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Greene, Geoffrey

One or more keywords matched the following properties of Greene, Geoffrey

Property	Value
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.

Property

Value

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 Type	Name
Concept	Estrogens, Non-Steroidal
Concept	Estrogens, Conjugated (USP)
Concept	Estrogen Antagonists
Concept	Estrogens
Concept	Receptors, Estrogen
Concept	Estrogen Receptor Modulators
Concept	Selective Estrogen Receptor Modulators
Concept	Estrogen Receptor beta
Concept	Estrogen Replacement Therapy
Concept	Estrogen Receptor alpha
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.
Concept	Estrogen Receptor Antagonists
Grant	Development and Characterization of Novel SERMs
Grant	STEROIDS AND GROWTH

Search Criteria

Estrogens