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One or more keywords matched the following properties of Greene, Geoffrey
keywords Estrogen Receptors
overview The overall objective of my research is to determine the molecular distinctions between estrogen, androgen, progestin, and glucocorticoid agonism and antagonism in hormone-dependent tissues and cancers and to use this information to identify, develop and characterize novel compounds that can be used as breast and prostate cancer chemopreventatives and chemotherapeutics. I have considerable experience and expertise with the identification and characterization of novel compounds (SERMs, SERDs, SPRMs) that selectively target the two estrogen receptors, ERalpha and ERbeta, and progesterone receptor (PR). More recently, my lab has also begun to focus on AR and GR therapeutics. One of our specific goals is to test and develop known and novel SERMs/SARMS/SPRMs/SGRMs for their ability to selectively alter ER/PR, ER/AR and ER/GR recruitment of coregulator subsets that reflect differential responses to these ligands. My lab has solved multiple crystal structures of the ERalpha and ERbeta ligand-binding domains bound to diverse SERMs, which has contributed significantly to our understanding of the structural basis for agonist and antagonist interactions with both ERs, and how the two ER subtypes differentially discriminate among ligands. We have also solved the crystal structure of AR LBD bound to DHT and ERalpha LBD bound to several stapled peptides that bind to and inhibit the transcriptional activating AF2 function of ERalpha. Structural studies are being expanded to include cryoEM analysis of receptor/DNA/coregulator complexes. In addition, we are actively characterizing ERalpha somatic mutations that have been observed in endocrine therapy resistant metastatic breast cancers, with the goal of targeting these mutant ERs with next generation SERMs/SERDs. More recently, we have been studying the role of NCoA3 and other nuclear receptor coregulators as mediators of survival, invasion and metastasis in TNBC. We use and are developing both cell-derived explant and PDX models as platforms for studying both ER+ and ER- breast cancer progression and treatment with existing as well as novel therapy combinations that target multiple steroid receptors and their coregulators. I have a strong background in understanding and modulating breast cancer genesis, progression, treatment and prevention.
One or more keywords matched the following items that are connected to Greene, Geoffrey
Item TypeName
Academic Article Cellular and subcellular studies of the radiation effects of Auger electron-emitting estrogens.
Academic Article Estrogen receptor accessory proteins augment receptor-DNA interaction and DNA bending.
Academic Article Estrogen receptor accessory proteins: effects on receptor-DNA interactions.
Academic Article Structural characterization of a subtype-selective ligand reveals a novel mode of estrogen receptor antagonism.
Academic Article Plasma membrane estrogen receptors exist and functions as dimers.
Academic Article Elemental isomerism: a boron-nitrogen surrogate for a carbon-carbon double bond increases the chemical diversity of estrogen receptor ligands.
Academic Article Structural basis for an unexpected mode of SERM-mediated ER antagonism.
Academic Article Conformation-specific affinity purification of proteins using engineered binding proteins: application to the estrogen receptor.
Academic Article Structure-guided optimization of estrogen receptor binding affinity and antagonist potency of pyrazolopyrimidines with basic side chains.
Academic Article An estrogen receptor-alpha knock-in mutation provides evidence of ligand-independent signaling and allows modulation of ligand-induced pathways in vivo.
Academic Article A structural explanation for ERalpha/ERbeta SERM discrimination.
Academic Article NFkappaB selectivity of estrogen receptor ligands revealed by comparative crystallographic analyses.
Academic Article Estrogen-dependent and -independent estrogen receptor-alpha signaling separately regulate male fertility.
Academic Article Characterization of the ovarian and reproductive abnormalities in prepubertal and adult estrogen non-responsive estrogen receptor alpha knock-in (ENERKI) mice.
Academic Article Recruitment of histone deacetylase 4 to the N-terminal region of estrogen receptor alpha.
Academic Article Molecular characterization of a B-ring unsaturated estrogen: implications for conjugated equine estrogen components of premarin.
Academic Article Modulation of alphaCaMKII signaling by rapid ERalpha action.
Academic Article Screening and association testing of common coding variation in steroid hormone receptor co-activator and co-repressor genes in relation to breast cancer risk: the Multiethnic Cohort.
Academic Article The effects of 17ß-estradiol and a selective estrogen receptor modulator, bazedoxifene, on ovarian carcinogenesis.
Academic Article Estrogen receptor localization in formalin-fixed, paraffin-embedded endometrium and endometriotic tissues.
Academic Article Identification of ligands with bicyclic scaffolds provides insights into mechanisms of estrogen receptor subtype selectivity.
