene-specific regulation by estrogen receptor-alpha in breast cancer cells
    Joshua D Stender
    Department of Biochemistry, University of Illinois at Urbana Champaign, Urbana, Illinois 61801 3704, USA
    Mol Endocrinol 25:1699-709. 2011
    ..These studies identify PITX1 as a new ERα transcriptional target that acts as a repressor to coordinate and fine tune target-specific, ERα-mediated transcriptional activity in human breast cancer cells...
  21. pmc Genomic collaboration of estrogen receptor alpha and extracellular signal-regulated kinase 2 in regulating gene and proliferation programs
    Zeynep Madak-Erdogan
    University of Illinois, Department of Molecular and Integrative Physiology, 407 South Goodwin Ave, Urbana, IL 61801 3704, USA
    Mol Cell Biol 31:226-36. 2011
    ....
  22. pmc Genome-wide dynamics of chromatin binding of estrogen receptors alpha and beta: mutual restriction and competitive site selection
    Tze Howe Charn
    Department of Bioengineering, University of Illinois, Urbana, Illinois 61801, USA
    Mol Endocrinol 24:47-59. 2010
    ....
  23. ncbi request reprint Impact of estrogen receptor beta on gene networks regulated by estrogen receptor alpha in breast cancer cells
    Edmund C Chang
    Department of Molecular and Integrative Physiology, University of Illinois, 524 Burrill Hall, 407 South Goodwin Avenue, Urbana, 61801 3704, USA
    Endocrinology 147:4831-42. 2006
    ..Our observations suggest that the relative levels of ERbeta and ERalpha in breast cancers are likely to impact cell proliferation and the activities of diverse signaling pathways and their response to ER ligands and endocrine therapies...
  24. ncbi request reprint Kinase-specific phosphorylation of the estrogen receptor changes receptor interactions with ligand, deoxyribonucleic acid, and coregulators associated with alterations in estrogen and tamoxifen activity
    Varsha S Likhite
    Department of Chemistry, University of Illinois, 600 South Mathews Avenue, Urbana, Illinois 61801, USA
    Mol Endocrinol 20:3120-32. 2006
    ....
  25. ncbi request reprint Gene expression preferentially regulated by tamoxifen in breast cancer cells and correlations with clinical outcome
    Jonna Frasor
    Department of Molecular and Integrative Physiology and Cell and Developmental Biology, University of Illinois and College of Medicine, Urbana, Illinois 61801 3704, USA
    Cancer Res 66:7334-40. 2006
    ..This may have a potential effect on the choice of tamoxifen versus aromatase inhibitors as adjuvant endocrine therapy...
  26. ncbi request reprint Molecular cloning of porcine estrogen receptor-beta complementary DNAs and developmental expression in periimplantation embryos
    Andrés A Kowalski
    Interdisciplinary Concentration in Animal Molecular and Cell Biology, Department of Animal Sciences, University of Florida, Gainesville, Florida 32611 0910, USA
    Biol Reprod 66:760-9. 2002
    ..These studies taken together suggest that embryonic ER-beta likely mediates the autocrine functions of estrogens in the dynamic regulation of embryonic growth and development at periimplantation...
  27. ncbi request reprint Estrogen regulation of the glucuronidation enzyme UGT2B15 in estrogen receptor-positive breast cancer cells
    William R Harrington
    Department of Molecular and Integrative Physiology, University of Illinois, Illinois 61801 3704, USA
    Endocrinology 147:3843-50. 2006
    ....
  28. ncbi request reprint Estrogen dendrimer conjugates that preferentially activate extranuclear, nongenomic versus genomic pathways of estrogen action
    William R Harrington
    University of Illinois, Department of Molecular and Integrative Physiology, 524 Burrill Hall, 407 South Goodwin Avenue, Urbana, Illinois 61801 3704, USA
    Mol Endocrinol 20:491-502. 2006
    ....
  29. ncbi request reprint Synthesis and evaluation of estrogen receptor ligands with bridged oxabicyclic cores containing a diarylethylene motif: estrogen antagonists of unusual structure
    Hai Bing Zhou
    Department of Chemistry, University of Illinois, 600 South Mathews Avenue, Urbana, Illinois 61801, USA
    J Med Chem 48:7261-74. 2005
    ..These compounds, based on the bicyclo[2.2.1]core system, expand the structural diversity of ligands that can be antagonists for the estrogen receptors...
