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PDB: 110 件

6E1F
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Crystal structure of the SWIRM domain of human histone lysine-specific demethylase LSD1
分子名称: Lysine-specific histone demethylase 1A, SULFATE ION
著者Luka, Z, Pakhomova, S, Reiter, N.J.
登録日2018-07-09
公開日2019-07-10
最終更新日2023-10-11
実験手法X-RAY DIFFRACTION (1.16 Å)
主引用文献Transient and highly ordered structural domains exist within the N-terminus of LSD1 and differentially interact with mononucleosomes
To be Published
5IT3
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Swirm domain of human Lsd1
分子名称: Lysine-specific histone demethylase 1A, MAGNESIUM ION
著者Jeffrey, P.D, Yuan, P.
登録日2016-03-16
公開日2016-05-18
最終更新日2024-03-20
実験手法X-RAY DIFFRACTION (1.4 Å)
主引用文献A Tlx-interacting peptide of Lsd1 inhibits the proliferation of brain tumor stem cells
To Be Published
5AFW
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Assembly of methylated LSD1 and CHD1 drives AR-dependent transcription and translocation
分子名称: 1,2-ETHANEDIOL, CHLORIDE ION, CHROMODOMAIN-HELICASE-DNA-BINDING PROTEIN 1, ...
著者Metzger, E, Willmann, D, McMillan, J, Petroll, K, Metzger, P, Gerhardt, S, vonMaessenhausen, A, Schott, A.K, Espejo, A, Eberlin, A, Wohlwend, D, Schuele, K.M, Schleicher, M, Perner, S, Bedford, M.T, Dengjel, J, Flaig, R, Einsle, O, Schuele, R.
登録日2015-01-26
公開日2016-01-13
最終更新日2024-01-10
実験手法X-RAY DIFFRACTION (1.6 Å)
主引用文献Assembly of Methylated Kdm1A and Chd1 Drives Androgen Receptor-Dependent Transcription and Translocation.
Nat.Struct.Mol.Biol., 23, 2016
7JK7
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Crystal structure of Importin alpha 2 in complex with LSD1 NLS S111E mutant
分子名称: GLYCEROL, Importin subunit alpha-1, Lysine-specific histone demethylase 1A
著者Tu, W.J, McCuaig, R, Tan, A.H.Y, Hardy, K, Seddiki, N, Ali, S, Dahlstron, J.E, Bean, E.G, Dunn, J, Forwood, J.K, Tsimbalyuk, S, Smith, K.M, Yip, D, Malik, L, Prasana, T, Milburn, P, Rao, S.
登録日2020-07-27
公開日2020-08-05
最終更新日2023-10-18
実験手法X-RAY DIFFRACTION (1.96 Å)
主引用文献Targeting Nuclear LSD1 to Reprogram Cancer Cells and Reinvigorate Exhausted T Cells via a Novel LSD1-EOMES Switch.
Front Immunol, 11, 2020
7JJM
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Crystal structure of Importin alpha 2 in complex with LSD1 NLS
分子名称: CHLORIDE ION, Importin subunit alpha-1, Lysine-specific histone demethylase 1A
著者Tu, W.J, McGuaig, R, Tan, H.Y.A, Hardy, C, Seddiki, N, Ali, S, Dahlstrom, J.E, Bean, E.G, Dunn, J, Forwood, J.K, Tsimbalyuk, S, Smith, K.M, Yip, D, Malik, L, Prasana, T, Milburn, P, Rao, S.
登録日2020-07-27
公開日2020-08-05
最終更新日2023-10-18
実験手法X-RAY DIFFRACTION (2.06 Å)
主引用文献Targeting Nuclear LSD1 to Reprogram Cancer Cells and Reinvigorate Exhausted T Cells via a Novel LSD1-EOMES Switch.
Front Immunol, 11, 2020
6KGO
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LSD1-S2157 five-membered ring adduct model
分子名称: 3-[3,5-bis(fluoranyl)-2-phenylmethoxy-phenyl]propanal, FLAVIN-ADENINE DINUCLEOTIDE, GLYCEROL, ...
著者Niwa, H, Sato, S, Umehara, T.
登録日2019-07-12
公開日2020-03-25
最終更新日2024-03-27
実験手法X-RAY DIFFRACTION (2.25 Å)
主引用文献Development and Structural Evaluation of N-Alkylated trans-2-Phenylcyclopropylamine-Based LSD1 Inhibitors.
