登録情報 | データベース: PDB / ID: 6iar |
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タイトル | Tricyclic indazoles a novel class of selective estrogen receptor degrader antagonists |
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要素 | Estrogen receptor |
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キーワード | DNA BINDING PROTEIN / Nuclear Hormone Receptor Inhibitor Downregulation Estrogen receptor modulators |
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機能・相同性 | 機能・相同性情報
regulation of epithelial cell apoptotic process / antral ovarian follicle growth / G protein-coupled estrogen receptor activity / regulation of branching involved in prostate gland morphogenesis / RUNX1 regulates transcription of genes involved in WNT signaling / RUNX1 regulates estrogen receptor mediated transcription / regulation of toll-like receptor signaling pathway / prostate epithelial cord arborization involved in prostate glandular acinus morphogenesis / nuclear estrogen receptor activity / epithelial cell proliferation involved in mammary gland duct elongation ...regulation of epithelial cell apoptotic process / antral ovarian follicle growth / G protein-coupled estrogen receptor activity / regulation of branching involved in prostate gland morphogenesis / RUNX1 regulates transcription of genes involved in WNT signaling / RUNX1 regulates estrogen receptor mediated transcription / regulation of toll-like receptor signaling pathway / prostate epithelial cord arborization involved in prostate glandular acinus morphogenesis / nuclear estrogen receptor activity / epithelial cell proliferation involved in mammary gland duct elongation / epithelial cell development / prostate epithelial cord elongation / negative regulation of smooth muscle cell apoptotic process / mammary gland branching involved in pregnancy / uterus development / vagina development / TFIIB-class transcription factor binding / androgen metabolic process / steroid hormone receptor signaling pathway / mammary gland alveolus development / TFAP2 (AP-2) family regulates transcription of growth factors and their receptors / estrogen receptor signaling pathway / cellular response to estrogen stimulus / estrogen response element binding / : / nuclear receptor-mediated steroid hormone signaling pathway / negative regulation of canonical NF-kappaB signal transduction / Nuclear signaling by ERBB4 / RNA polymerase II preinitiation complex assembly / negative regulation of miRNA transcription / protein localization to chromatin / 14-3-3 protein binding / cellular response to estradiol stimulus / transcription coregulator binding / nitric-oxide synthase regulator activity / steroid binding / TBP-class protein binding / ESR-mediated signaling / transcription corepressor binding / positive regulation of nitric-oxide synthase activity / SUMOylation of intracellular receptors / stem cell differentiation / nuclear estrogen receptor binding / positive regulation of DNA-binding transcription factor activity / Nuclear Receptor transcription pathway / euchromatin / negative regulation of DNA-binding transcription factor activity / Constitutive Signaling by Aberrant PI3K in Cancer / nuclear receptor activity / transcription coactivator binding / beta-catenin binding / positive regulation of fibroblast proliferation / response to estrogen / Regulation of RUNX2 expression and activity / male gonad development / PIP3 activates AKT signaling / positive regulation of nitric oxide biosynthetic process / sequence-specific double-stranded DNA binding / Ovarian tumor domain proteases / regulation of inflammatory response / response to estradiol / ATPase binding / PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling / phospholipase C-activating G protein-coupled receptor signaling pathway / positive regulation of cytosolic calcium ion concentration / DNA-binding transcription activator activity, RNA polymerase II-specific / fibroblast proliferation / transcription regulator complex / Estrogen-dependent gene expression / Extra-nuclear estrogen signaling / calmodulin binding / DNA-binding transcription factor activity, RNA polymerase II-specific / chromatin remodeling / RNA polymerase II cis-regulatory region sequence-specific DNA binding / DNA-binding transcription factor activity / negative regulation of gene expression / chromatin binding / regulation of transcription by RNA polymerase II / positive regulation of DNA-templated transcription / chromatin / regulation of DNA-templated transcription / protein kinase binding / enzyme