  30. pmc Estrogen down-regulation of the corepressor N-CoR: mechanism and implications for estrogen derepression of N-CoR-regulated genes
    Jonna Frasor
    Department of Molecular and Integrative Physiology, University of Illinois at Urbana Champaign, Urbana, IL 61801, USA
    Proc Natl Acad Sci U S A 102:13153-7. 2005
    ....
  31. ncbi request reprint Isocoumarins as estrogen receptor beta selective ligands: Isomers of isoflavone phytoestrogens and their metabolites
    Meri De Angelis
    Department of Chemistry, University of Illinois, Urbana, 61801, USA
    Bioorg Med Chem 13:6529-42. 2005
    ..Two of the best compounds, which combine high transcriptional potency with an ERbeta selectivity greater than 1000, should prove to be excellent probes of ERbeta function in vivo...
  32. ncbi request reprint Cyclin D1 antagonizes BRCA1 repression of estrogen receptor alpha activity
    Chenguang Wang
    Department of Oncology, Lombardi Comprehensive Cancer Center, Georgetown University School of Medicine, Washington, District of Columbia 20007, USA
    Cancer Res 65:6557-67. 2005
    ..As cyclin D1 abundance is regulated by oncogenic and mitogenic signals, the antagonism of the BRCA1-mediated ERalpha repression by cyclin D1 may contribute to the selective induction of BRCA1-regulated target genes...
  33. ncbi request reprint Estrogen-occupied estrogen receptor represses cyclin G2 gene expression and recruits a repressor complex at the cyclin G2 promoter
    Fabio Stossi
    Department of Molecular and Integrative Physiology, Department of Chemistry, University of Illinois at Urbana Champaign, Urbana, IL 61801, USA
    J Biol Chem 281:16272-8. 2006
    ....
  34. ncbi request reprint Structure-guided optimization of estrogen receptor binding affinity and antagonist potency of pyrazolopyrimidines with basic side chains
    Hai Bing Zhou
    Department of Chemistry, University of Illinois, Urbana, Illinois 61801, USA
    J Med Chem 50:399-403. 2007
    ....
  35. pmc Whole-genome cartography of estrogen receptor alpha binding sites
    Chin Yo Lin
    Genome Institute of Singapore, Singapore, Republic of Singapore
    PLoS Genet 3:e87. 2007
    ..Taken together, this genome-scale analysis suggests complex but definable rules governing ERalpha binding and gene regulation...
  36. ncbi request reprint Estrogen-regulated gene networks in human breast cancer cells: involvement of E2F1 in the regulation of cell proliferation
    Joshua D Stender
    Department of Biochemistry, University of Illinois at Urbana Champaign, Urbana, Illinois 61801 3704, USA
    Mol Endocrinol 21:2112-23. 2007
    ....
  37. ncbi request reprint Antagonists selective for estrogen receptor alpha
    Jun Sun
    Department of Molecular and Integrative Physiology, University of Illinois and University of Illinois College of Medicine, Urbana, Illinois 61801, USA
    Endocrinology 143:941-7. 2002
    ..These compounds should be useful in studying the biological functions of ER(alpha) and ER(beta) and in selectively blocking responses that are mediated through ER(alpha)...
  38. pmc Nuclear and extranuclear pathway inputs in the regulation of global gene expression by estrogen receptors
    Zeynep Madak-Erdogan
    Department of Cell and Developmental Biology, University of Illinois, Urbana, Illinois 61801, USA
    Mol Endocrinol 22:2116-27. 2008
    ..This study thus highlights the importance of inputs from both nuclear and extranuclear ER signaling pathways in regulating patterns of gene expression in breast cancer cells...
  39. pmc The roles of membrane estrogen receptor subtypes in modulating dopamine transporters in PC-12 cells
    Rebecca A Alyea
    Department of Biochemistry and Molecular Biology, University of Texas Medical Branch, Galveston, Texas, USA
    J Neurochem 106:1525-33. 2008
    ..Therefore, ERalpha is largely responsible for non-genomic estrogenic effects on DAT activity...
