登録情報 | データベース: PDB / ID: 6mbo |
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タイトル | GLP Methyltransferase with Inhibitor EML741-P212121 Crystal Form |
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要素 | Histone-lysine N-methyltransferase EHMT1 |
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キーワード | TRANSFERASE/TRANSFERASE INHIBITOR / Histone / H3 / Methylation Inhibition / TRANSFERASE / TRANSFERASE-TRANSFERASE INHIBITOR complex |
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機能・相同性 | 機能・相同性情報
[histone H3]-lysine9 N-methyltransferase / peptidyl-lysine monomethylation / peptidyl-lysine dimethylation / histone H3K9 methyltransferase activity / histone H3K9me2 methyltransferase activity / histone H3K27 methyltransferase activity / facultative heterochromatin formation / C2H2 zinc finger domain binding / protein-lysine N-methyltransferase activity / DNA methylation-dependent constitutive heterochromatin formation ...[histone H3]-lysine9 N-methyltransferase / peptidyl-lysine monomethylation / peptidyl-lysine dimethylation / histone H3K9 methyltransferase activity / histone H3K9me2 methyltransferase activity / histone H3K27 methyltransferase activity / facultative heterochromatin formation / C2H2 zinc finger domain binding / protein-lysine N-methyltransferase activity / DNA methylation-dependent constitutive heterochromatin formation / Transcriptional Regulation by E2F6 / regulation of embryonic development / Transcriptional Regulation by VENTX / response to fungicide / Regulation of endogenous retroelements by the Human Silencing Hub (HUSH) complex / 転移酵素; 一炭素原子の基を移すもの; メチル基を移すもの / epigenetic regulation of gene expression / transcription corepressor binding / methyltransferase activity / Regulation of TP53 Activity through Methylation / PKMTs methylate histone lysines / p53 binding / positive regulation of cold-induced thermogenesis / chromatin organization / Senescence-Associated Secretory Phenotype (SASP) / nuclear body / negative regulation of DNA-templated transcription / chromatin / negative regulation of transcription by RNA polymerase II / zinc ion binding / nucleoplasm / nucleus類似検索 - 分子機能 Histone-lysine N-methyltransferase EHMT1 / Histone-lysine N-methyltransferase EHMT1/EHMT2 / : / Histone-lysine N-methyltransferase EHMT1/EHMT2, Cys-rich region / Pre-SET motif / Pre-SET domain / Pre-SET domain profile. / N-terminal to some SET domains / Beta-clip-like / SET domain ...Histone-lysine N-methyltransferase EHMT1 / Histone-lysine N-methyltransferase EHMT1/EHMT2 / : / Histone-lysine N-methyltransferase EHMT1/EHMT2, Cys-rich region / Pre-SET motif / Pre-SET domain / Pre-SET domain profile. / N-terminal to some SET domains / Beta-clip-like / SET domain / Ankyrin repeats (many copies) / SET (Su(var)3-9, Enhancer-of-zeste, Trithorax) domain / SET domain / SET domain superfamily / SET domain profile. / SET domain / Beta Complex / Ankyrin repeats (3 copies) / Ankyrin repeat profile. / Ankyrin repeat region circular profile. / ankyrin repeats / Ankyrin repeat / Ankyrin repeat-containing domain superfamily / Mainly Beta類似検索 - ドメイン・相同性 Chem-JDG / S-ADENOSYL-L-HOMOCYSTEINE / Histone-lysine N-methyltransferase EHMT1類似検索 - 構成要素 |
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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: 1.591 Å |
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データ登録者 | Horton, J.R. / Cheng, X. |
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資金援助 | 米国, 1件 組織 | 認可番号 | 国 |
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National Institutes of Health/National Institute of General Medical Sciences (NIH/NIGMS) | GM049245-23 | 米国 |
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引用 | ジャーナル: J. Med. Chem. / 年: 2019 タイトル: Discovery of a Novel Chemotype of Histone Lysine Methyltransferase EHMT1/2 (GLP/G9a) Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Co-crystal Structure. 著者: Milite, C. / Feoli, A. / Horton, J.R. / Rescigno, D. / Cipriano, A. / Pisapia, V. / Viviano, M. / Pepe, G. / Amendola, G. / Novellino, E. / Cosconati, S. / Cheng, X. / Castellano, S. / Sbardella, G. |
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履歴 | 登録 | 2018年8月30日 | 登録サイト: RCSB / 処理サイト: RCSB |
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改定 1.0 | 2019年2月27日 | Provider: repository / タイプ: Initial release |
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改定 1.1 | 2019年3月27日 | Group: Data collection / Database references / カテゴリ: citation Item: _citation.journal_volume / _citation.page_first ..._citation.journal_volume / _citation.page_first / _citation.page_last / _citation.title |
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改定 1.2 | 2020年1月1日 | Group: Author supporting evidence / カテゴリ: pdbx_audit_support / Item: _pdbx_audit_support.funding_organization |
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改定 1.3 | 2023年10月11日 | Group: Data collection / Database references ...Data collection / Database references / Derived calculations / Refinement description カテゴリ: chem_comp_atom / chem_comp_bond ...chem_comp_atom / chem_comp_bond / database_2 / pdbx_initial_refinement_model / pdbx_struct_conn_angle / struct_conn Item: _database_2.pdbx_DOI / _database_2.pdbx_database_accession ..._database_2.pdbx_DOI / _database_2.pdbx_database_accession / _pdbx_struct_conn_angle.ptnr1_auth_seq_id / _pdbx_struct_conn_angle.ptnr1_label_seq_id / _pdbx_struct_conn_angle.ptnr2_auth_seq_id / _pdbx_struct_conn_angle.ptnr2_label_asym_id / _pdbx_struct_conn_angle.ptnr3_auth_seq_id / _pdbx_struct_conn_angle.ptnr3_label_seq_id / _pdbx_struct_conn_angle.value / _struct_conn.pdbx_dist_value / _struct_conn.ptnr2_auth_seq_id / _struct_conn.ptnr2_label_asym_id |
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