binding / negative regulation of transcription by RNA polymerase II / Golgi apparatus / signal transduction / positive regulation of transcription by RNA polymerase II / protein-containing complex / zinc ion binding / nucleoplasm / identical protein binding / membrane / nucleus / plasma membrane / cytoplasm / cytosol類似検索 - 分子機能 Estrogen receptor / Oestrogen-type nuclear receptor final C-terminal domain / : / Oestrogen receptor / Oestrogen-type nuclear receptor final C-terminal / Estrogen receptor/oestrogen-related receptor / : / Retinoid X Receptor / Retinoid X Receptor / Nuclear hormone receptor ...Estrogen receptor / Oestrogen-type nuclear receptor final C-terminal domain / : / Oestrogen receptor / Oestrogen-type nuclear receptor final C-terminal / Estrogen receptor/oestrogen-related receptor / : / Retinoid X Receptor / Retinoid X Receptor / Nuclear hormone receptor / Nuclear hormones receptors DNA-binding region signature. / Zinc finger, nuclear hormone receptor-type / Zinc finger, C4 type (two domains) / Nuclear hormone receptors DNA-binding domain profile. / c4 zinc finger in nuclear hormone receptors / Nuclear hormone receptor, ligand-binding domain / Nuclear hormone receptor-like domain superfamily / Nuclear receptor (NR) ligand-binding (LBD) domain profile. / Ligand binding domain of hormone receptors / Zinc finger, NHR/GATA-type / Ligand-binding domain of nuclear hormone receptor / Orthogonal Bundle / Mainly Alpha類似検索 - ドメイン・相同性 |
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生物種 | Homo sapiens (ヒト) |
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手法 | X線回折 / シンクロトロン / 分子置換 / 解像度: 1.84 Å |
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データ登録者 | Scott, J.S. / Bailey, A. / Buttar, D. / Carbajo, R.J. / Curwen, J. / Davies, R.D.M. / Degorce, S.L. / Donald, C. / Gangl, E. / Greenwood, R. ...Scott, J.S. / Bailey, A. / Buttar, D. / Carbajo, R.J. / Curwen, J. / Davies, R.D.M. / Degorce, S.L. / Donald, C. / Gangl, E. / Greenwood, R. / Groombridge, S.D. / Johnson, T. / Lamont, S. / Lawson, M. / Lister, A. / Morrow, C. / Moss, T. / Pink, J.H. / Polanski, R. |
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引用 | ジャーナル: J.Med.Chem. / 年: 2019 タイトル: Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists. 著者: Scott, J.S. / Bailey, A. / Buttar, D. / Carbajo, R.J. / Curwen, J. / Davey, P.R.J. / Davies, R.D.M. / Degorce, S.L. / Donald, C. / Gangl, E. / Greenwood, R. / Groombridge, S.D. / Johnson, T. ...著者: Scott, J.S. / Bailey, A. / Buttar, D. / Carbajo, R.J. / Curwen, J. / Davey, P.R.J. / Davies, R.D.M. / Degorce, S.L. / Donald, C. / Gangl, E. / Greenwood, R. / Groombridge, S.D. / Johnson, T. / Lamont, S. / Lawson, M. / Lister, A. / Morrow, C.J. / Moss, T.A. / Pink, J.H. / Polanski, R. |
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履歴 | 登録 | 2018年11月27日 | 登録サイト: PDBE / 処理サイト: PDBE |
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改定 1.0 | 2019年1月23日 | Provider: repository / タイプ: Initial release |
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改定 1.1 | 2019年2月6日 | Group: Data collection / Database references カテゴリ: citation / citation_author / pdbx_database_proc Item: _citation.title / _citation_author.identifier_ORCID / _citation_author.name |
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改定 1.2 | 2019年4月24日 | Group: Data collection / Database references カテゴリ: citation / database_PDB_rev ...citation / database_PDB_rev / database_PDB_rev_record / pdbx_database_proc Item: _citation.journal_abbrev / _citation.journal_id_ISSN ..._citation.journal_abbrev / _citation.journal_id_ISSN / _citation.journal_volume / _citation.page_first / _citation.page_last |
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改定 1.3 | 2024年5月15日 | Group: Data collection / Database references / Derived calculations カテゴリ: chem_comp_atom / chem_comp_bond ...chem_comp_atom / chem_comp_bond / database_2 / pdbx_struct_assembly / pdbx_struct_assembly_gen / pdbx_struct_assembly_prop / pdbx_struct_oper_list Item: _database_2.pdbx_DOI / _database_2.pdbx_database_accession ..._database_2.pdbx_DOI / _database_2.pdbx_database_accession / _pdbx_struct_assembly.oligomeric_count / _pdbx_struct_assembly.oligomeric_details / _pdbx_struct_assembly_gen.oper_expression / _pdbx_struct_assembly_prop.value |
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Remark 650 | HELIX DETERMINATION METHOD: MOE |
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Remark 700 | SHEET DETERMINATION METHOD: MOE |
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