  40. ncbi request reprint Estrogen receptor regulation of carbonic anhydrase XII through a distal enhancer in breast cancer
    Daniel H Barnett
    Department of Cell and Developmental Biology, College of Medicine, University of Illinois at Urbana Champaign, Urbana, IL 61801 3704, USA
    Cancer Res 68:3505-15. 2008
    ..Our findings highlight the crucial role of ER in the regulation of the CA12 gene, and provide insight into the transcriptional regulatory mechanism that accounts for the strong association of CA12 and ER in human breast cancers...
  41. pmc A human estrogen receptor (ER)alpha mutation with differential responsiveness to nonsteroidal ligands: novel approaches for studying mechanism of ER action
    Ramasamy Paulmurugan
    Department of Radiology, Stanford University School of Medicine, James H Clark Center, Stanford, CA 94305 5427, USA
    Mol Endocrinol 22:1552-64. 2008
    ..This system provides a model for ER-mutants that show differential ligand responsiveness to gene activation to gain insight into the phenomenon of hormone resistance observed in endocrine therapies of ER-positive breast cancers...
  42. pmc NFkappaB selectivity of estrogen receptor ligands revealed by comparative crystallographic analyses
    Kendall W Nettles
    Department of Cancer Biology, The Scripps Research Institute, 5353 Parkside Drive, Jupiter, Florida 33458, USA
    Nat Chem Biol 4:241-7. 2008
    ..The ability to crystallize many receptor-ligand complexes with distinct pharmacophores allows one to define structural features of signaling specificity that would not be apparent in a single structure...
  43. doi request reprint Monoaryl-substituted salicylaldoximes as ligands for estrogen receptor beta
    Filippo Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Pisa, Italy
    J Med Chem 51:1344-51. 2008
    ..The chloro-substituted derivative showed the highest beta affinity and selectivity, and it also proved to be an ERbeta partial agonist with an EC 50 of 11 nM...
  44. ncbi request reprint Protein kinase A activation of estrogen receptor alpha transcription does not require proteasome activity and protects the receptor from ligand-mediated degradation
    Houng Wei Tsai
    Division of Endocrinology and Metabolism, Department of Internal Medicine, University of Virginia, Box 800578, Charlottesville, Virginia 22908, USA
    Endocrinology 145:2730-8. 2004
    ....
  45. pmc A repressive role for prohibitin in estrogen signaling
    Bin He
    Department of Molecular Biology, Baylor College of Medicine, One Baylor Plaza, Houston, TX 77030, USA
    Mol Endocrinol 22:344-60. 2008
    ..Our results indicate that PHB functions as a transcriptional corepressor for ERalpha in vitro and in vivo, and that its heteromerization with REA acts as a novel mechanism to limit its corepressor activity...
  46. ncbi request reprint Elemental isomerism: a boron-nitrogen surrogate for a carbon-carbon double bond increases the chemical diversity of estrogen receptor ligands
    Hai Bing Zhou
    Department of Chemistry, University of Illinois, Urbana, IL 61801, USA
    Chem Biol 14:659-69. 2007
    ....
  47. ncbi request reprint Distinctive actions of membrane-targeted versus nuclear localized estrogen receptors in breast cancer cells
    Deshanie Rai
    Department of Molecular and Integrative Physiology, University of Illinois and College of Medicine, 524 Burrill Hall, 407 South Goodwin Avenue, Urbana, Illinois 61801 3704, USA
    Mol Endocrinol 19:1606-17. 2005
    ..Hence, this study reveals distinct actions of the MT-ER vs. the WT-ER in effecting estrogen actions in breast cancer cells...
  48. ncbi request reprint Estrogen receptor regulation of quinone reductase in breast cancer: implications for estrogen-induced breast tumor growth and therapeutic uses of tamoxifen
    Monica M Montano
    Department of Pharmacology, Case Western Reserve University, Cleveland, OH 44122, USA
    Front Biosci 10:1440-61. 2005
    ..It is possible that the basis for some of the anticancer action of antiestrogens is that the induction of NQO1 inhibits the genotoxic effects induced by the oxidative metabolism of estrogens...
  49. ncbi request reprint Biomedicine. Defining the "S" in SERMs
    Benita S Katzenellenbogen
    Department of Molecular and Integrative Physiology, University of Illinois and College of Medicine at Urbana Champaign, Urbana, IL 61801, USA
    Science 295:2380-1. 2002
  50. ncbi request reprint Profiling of estrogen up- and down-regulated gene expression in human breast cancer cells: insights into gene networks and pathways underlying estrogenic control of proliferation and cell phenotype
    Jonna Frasor
    Department of Molecular and Integrative Physiology, University of Illinois, Urbana, Illinois 61801, USA
    Endocrinology 144:4562-74. 2003
    ..Our studies highlight the diverse gene networks and metabolic and cell regulatory pathways through which this hormone operates to achieve its widespread effects on breast cancer cells...
