The turnover of estrogen receptor α by the selective estrogen receptor degrader (SERD) fulvestrant is a saturable process that is not required for antagonist efficacy - Wikidata - awgldk - TriplyDB

The turnover of estrogen receptor α by the selective estrogen receptor degrader (SERD) fulvestrant is a saturable process that is not required for antagonist efficacy

The turnover of estrogen receptor α by the selective estrogen receptor degrader (SERD) fulvestrant is a saturable process that is not required for antagonist efficacy

http://www.wikidata.org/entity/Q35027844

about

Steroid hormone receptors and prostate cancer: role of structural dynamics in therapeutic targeting Current medical treatment of estrogen receptor-positive breast cancer Antiestrogens: structure-activity relationships and use in breast cancer treatment Cytochrome P450 1A2 Metabolizes 17β-Estradiol to Suppress Hepatocellular Carcinoma Bazedoxifene exhibits antiestrogenic activity in animal models of tamoxifen-resistant breast cancer: implications for treatment of advanced disease.Ligand-free estrogen receptor activity complements IGF1R to induce the proliferation of the MCF-7 breast cancer cells.17,β-estradiol inhibits hepatitis C virus mainly by interference with the release phase of its life cycle Transcriptional regulation of mixed lineage kinase 3 by estrogen and its implication in ER-positive breast cancer pathogenesis Evaluation of the pharmacological activities of RAD1901, a selective estrogen receptor degrader.RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models.The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer.A Screening Assay Cascade to Identify and Characterize Novel Selective Estrogen Receptor Downregulators (SERDs).Estrogen receptor mutations and their role in breast cancer progression The terminal substituents of 7α, 6-hexanyl derivatives of estradiol determine their selective estrogen receptor modulator versus agonist activities.Research resource: Transcriptional profiling in a cellular model of breast cancer reveals functional and mechanistic differences between clinically relevant SERM and between SERM/estrogen complexes Role of SUMOylation in full antiestrogenicity Efficacy of SERD/SERM Hybrid-CDK4/6 Inhibitor Combinations in Models of Endocrine Therapy-Resistant Breast Cancer.Induction of the Estrogenic Marker Calbindn-D₉k by Octamethylcyclotetrasiloxane Interaction of 14-3-3 proteins with the estrogen receptor alpha F domain provides a drug target interface.Minireview: dynamic structures of nuclear hormone receptors: new promises and challenges.Full antagonism of the estrogen receptor without a prototypical ligand side chain.Environmental Xenoestrogens Super-Activate a Variant Murine ER Beta in Cholangiocytes.Androgen receptor antagonists: a patent review (2008-2011).Palbociclib Combined with Fulvestrant in Premenopausal Women with Advanced Breast Cancer and Prior Progression on Endocrine Therapy: PALOMA-3 Results.Adamantyl Antiestrogens with Novel Side Chains Reveal a Spectrum of Activities in Suppressing Estrogen Receptor Mediated Activities in Breast Cancer Cells.Selective estrogen receptor modulators in clinical practice: a safety overview.Estrogen-activated MDM2 disrupts mammary tissue architecture through a p53-independent pathway.The role of fulvestrant in endometrial cancer.Cholesterol biosynthesis inhibitors as potent novel anti-cancer agents: suppression of hormone-dependent breast cancer by the oxidosqualene cyclase inhibitor RO 48-8071.Effects of the estrogen receptor antagonist fulvestrant on F344 rat prolactinoma models.Biased signalling: from simple switches to allosteric microprocessors.Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity.Application of the CRISPR/Cas9 System to Drug Resistance in Breast Cancer.A quantitative mass spectrometry-based approach to monitor the dynamics of endogenous chromatin-associated protein complexes.

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P2860

The turnover of estrogen receptor α by the selective estrogen receptor degrader (SERD) fulvestrant is a saturable process that is not required for antagonist efficacy

http://www.wikidata.org/entity/Q35027844

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2011 nî lūn-bûn

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2011 թուականի Ապրիլին հրատարակուած գիտական յօդուած

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2011 թվականի ապրիլին հրատարակված գիտական հոդված

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2011年の論文

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2011年論文

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2011年論文

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2011年論文

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2011年論文

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J.BCP.2011.03.031

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Biochemical Pharmacology

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Donald P McDonnell

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Jeffrey R Marks

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Suzanne E Wardell

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P2860

Analysis of Relative Gene Expression Data Using Real-Time Quantitative PCR and the 2−ΔΔCT Method

Structural insights into the mode of action of a pure antiestrogen

AIB1, a steroid receptor coactivator amplified in breast and ovarian cancer

Comparative analyses of mechanistic differences among antiestrogens

Adaptive hypersensitivity to estradiol: potential mechanism for secondary hormonal responses in breast cancer patients.

Activation of the MAPK pathway enhances sensitivity of MCF-7 breast cancer cells to the mitogenic effect of estradiol.

Mechanisms of acquired resistance to endocrine therapy in hormone-dependent breast cancer cells.

Receptor-selective coactivators as tools to define the biology of specific receptor-coactivator pairs.

Distinctive traits of normal and tumor-derived human mammary epithelial cells expressed in a medium that supports long-term growth of both cell types.

A model of acquired autoresistance to a potent ErbB2 tyrosine kinase inhibitor and a therapeutic strategy to prevent its onset in breast cancer

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