Search Results - "Greene, Geoffrey L"
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Lasofoxifene as a potential treatment for therapy-resistant ER-positive metastatic breast cancer
Published in Breast cancer research : BCR (12-05-2021)“…Endocrine therapy remains the mainstay of treatment for estrogen receptor-positive (ER+) breast cancer. Constitutively active mutations in the ligand binding…”
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Overcoming mutation-based resistance to antiandrogens with rational drug design
Published in eLife (09-04-2013)“…The second-generation antiandrogen enzalutamide was recently approved for patients with castration-resistant prostate cancer. Despite its success, the duration…”
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3
Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation
Published in eLife (02-02-2016)“…Somatic mutations in the estrogen receptor alpha (ERα) gene (ESR1), especially Y537S and D538G, have been linked to acquired resistance to endocrine therapies…”
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Lasofoxifene as a potential treatment for aromatase inhibitor-resistant ER-positive breast cancer
Published in Breast cancer research : BCR (07-06-2024)“…Breast cancers treated with aromatase inhibitors (AIs) can develop AI resistance, which is often driven by estrogen receptor-alpha (ERα/ESR1) activating…”
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5
Selective pressure of endocrine therapy activates the integrated stress response through NFκB signaling in a subpopulation of ER positive breast cancer cells
Published in Breast cancer research : BCR (09-03-2022)“…While estrogen receptor (ER) positive breast tumors generally respond well to endocrine therapy (ET), up to 40% of patients will experience relapse, either…”
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The SERM/SERD bazedoxifene disrupts ESR1 helix 12 to overcome acquired hormone resistance in breast cancer cells
Published in eLife (29-11-2018)“…Acquired resistance to endocrine therapy remains a significant clinical burden for breast cancer patients. Somatic mutations in the (estrogen receptor alpha…”
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ERα/PR crosstalk is altered in the context of the ERα Y537S mutation and contributes to endocrine therapy-resistant tumor proliferation
Published in NPJ breast cancer (30-11-2023)“…The constitutively active ESR1 Y537S mutation is associated with endocrine therapy (ET) resistance and progression of metastatic breast cancer through its…”
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Discovery of a Glucocorticoid Receptor (GR) Activity Signature Using Selective GR Antagonism in ER-Negative Breast Cancer
Published in Clinical cancer research (15-07-2018)“…Although high glucocorticoid receptor (GR) expression in early-stage estrogen receptor (ER)-negative breast cancer is associated with shortened relapse-free…”
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Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells
Published in eLife (16-05-2022)“…Chemical manipulation of estrogen receptor alpha ligand binding domain structural mobility tunes receptor lifetime and influences breast cancer therapeutic…”
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10
The Lineage Determining Factor GRHL2 Collaborates with FOXA1 to Establish a Targetable Pathway in Endocrine Therapy-Resistant Breast Cancer
Published in Cell reports (Cambridge) (22-10-2019)“…Notwithstanding the positive clinical impact of endocrine therapies in estrogen receptor-alpha (ERα)-positive breast cancer, de novo and acquired resistance…”
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11
Ligand control of coregulator recruitment to nuclear receptors
Published in Annual review of physiology (01-01-2005)“…Nuclear receptors modulate transcription through ligand-mediated recruitment of transcriptional coregulator proteins. The structural connection between ligand…”
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12
The uterine and vascular actions of estetrol delineate a distinctive profile of estrogen receptor α modulation, uncoupling nuclear and membrane activation
Published in EMBO molecular medicine (01-10-2014)“…Estetrol (E 4 ) is a natural estrogen with a long half‐life produced only by the human fetal liver during pregnancy. The crystal structures of the estrogen…”
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MicroRNA-30c targets cytoskeleton genes involved in breast cancer cell invasion
Published in Breast cancer research and treatment (01-01-2013)“…Metastasis remains a significant challenge in treating cancer. A better understanding of the molecular mechanisms underlying metastasis is needed to develop…”
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Reinvestigating the Synthesis and Characterization of Ethyl 3‑[5-(2-Ethoxycarbonyl-1-methylvinyloxy)-1-methyl‑1H‑indol-3-yl]-but-2-enoate
Published in ACS omega (05-09-2023)“…We reinvestigated the reported method for the synthesis of ethyl 3-[5-(2-ethoxycarbonyl-1-methylvinyloxy)-1-methyl-1H-indol-3-yl]-but-2-enoate (MIBE), which…”
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Plasma Membrane Estrogen Receptors Exist and Functions as Dimers
Published in Molecular endocrinology (Baltimore, Md.) (01-12-2004)“…A small pool of estrogen receptors (ERα and -β) localize at the plasma membrane and rapidly signal to affect cellular physiology. Although nuclear ERs function…”
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Capture of associated targets on chromatin links long-distance chromatin looping to transcriptional coordination
Published in Nature communications (16-09-2016)“…Here we describe a sensitive and novel method of identifying endogenous DNA–DNA interactions. Capture of Associated Targets on CHromatin (CATCH) uses efficient…”
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Structural Basis for an Unexpected Mode of SERM-Mediated ER Antagonism
Published in Molecular cell (13-05-2005)“…Tamoxifen is effective for the prevention and treatment of estrogen-dependent breast cancers, but is associated with an increased incidence of endometrial…”
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Cross-talk between the ligand- and DNA-binding domains of estrogen receptor
Published in Proteins, structure, function, and bioinformatics (01-11-2013)“…ABSTRACT Estrogen receptor alpha (ERα) is a hormone‐responsive transcription factor that contains several discrete functional domains, including a…”
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Mapping ERβ genomic binding sites reveals unique genomic features and identifies EBF1 as an ERβ interactor
Published in PloS one (08-08-2013)“…Considerable effort by numerous laboratories has resulted in an improved understanding of estrogen and SERM action mediated by the two estrogen receptors, ERα…”
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Examining the pathogenesis of breast cancer using a novel agent-based model of mammary ductal epithelium dynamics
Published in PloS one (21-05-2013)“…The study of the pathogenesis of breast cancer is challenged by the long time-course of the disease process and the multi-factorial nature of generating…”
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