  51. ncbi request reprint Characterization of the biological roles of the estrogen receptors, ERalpha and ERbeta, in estrogen target tissues in vivo through the use of an ERalpha-selective ligand
    Heather A Harris
    Women s Health Research Institute, Wyeth Research, Collegeville, Pennsylvania 19426, USA
    Endocrinology 143:4172-7. 2002
    ....
  52. ncbi request reprint Novel estrogen receptor ligands based on an anthranylaldoxime structure: role of the phenol-type pseudocycle in the binding process
    Filippo Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 46:4032-42. 2003
    ..The limited size of this pocket does not allow accommodation of N-substituents larger than a methyl group, which is consistent with the low binding affinity of the N-Et compound 5c...
  53. ncbi request reprint Activities of estrogen receptor alpha- and beta-selective ligands at diverse estrogen responsive gene sites mediating transactivation or transrepression
    William R Harrington
    Department of Molecular and Integrative Physiology, University of Illinois, 407 S Goodwin Avenue, 524 Burrill Hall, Urbana, IL 61801 3704, USA
    Mol Cell Endocrinol 206:13-22. 2003
    ....
  54. ncbi request reprint Modulation of estrogen receptor activity by selective coregulators
    Paolo G V Martini
    Department of Molecular and Integrative Physiology, College of Medicine, University of Illinois, 524 Burrill Hall, 407 South Goodwin Avenue, Urbana, IL 61801, USA
    J Steroid Biochem Mol Biol 85:117-22. 2003
    ..Analysis of the mechanisms underlying the activities of these two proteins highlights a new role for REA and PTalpha as activity-modulating proteins that confer receptor specificity...
  55. ncbi request reprint Response-specific and ligand dose-dependent modulation of estrogen receptor (ER) alpha activity by ERbeta in the uterus
    Jonna Frasor
    Department of Molecular and Integrative Physiology, University of Illinois, 407 South Goodwin Avenue, Urbana, IL 61801 3704, USA
    Endocrinology 144:3159-66. 2003
    ..In addition, ERbeta can modulate ERalpha activity in a response-specific and dose-dependent manner...
  56. ncbi request reprint Bridged bicyclic cores containing a 1,1-diarylethylene motif are high-affinity subtype-selective ligands for the estrogen receptor
    Rajeev S Muthyala
    Department of Chemistry, University of Illinois, Urbana, Illinois 61801, USA
    J Med Chem 46:1589-602. 2003
    ..Some of the compounds show significant affinity selectivity in favor of ERbeta (4- to 5-fold), and in cell-based assays for transcriptional activity most are partial agonists on ERalpha and full antagonists on ERbeta...
  57. ncbi request reprint DNA shuffling method for generating estrogen receptor alpha and beta chimeras in yeast
    Jun Sun
    University of Illinois, 407 South Goodwin Avenue, Urbana, IL 61801 3704, USA
    Biotechniques 34:278-80, 282, 284 passim. 2003
    ..This method should prove to be useful for generating chimeric gene products from parent templates that share relatively low sequence identity...
  58. ncbi request reprint Molecular basis for the subtype discrimination of the estrogen receptor-beta-selective ligand, diarylpropionitrile
    Jun Sun
    Department of Molecular and Integrative Physiology, University of Illinois, Urbana, Illinois 61801, USA
    Mol Endocrinol 17:247-58. 2003
    ..Our findings highlight that a limited number of critical interactions of DPN with the ERbeta ligand-binding pocket underlie its ER subtype-selective character...
  59. ncbi request reprint Estrogenic diazenes: heterocyclic non-steroidal estrogens of unusual structure with selectivity for estrogen receptor subtypes
    Usha Ghosh
    Department of Chemistry, University of Illinois, IL 61801, Urbana, USA
    Bioorg Med Chem 11:629-57. 2003
    ....