Academic Article Immunocytochemical identification of estrogen receptor in ovarian carcinomas. Localization with monoclonal estrophilin antibodies compared with biochemical assays.
Academic Article Estrogen and progesterone receptor measurements with monoclonal antibodies.
Academic Article The interaction of human estrogen receptor with DNA is modulated by receptor-associated proteins.
Academic Article Structural plasticity in the oestrogen receptor ligand-binding domain.
Academic Article CBP Is a dosage-dependent regulator of nuclear factor-kappaB suppression by the estrogen receptor.
Academic Article RAC3 is a pro-migratory co-activator of ERa.
Academic Article Consensus statement: Expedition Inspiration fund for breast cancer research meeting 2002.
Academic Article Allosteric control of ligand selectivity between estrogen receptors alpha and beta: implications for other nuclear receptors.
Academic Article Immunohistochemical analysis of estrogen and progesterone receptors in benign breast diseases.
Academic Article Immunohistochemical assessment of estrogen receptor distribution in the human endometrium throughout the menstrual cycle.
Academic Article Estrophilin: pro and anti.
Academic Article Immunohistochemical analysis of human uterine estrogen and progesterone receptors throughout the menstrual cycle.
Academic Article In vivo imaging reveals estrogen receptor's hidden personality.
Academic Article Examining the pathogenesis of breast cancer using a novel agent-based model of mammary ductal epithelium dynamics.
Academic Article Estrogen receptor expression in human breast cancer associated with an estrogen receptor gene restriction fragment length polymorphism.
Academic Article A single domain of the estrogen receptor confers deoxyribonucleic acid binding and transcriptional activation of the rat prolactin gene.
Academic Article Estrogen receptor localization in the female genital tract.
Academic Article Immunoelectron microscopic localization of estrogen receptor with monoclonal estrophilin antibodies.
Academic Article Relation of estrogen receptor expression to clonal growth and antiestrogen effects on human breast cancer cells.
Academic Article Immunocytochemical localization of estrogen receptors in the macaque reproductive tract with monoclonal antiestrophilins.
Academic Article An immunocytochemical method for demonstrating estrogen receptor in human uterus using monoclonal antibodies to human estrophilin.
Academic Article Differences between estrogen- and antiestrogen-estrogen receptor complexes from human breast tumors identified with an antibody raised against the estrogen receptor.
Academic Article Detection of the HER-2/neu proto-oncogene protein p185erbB2 by a novel monoclonal antibody (MAB-145ww) in breast cancer membranes from oestrogen and progesterone receptor assays.
Academic Article Estrogen receptor gene methylation in human breast tumors.
Academic Article Estrogen plus progesterone increases progestin receptor immunoreactivity in the brain of ovariectomized guinea pigs.
Academic Article Subcellular distribution of estrogen receptor and progesterone receptor with and without specific ligand.
Academic Article Identification of cysteine 530 as the covalent attachment site of an affinity-labeling estrogen (ketononestrol aziridine) and antiestrogen (tamoxifen aziridine) in the human estrogen receptor.
Academic Article Immunocytochemical assay of progesterone receptors in paraffin-embedded specimens of endometrial carcinoma and hyperplasia: a preliminary evaluation.
Academic Article Prolactin activates ERa in the absence of ligand in female mammary development and carcinogenesis in vivo.
Academic Article Estrogen inhibits vascular smooth muscle cell-dependent adventitial fibroblast migration in vitro.
Academic Article Titration by estrogen receptor activation function-2 of targets that are downstream from coactivators.
Academic Article The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen.
Academic Article Estrogen response elements function as allosteric modulators of estrogen receptor conformation.
Academic Article Molecular characterization by mass spectrometry of the human estrogen receptor ligand-binding domain expressed in Escherichia coli.
Academic Article Estrogen receptor determination in endometrial carcinoma: ligand binding assay versus enzyme immunoassay.
Academic Article Human estrogen receptor bound to an estrogen response element bends DNA.
Academic Article Immunocytochemical determination of estrogen receptor, progesterone receptor, and 1,25-dihydroxyvitamin D3 receptor in breast cancer and relationship to prognosis.
Academic Article Immunocytochemical estrogen and progestin receptor assays in breast cancer with monoclonal antibodies. Histopathologic, demographic, and biochemical correlations and relationship to endocrine response and survival.
Academic Article Regulation of estrogen receptor messenger ribonucleic acid and protein levels in human breast cancer cell lines by sex steroid hormones, their antagonists, and growth factors.
Academic Article Specific binding of estrogen receptor to the estrogen response element.
Academic Article Receptor interconversion model of hormone action. II. Nucleotide-mediated conversion of estrogen receptors from nonsteroid binding to the lower affinity binding state.
