登録情報 | データベース: PDB / ID: 7vqs |
---|
タイトル | Crystal structure of LSD1 in complex with compound 4 |
---|
要素 | Lysine-specific histone demethylase 1A |
---|
キーワード | OXIDOREDUCTASE / DEMETHYLASE / AMINE OXIDASE / CHROMATIN / HISTONE / FAD / MECHANISM-BASED INHIBITOR |
---|
機能・相同性 | 機能・相同性情報
guanine metabolic process / regulation of DNA methylation-dependent heterochromatin formation / protein demethylation / [histone H3]-N6,N6-dimethyl-L-lysine4 FAD-dependent demethylase / FAD-dependent H3K4me/H3K4me3 demethylase activity / demethylase activity / telomeric repeat-containing RNA binding / histone H3K4 demethylase activity / muscle cell development / neuron maturation ...guanine metabolic process / regulation of DNA methylation-dependent heterochromatin formation / protein demethylation / [histone H3]-N6,N6-dimethyl-L-lysine4 FAD-dependent demethylase / FAD-dependent H3K4me/H3K4me3 demethylase activity / demethylase activity / telomeric repeat-containing RNA binding / histone H3K4 demethylase activity / muscle cell development / neuron maturation / positive regulation of neural precursor cell proliferation / regulation of androgen receptor signaling pathway / MRF binding / DNA repair complex / DNA repair-dependent chromatin remodeling / nuclear androgen receptor binding / regulation of double-strand break repair via homologous recombination / positive regulation of neuroblast proliferation / negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediator / positive regulation of stem cell proliferation / negative regulation of DNA binding / histone H3K9 demethylase activity / negative regulation of DNA damage response, signal transduction by p53 class mediator / positive regulation of cell size / histone demethylase activity / positive regulation of epithelial to mesenchymal transition / response to fungicide / cellular response to cAMP / NR1H3 & NR1H2 regulate gene expression linked to cholesterol transport and efflux / nuclear receptor coactivator activity / negative regulation of protein binding / Regulation of PTEN gene transcription / positive regulation of protein ubiquitination / HDACs deacetylate histones / promoter-specific chromatin binding / Activated PKN1 stimulates transcription of AR (androgen receptor) regulated genes KLK2 and KLK3 / HDMs demethylate histones / negative regulation of DNA-binding transcription factor activity / cellular response to gamma radiation / cerebral cortex development / positive regulation of neuron projection development / regulation of protein localization / cellular response to UV / p53 binding / positive regulation of cold-induced thermogenesis / Factors involved in megakaryocyte development and platelet production / flavin adenine dinucleotide binding / DNA-binding transcription factor binding / Estrogen-dependent gene expression / RNA polymerase II-specific DNA-binding transcription factor binding / transcription regulator complex / Potential therapeutics for SARS / chromosome, telomeric region / oxidoreductase activity / transcription coactivator activity / negative regulation of DNA-templated transcription / chromatin binding / chromatin / regulation of transcription by RNA polymerase II / enzyme binding / negative regulation of transcription by RNA polymerase II / positive regulation of transcription by RNA polymerase II / protein-containing complex / nucleoplasm / identical protein binding / nucleus類似検索 - 分子機能 Histone lysine-specific demethylase / SWIRM domain / SWIRM domain / SWIRM domain profile. / Amine oxidase / Flavin containing amine oxidoreductase / Homeobox-like domain superfamily / FAD/NAD(P)-binding domain superfamily / Winged helix-like DNA-binding domain superfamily類似検索 - ドメイン・相同性 Chem-7UQ / FLAVIN-ADENINE DINUCLEOTIDE / L(+)-TARTARIC ACID / Lysine-specific histone demethylase 1A類似検索 - 構成要素 |
---|
生物種 | Homo sapiens (ヒト) |
---|
手法 | X線回折 / シンクロトロン / 分子置換 / 解像度: 2.94 Å |
---|
データ登録者 | Niwa, H. / Koda, Y. / Sato, S. / Yamamoto, H. / Koyama, H. / Umehara, T. |
---|
資金援助 | 日本, 1件 組織 | 認可番号 | 国 |
---|
Japan Society for the Promotion of Science (JSPS) | 20H03388, 20K21406 | 日本 |
|
---|
引用 | ジャーナル: Acs Med.Chem.Lett. / 年: 2022 タイトル: Design and Synthesis of Tranylcypromine-Derived LSD1 Inhibitors with Improved hERG and Microsomal Stability Profiles. 著者: Koda, Y. / Sato, S. / Yamamoto, H. / Niwa, H. / Watanabe, H. / Watanabe, C. / Sato, T. / Nakamura, K. / Tanaka, A. / Shirouzu, M. / Honma, T. / Fukami, T. / Koyama, H. / Umehara, T. |
---|
履歴 | 登録 | 2021年10月20日 | 登録サイト: PDBJ / 処理サイト: PDBJ |
---|
改定 1.0 | 2022年6月1日 | Provider: repository / タイプ: Initial release |
---|
改定 1.1 | 2023年11月29日 | Group: Data collection / Refinement description カテゴリ: chem_comp_atom / chem_comp_bond / pdbx_initial_refinement_model |
---|
|
---|