  60. ncbi request reprint Allosteric control of ligand selectivity between estrogen receptors alpha and beta: implications for other nuclear receptors
    Kendall W Nettles
    Ben May Institute for Cancer Research, University of Chicago, Chicago, IL 60637 USA
    Mol Cell 13:317-27. 2004
    ..These results demonstrate the importance of long-range interactions in the transmission of information through the ligand binding domain as well as in determining the ligand selectivity of closely related NR receptor subtypes...
  61. ncbi request reprint Selective estrogen receptor modulators: discrimination of agonistic versus antagonistic activities by gene expression profiling in breast cancer cells
    Jonna Frasor
    Department of Molecular and Integrative Physiology, University of Illinois and College of Medicine, 407 South Goodwin Avenue, Urbana, IL 61801, USA
    Cancer Res 64:1522-33. 2004
    ..Hence, gene expression profiling can discern fundamental differences among SERMs and provides insight into the distinct biologies of TOT, Ral, and ICI in breast cancer...
  62. ncbi request reprint 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
    Rajeev S Muthyala
    Department of Chemistry, University of Illinois, 600 South Mathews Avenue, Urbana, IL 61801, USA
    Bioorg Med Chem 12:1559-67. 2004
    ..The availability and the in vitro characterization of the equol enantiomers should enable their biological effects to be studied in detail...
  63. ncbi request reprint Indazole estrogens: highly selective ligands for the estrogen receptor beta
    Meri De Angelis
    Department of Chemistry, University of Illinois, 600 South Matthews Avenue, Urbana, Illinois 61801, USA
    J Med Chem 48:1132-44. 2005
    ..These findings also contribute to an evolving pharmacophore that characterizes certain nonsteroidal ligands having high ERbeta subtype affinity and potency selectivity...
  64. pmc Genetic deletion of the repressor of estrogen receptor activity (REA) enhances the response to estrogen in target tissues in vivo
    Seong Eun Park
    University of Illinois, Department of Molecular and Integrative Physiology, 524 Burrill Hall, 407 South Goodwin Ave, Urbana, IL 61801 3704, USA
    Mol Cell Biol 25:1989-99. 2005
    ..These studies demonstrate that REA is a significant modulator of estrogen responsiveness in vivo: it normally restrains estrogen actions, moderating ER stimulation and enhancing ER repression of E2-regulated genes...
  65. ncbi request reprint Pyrazolo[1,5-a]pyrimidines: estrogen receptor ligands possessing estrogen receptor beta antagonist activity
    Dennis R Compton
    Department of Chemistry and Department of Molecular and Integrative Physiology, University of Illinois, 600 South Matthews Avenue, Urbana, Illinois 61801, USA
    J Med Chem 47:5872-93. 2004
    ....
  66. ncbi request reprint Directed evolution of human estrogen receptor variants with significantly enhanced androgen specificity and affinity
    Zhilei Chen
    Center for Biophysics and Computational Biology and the Department of Molecular and Integrative Physiology, University of Illinois, Urbana, Illinois 61801, USA
    J Biol Chem 279:33855-64. 2004
    ....
  67. ncbi request reprint Therapeutic targeting in the estrogen receptor hormonal pathway
    Benita S Katzenellenbogen
    Department of Molecular and Integrative Physiology, University of Illinois and College of Medicine, Urbana, IL, USA
    Semin Oncol 31:28-38. 2004
    ....
  68. ncbi request reprint Structural characterization of a subtype-selective ligand reveals a novel mode of estrogen receptor antagonism
    Andrew K Shiau
    The Howard Hughes Medical Institute and Department of Biochemistry and Biophysics, University of California, San Francisco, California 94143, USA
    Nat Struct Biol 9:359-64. 2002
    ..Instead, THC antagonizes ER beta through a novel mechanism we term 'passive antagonism'...
  69. ncbi request reprint Transcriptional profiling of estrogen-regulated gene expression via estrogen receptor (ER) alpha or ERbeta in human osteosarcoma cells: distinct and common target genes for these receptors
    Fabio Stossi
    Department of Molecular and Integrative Physiology, University of Illinois, 524 Burrill Hall, 407 South Goodwin Avenue, Urbana, Illinois 61801 3704, USA
    Endocrinology 145:3473-86. 2004
    ..These studies indicate both common as well as distinct target genes for these two ERs, and identify many novel genes not previously known to be under estrogen regulation...