Academic Article Sequence and expression of human estrogen receptor complementary DNA.
Academic Article Mapping ERß genomic binding sites reveals unique genomic features and identifies EBF1 as an ERß interactor.
Academic Article Estrogen receptor (alpha and beta) expression in the excurrent ducts of the adult male rat reproductive tract.
Academic Article The ER-positive/PgR-negative breast cancer phenotype is not associated with mutations within the DNA binding domain.
Academic Article An immunohistochemical evaluation of progesterone receptor in frozen sections, paraffin sections, and cytologic imprints of breast carcinomas.
Academic Article Immunocytochemical analysis of estrogen receptors as a predictor of prognosis in breast cancer patients: comparison with quantitative biochemical methods.
Academic Article Immunostaining of estrogen receptor in paraffin sections of breast carcinomas using monoclonal antibody D75P3 gamma: effects of fixation.
Academic Article Structural analysis of covalently labeled estrogen receptors by limited proteolysis and monoclonal antibody reactivity.
Academic Article Immunochemical studies of estrogen receptors.
Academic Article Selection and characterization of a breast cancer cell line resistant to the antiestrogen LY 117018.
Academic Article Characterization of the subunit nature of nuclear estrogen receptors by chemical cross-linking and dense amino acid labeling.
Academic Article Estrogen receptor transformation in MCF-7 breast cancer cells: characterization by immunochemical and sedimentation analyses.
Academic Article Structure and dynamics of the estrogen receptor.
Academic Article Monoclonal antibody recognition of multiple forms of estrogen receptor tagged with [125I]methoxy-iodovinyl estradiol in ovarian carcinomas.
Academic Article Comparison of immunocytochemical and steroid-binding assays for estrogen receptor in human breast tumors.
Academic Article A novel nuclear form of estradiol receptor in MCF-7 human breast cancer cells.
Academic Article The uterine and vascular actions of estetrol delineate a distinctive profile of estrogen receptor a modulation, uncoupling nuclear and membrane activation.
Academic Article Ligand-modulated regulation of progesterone receptor messenger ribonucleic acid and protein in human breast cancer cell lines.
Academic Article Estrogen receptors in the nuclear matrix: direct demonstration using monoclonal antireceptor antibody.
Academic Article Structural organization and regulation of the chicken estrogen receptor.
Academic Article The use of monoclonal antibodies to estrogen receptors (ER) for immunoperoxidase detection of ER in paraffin sections of human breast cancer tissue.
Academic Article Estrogen receptors, antibodies and hormone dependent cancer.
Academic Article The immunoendocrinology of estrophilin.
Academic Article Antibodies to estrogen receptor: immunochemical similarity of estrophilin from various mammalian species.
Academic Article Cross-talk between the ligand- and DNA-binding domains of estrogen receptor.
Academic Article Cell membrane and nuclear estrogen receptors (ERs) originate from a single transcript: studies of ERalpha and ERbeta expressed in Chinese hamster ovary cells.
Academic Article Expression of an estrogen receptor by human coronary artery and umbilical vein endothelial cells.
Academic Article Analysis of the structural core of the human estrogen receptor ligand binding domain by selective proteolysis/mass spectrometric analysis.
Academic Article Immunocytochemical assay for estrogen receptor with monoclonal antibody D753P gamma in routinely processed formaldehyde-fixed breast tissue. Comparison with frozen section assay and with monoclonal antibody H222.
Academic Article Demonstration of steroid hormone receptors and steroid action in primary cultures of rat glial cells.
Academic Article Estrogen and progesterone receptor structure and action in breast cancer cells.
Academic Article Construction of cell lines that express high levels of the human estrogen receptor and are killed by estrogens.
Academic Article Comparison of an immunocytochemical assay for progesterone receptor with a biochemical method of measurement and immunocytochemical examination of the relationship between progesterone and estrogen receptors.
Academic Article Immunohistochemical assessment of estrogen and progesterone receptors in stored imprints and cryostat sections of breast carcinomas.
Academic Article Estrogen and progestin receptors and aromatase activity in rhesus monkey prostate.
Academic Article Estrogen binding, receptor mRNA, and biologic response in osteoblast-like osteosarcoma cells.
Academic Article In memoriam: Elwood Jensen (1920-2012).
Academic Article Estrogen receptor pathways to AP-1.
Academic Article Estrogen receptor immunocytochemistry in endometrial carcinoma: a prognostic marker for survival.
Academic Article Estrogen receptor affinity and location of consensus and imperfect estrogen response elements influence transcription activation of simplified promoters.
