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Greene, Geoffrey
One or more keywords matched the following properties of Greene, Geoffrey
PropertyValue
keywords Breast Cancer
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
Concept Breast Neoplasms
Academic Article Plasma membrane estrogen receptors exist and functions as dimers.
Academic Article Green tea catechins inhibit angiogenesis through suppression of STAT3 activation.
Academic Article Purification of T47D human progesterone receptor and immunochemical characterization with monoclonal antibodies.
Academic Article Removal of lactate dehydrogenase-elevating virus from human-in-mouse breast tumor xenografts by cell-sorting.
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 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 Inhibition of mammary tumorigenesis in the C3(1)/SV40 mouse model by green tea.
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 Immunohistochemical analysis of estrogen and progesterone receptors in benign breast diseases.
Academic Article Localization of progesterone receptor with monoclonal antibodies to the human progestin receptor.
Academic Article MicroRNA-30c targets cytoskeleton genes involved in breast cancer cell invasion.
Academic Article Examining the pathogenesis of breast cancer using a novel agent-based model of mammary ductal epithelium dynamics.
Academic Article MicroRNA-30c inhibits human breast tumour chemotherapy resistance by regulating TWF1 and IL-11.
Academic Article Estrogen receptor expression in human breast cancer associated with an estrogen receptor gene restriction fragment length polymorphism.
Academic Article Relation of estrogen receptor expression to clonal growth and antiestrogen effects on human breast cancer cells.
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 Subcellular distribution of estrogen receptor and progesterone receptor with and without specific ligand.
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 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 Regulation of progesterone receptor messenger ribonucleic acid and protein levels in MCF-7 cells by estradiol: analysis of estrogen's effect on progesterone receptor synthesis and degradation.
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 progesterone receptor gene maps to human chromosome band 11q13, the site of the mammary oncogene int-2.
Academic Article Progesterone receptor gene restriction fragment length polymorphisms in human breast tumors.
Academic Article Cellular progesterone receptor phosphorylation in response to ligands activating protein kinases.
Academic Article Progesterone receptor distribution in the human endometrium. Analysis using monoclonal antibodies to the human progesterone receptor.
Academic Article Ligand-modulated regulation of progesterone receptor messenger ribonucleic acid and protein in human breast cancer cell lines.
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 use of fine needle aspirates in the evaluation of progesterone receptor content in breast cancer.
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 Estrogen and progesterone receptor structure and action in breast cancer cells.
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 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 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 Cloning of the human oestrogen receptor cDNA.
Academic Article Receptors reconsidered: a 20-year perspective.
Academic Article Monoclonal antibodies localize oestrogen receptor in the nuclei of target cells.
Academic Article 14q32-encoded microRNAs mediate an oligometastatic phenotype.
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 Interferon-Stimulated Genes Are Transcriptionally Repressed by PR in Breast Cancer.
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 Endoxifen, 4-Hydroxytamoxifen and an Estrogenic Derivative Modulate Estrogen Receptor Complex Mediated Apoptosis in Breast Cancer.
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 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 Facilitating Drug Discovery in Breast Cancer by Virtually Screening Patients Using In Vitro Drug Response Modeling.
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 Selective pressure of endocrine therapy activates the integrated stress response through NF?B signaling in a subpopulation of ER positive breast cancer cells.
Academic Article Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells.
Academic Article Endocrine Therapy-Resistant Breast Cancer Cells Are More Sensitive to Ceramide Kinase Inhibition and Elevated Ceramide Levels Than Therapy-Sensitive Breast Cancer Cells.
Academic Article Labeling of a mutant estrogen receptor with an Affimer in a breast cancer cell line.
Academic Article Unconventional isoquinoline-based SERMs elicit fulvestrant-like transcriptional programs in ER+ breast cancer cells.
Academic Article Dynamic epi-transcriptomic landscape mapping with disease progression in estrogen receptor-positive breast cancer.
Grant Development and Characterization of Novel SERMs
Grant BREAST CANCER PLANNING GRANT
Grant STEROIDS AND GROWTH
Academic Article Glucocorticoid Receptor Activation in Lobular Breast Cancer Is Associated with Reduced Cell Proliferation and Promotion of Metastases.
Academic Article ERa/PR crosstalk is altered in the context of the ERa Y537S mutation and contributes to endocrine therapy-resistant tumor proliferation.
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  • Breast Neoplasms