  70. ncbi request reprint Estrogen receptor isoform-specific induction of progesterone receptors in human osteoblasts
    David J Rickard
    Department of Biochemistry and Molecular Biology, Mayo Clinic, Rochester, Minnesota 55905, USA
    J Bone Miner Res 17:580-92. 2002
    ..Together, these results show that although estrogen can up-regulate endogenous PR gene expression in osteoblasts via both ER isoforms, ER-alpha is the predominant inducer...
  71. pmc Alteration of large-scale chromatin structure by estrogen receptor
    Anne C Nye
    Department of Cell and Structural Biology, University of Illinois at Urbana Champaign, Urbana, Illinois 61801, USA
    Mol Cell Biol 22:3437-49. 2002
    ..This work demonstrates that when tethered or recruited to DNA, ER possesses a novel large-scale chromatin unfolding activity...
  72. ncbi request reprint Selective recognition of distinct classes of coactivators by a ligand-inducible activation domain
    Mari Luz Acevedo
    Department of Molecular Biology and Genetics, Cornell University, Ithaca, NY 14853, USA
    Mol Cell 13:725-38. 2004
    ..Collectively, our results suggest that "facilitated recruitment," rather than competition, drives the sequential recruitment of SRC complexes and Mediator by NRs...
  73. ncbi request reprint Localization of androgen and estrogen receptors in adult male mouse reproductive tract
    Qing Zhou
    Department of Veterinary Biosciences, University of Illinois, Urbana 61802, USA
    J Androl 23:870-81. 2002
    ..This study demonstrates that the reproductive tracts of male mice differ considerably from those of rats in expression of ARs and ERs and that caution is needed when extrapolating nuclear steroid receptor data across mammalian species...
  74. ncbi request reprint Estrogen receptor inducibility of the human Na+/H+ exchanger regulatory factor/ezrin-radixin-moesin binding protein 50 (NHE-RF/EBP50) gene involving multiple half-estrogen response elements
    Tracy R Ediger
    Department of Cell and Structural Biology, University of Illinois and College of Medicine, Urbana, Illinois 61801 3704, USA
    Mol Endocrinol 16:1828-39. 2002
    ..Our findings highlight a paradigm for gene regulation via numerous half-ERE sites that expands the range of modes by which DNA recognition sites mediate the actions of this nuclear receptor...
  75. ncbi request reprint Regulation of nuclear receptor transcriptional activity by a novel DEAD box RNA helicase (DP97)
    Ramji R Rajendran
    Department of Cell and Structural Biology, University of Illinois, Urbana, Illinois 61801, USA
    J Biol Chem 278:4628-38. 2003
    ..Our findings add to the growing evidence that RNA helicases can associate with nuclear receptors and function as coregulators to modulate receptor transcriptional activity...
  76. ncbi request reprint Lipin1 regulation by estrogen in uterus and liver: implications for diabetes and fertility
    P Mangala Gowri
    University of Illinois, Department of Molecular and Integrative Physiology, 524 Burrill Hall, 407 South Goodwin Avenue, Urbana, Illinois 61801 3704, USA
    Endocrinology 148:3685-93. 2007
    ..Estrogen regulation of lipin1 may provide a mechanistic link between estrogens, lipid metabolism, and lipid signaling...
  77. pmc Haploinsufficiency of the corepressor of estrogen receptor activity (REA) enhances estrogen receptor function in the mammary gland
    Paola Mussi
    Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, TX 77030, USA
    Proc Natl Acad Sci U S A 103:16716-21. 2006
    ..Consequently, a reduction or loss of REA function may cause overactivation of ER and increase breast cancer risk in humans...
  78. ncbi request reprint The androgen derivative 5alpha-androstane-3beta,17beta-diol inhibits prostate cancer cell migration through activation of the estrogen receptor beta subtype
    Vittoria Guerini
    Institute of Endocrinology, University of Milan, Italy
    Cancer Res 65:5445-53. 2005
    ....
  79. ncbi request reprint Metabolite ligands of estrogen receptor-beta reduce primate coronary hyperreactivity
    Rajesh G Mishra
    Dimera Incorporated, 2525 NW Lovejoy, Suite 311, Portland, OR 97210, USA
    Am J Physiol Heart Circ Physiol 290:H295-303. 2006
    ..E3- and 3beta-Adiol-mediated reduction in persistent Ca2+ signals is associated with ER-beta-mediated attenuation of TPR expression and may partly explain estrogen benefits in coronary vascular muscle...