Academic Article The limits of the cellular capacity to mediate an estrogen response.
Academic Article Inhibition of estrogen receptor action by a naturally occurring variant in human breast tumors.
Academic Article Interaction of [3H] estradiol - and [3H] monohydroxytamoxifen-estrogen receptor complexes with a monoclonal antibody.
Academic Article ESR1 ligand-binding domain mutations in hormone-resistant breast cancer.
Academic Article Molecular basis of agonism and antagonism in the oestrogen receptor.
Academic Article Cloning of the human estrogen receptor cDNA.
Academic Article Immunochemical studies of estrogen receptors.
Academic Article Monoclonal antibodies as probes for estrogen receptor detection and characterization.
Academic Article Monoclonal antibodies to human estrogen receptor.
Academic Article Monoclonal antibodies to estrophilin: probes for the study of estrogen receptors.
Academic Article Oestrogen receptor function at classical and alternative response elements.
Academic Article Cloning of the human oestrogen receptor cDNA.
Academic Article Recognition of two forms of the estrogen receptor in the guinea-pig uterus at different stages of development by a monoclonal antibody to the human estrogen receptor. Dynamics of the translocation of these two forms to the nucleus.
Academic Article Estrogen receptors in human prostate: evidence for multiple binding sites.
Academic Article Receptors reconsidered: a 20-year perspective.
Academic Article Antibodies to estrophilin: comparison between rabbit and goat antisera.
Academic Article Effect of antibodies to estrogen receptor on the binding of 3H-labeled antiestrogens and androstanediol in the uterus.
Academic Article Monoclonal antibodies localize oestrogen receptor in the nuclei of target cells.
Academic Article Stapled Peptides with ?-Methylated Hydrocarbon Chains for the Estrogen Receptor/Coactivator Interaction.
Academic Article Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation.
Academic Article Genomic agonism and phenotypic antagonism between estrogen and progesterone receptors in breast cancer.
Academic Article Activating ESR1 Mutations Differentially Affect the Efficacy of ER Antagonists.
Academic Article The SERM/SERD bazedoxifene disrupts ESR1 helix 12 to overcome acquired hormone resistance in breast cancer cells.
Academic Article Structural underpinnings of oestrogen receptor mutations in endocrine therapy resistance.
Academic Article A "cross-stitched" peptide with improved helicity and proteolytic stability.
Academic Article Endoxifen, 4-Hydroxytamoxifen and an Estrogenic Derivative Modulate Estrogen Receptor Complex Mediated Apoptosis in Breast Cancer.
Academic Article Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity.
Academic Article Progesterone receptor isoforms, agonists and antagonists differentially reprogram estrogen signaling.
Academic Article Discovery of a Glucocorticoid Receptor (GR) Activity Signature Using Selective GR Antagonism in ER-Negative Breast Cancer.
Academic Article Next-Generation ERa Inhibitors for Endocrine-Resistant ER+ Breast Cancer.
Academic Article Antagonists for Constitutively Active Mutant Estrogen Receptors: Insights into the Roles of Antiestrogen-Core and Side-Chain.
Academic Article The Lineage Determining Factor GRHL2 Collaborates with FOXA1 to Establish a Targetable Pathway in Endocrine Therapy-Resistant Breast Cancer.
Academic Article The NF-?B Pathway Promotes Tamoxifen Tolerance and Disease Recurrence in Estrogen Receptor-Positive Breast Cancers.
Academic Article The Structure-Function Relationship of Angular Estrogens and Estrogen Receptor Alpha to Initiate Estrogen-Induced Apoptosis in Breast Cancer Cells.
Academic Article Rapid Induction of the Unfolded Protein Response and Apoptosis by Estrogen Mimic TTC-352 for the Treatment of Endocrine-Resistant Breast Cancer.
Academic Article Lasofoxifene as a potential treatment for therapy-resistant ER-positive metastatic breast cancer.
Academic Article Defining the Energetic Basis for a Conformational Switch Mediating Ligand-Independent Activation of Mutant Estrogen Receptors in Breast Cancer.
Academic Article A small-molecule activator of the unfolded protein response eradicates human breast tumors in mice.
Academic Article Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells.
Academic Article Labeling of a mutant estrogen receptor with an Affimer in a breast cancer cell line.
Academic Article Dynamic epi-transcriptomic landscape mapping with disease progression in estrogen receptor-positive breast cancer.
Grant Development and Characterization of Novel SERMs
Academic Article Lasofoxifene as a potential treatment for aromatase inhibitor-resistant ER-positive breast cancer.
Search Criteria
  • Estrogens