  80. ncbi request reprint Expression of steroid hormone receptors in BRCA1-associated ovarian carcinomas
    Morteza Aghmesheh
    Oncology Research Centre, Prince of Wales Hospital, Randwick, NSW 2031, Australia
    Gynecol Oncol 97:16-25. 2005
    ..However, the expression pattern of ERalpha and other hormone receptors in BRCA1-associated ovarian cancer was unknown...

Research Grants32

  1. ANTIESTROGENS--MECHANISM OF ANTAGONIST ACTION
    Benita Katzenellenbogen; Fiscal Year: 2003
    ..abstract_text> ..
  2. ANTIESTROGENS--MECHANISM OF ANTAGONIST ACTION
    Benita Katzenellenbogen; Fiscal Year: 2000
    ..abstract_text> ..
  3. DOMINANT NEGATIVE ESTROGEN RECEPTORS AND BREAST CANCER
    Benita Katzenellenbogen; Fiscal Year: 2000
    ..I. will introduce the gene- selective DN-ERs into cells using her efficient adenovirus system, determine their effects on gene expression, and examine their importance in ER regulated breast cancer cell proliferation and invasiveness. ..
  4. ANTIESTROGENS--MECHANISM OF ANTAGONIST ACTION
    Benita Katzenellenbogen; Fiscal Year: 2001
    ..abstract_text> ..
  5. DOMINANT NEGATIVE ESTROGEN RECEPTORS AND BREAST CANCER
    Benita Katzenellenbogen; Fiscal Year: 2001
    ..I. will introduce the gene- selective DN-ERs into cells using her efficient adenovirus system, determine their effects on gene expression, and examine their importance in ER regulated breast cancer cell proliferation and invasiveness. ..
  6. ANTIESTROGENS--MECHANISM OF ANTAGONIST ACTION
    Benita Katzenellenbogen; Fiscal Year: 2002
    ..abstract_text> ..
  7. DOMINANT NEGATIVE ESTROGEN RECEPTORS AND BREAST CANCER
    Benita Katzenellenbogen; Fiscal Year: 2002
    ..I. will introduce the gene- selective DN-ERs into cells using her efficient adenovirus system, determine their effects on gene expression, and examine their importance in ER regulated breast cancer cell proliferation and invasiveness. ..
  8. ANTIESTROGENS: MECHANISM OF ANTAGONIST ACTION
    Benita Katzenellenbogen; Fiscal Year: 2004
    ..abstract_text> ..
  9. ANTIESTROGENS: MECHANISM OF ANTAGONIST ACTION
    Benita Katzenellenbogen; Fiscal Year: 2005
    ..abstract_text> ..
  10. ANTIESTROGENS: MECHANISM OF ANTAGONIST ACTION
    Benita Katzenellenbogen; Fiscal Year: 2006
    ..abstract_text> ..
  11. ANTIESTROGENS: MECHANISM OF ANTAGONIST ACTION
    Benita Katzenellenbogen; Fiscal Year: 2007
    ..abstract_text> ..
  12. ANTIESTROGENS--MECHANISM OF ANTAGONIST ACTION
    Benita Katzenellenbogen; Fiscal Year: 1999
    ..abstract_text> ..
  13. DOMINANT NEGATIVE ESTROGEN RECEPTORS AND BREAST CANCER
    Benita Katzenellenbogen; Fiscal Year: 1999
    ..I. will introduce the gene- selective DN-ERs into cells using her efficient adenovirus system, determine their effects on gene expression, and examine their importance in ER regulated breast cancer cell proliferation and invasiveness. ..
  14. ANTIESTROGENS: MECHANISM OF ANTAGONIST ACTION
    Benita Katzenellenbogen; Fiscal Year: 1990
    ..These studies should provide a significant advancement in understanding the mechanism of action of these intriguing and medically important compounds...
  15. DOMINANT NEGATIVE ESTROGEN RECEPTORS AND BREAST CANCER
    Benita Katzenellenbogen; Fiscal Year: 1993
    ....
  16. ANTIESTROGENS: REPRODUCTIVE TISSUE AND TUMOR GROWTH
    Benita Katzenellenbogen; Fiscal Year: 1980
    ..Our studies will assess the interaction of antiestrogens with estrogen receptors in target tissues and their in vivo pharmacokinetic behavior...