Chemmedchem, 15, 2020
6KGP
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LSD1-S2157 N5 adduct model
分子名称: 3-[3,5-bis(fluoranyl)-2-phenylmethoxy-phenyl]propanal, FLAVIN-ADENINE DINUCLEOTIDE, GLYCEROL, ...
著者Niwa, H, Sato, S, Umehara, T.
登録日2019-07-12
公開日2020-03-25
最終更新日2024-03-27
実験手法X-RAY DIFFRACTION (2.25 Å)
主引用文献Development and Structural Evaluation of N-Alkylated trans-2-Phenylcyclopropylamine-Based LSD1 Inhibitors.
Chemmedchem, 15, 2020
2Z3Y
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Crystal structure of Lysine-specific demethylase1
分子名称: Lysine-specific histone demethylase 1, [(2R,3S,4R,5R)-5-(6-AMINO-9H-PURIN-9-YL)-3,4-DIHYDROXYTETRAHYDROFURAN-2-YL]METHYL (2R,3S,4S)-5-[7,8-DIMETHYL-2,4-DIOXO-5-(3-PHENYLPROPANOYL)-1,3,4,5-TETRAHYDROBENZO[G]PTERIDIN-10(2H)-YL]-2,3,4-TRIHYDROXYPENTYL DIHYDROGEN DIPHOSPHATE
著者Mimasu, S, Sengoku, T, Umehara, T, Yokoyama, S, RIKEN Structural Genomics/Proteomics Initiative (RSGI)
登録日2007-06-08
公開日2008-01-01
最終更新日2024-03-13
実験手法X-RAY DIFFRACTION (2.25 Å)
主引用文献Crystal structure of histone demethylase LSD1 and tranylcypromine at 2.25A
Biochem.Biophys.Res.Commun., 366, 2008
7E0G
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Crystal structure of Lysine Specific Demethylase 1 (LSD1) with TAK-418, FAD-adduct
分子名称: GLYCEROL, IMIDAZOLE, Lysine-specific histone demethylase 1A, ...
著者Oki, H.
登録日2021-01-28
公開日2021-03-24
最終更新日2023-11-29
実験手法X-RAY DIFFRACTION (2.25 Å)
主引用文献LSD1 enzyme inhibitor TAK-418 unlocks aberrant epigenetic machinery and improves autism symptoms in neurodevelopmental disorder models.
Sci Adv, 7, 2021
2Z5U
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Crystal structure of Lysine-specific histone demethylase 1
分子名称: FAD-trans-2-Phenylcyclopropylamine Adduct, Lysine-specific histone demethylase 1
著者Mimasu, S, Sengoku, T, Yokoyama, S, RIKEN Structural Genomics/Proteomics Initiative (RSGI)
登録日2007-07-17
公開日2008-04-01
最終更新日2023-11-01
実験手法X-RAY DIFFRACTION (2.25 Å)
主引用文献Crystal structure of histone demethylase LSD1 and tranylcypromine at 2.25 A
Biochem.Biophys.Res.Commun., 366, 2008
7XW8
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Crystal structure of Lysine Specific Demethylase 1 (LSD1) with TAK-418 distomer, FAD-adduct
分子名称: GLYCEROL, Lysine-specific histone demethylase 1A, MAGNESIUM ION, ...
著者Oki, H.
登録日2022-05-26
公開日2022-10-12
最終更新日2023-11-29
実験手法X-RAY DIFFRACTION (2.28 Å)
主引用文献Design, synthesis, and structure-activity relationship of TAK-418 and its derivatives as a novel series of LSD1 inhibitors with lowered risk of hematological side effects.
Eur.J.Med.Chem., 239, 2022
2DW4
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Crystal structure of human LSD1 at 2.3 A resolution
分子名称: FLAVIN-ADENINE DINUCLEOTIDE, Lysine-specific histone demethylase 1
著者Sengoku, T, Yokoyama, S, RIKEN Structural Genomics/Proteomics Initiative (RSGI)
登録日2006-08-02
公開日2007-09-04
最終更新日2024-03-13
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Crystal structure of histone demethylase LSD1 and tranylcypromine at 2.25A
Biochem.Biophys.Res.Commun., 366, 2008
6KGR
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LSD1-FCPA-MPE N5 adduct model
分子名称: (4S)-2-METHYL-2,4-PENTANEDIOL, 3-[4-[5-fluoranyl-2-(trifluoromethyl)phenyl]phenyl]propanal, FLAVIN-ADENINE DINUCLEOTIDE, ...
著者Niwa, H, Sato, S, Handa, N, Umehara, T.
登録日2019-07-12
公開日2020-03-25
最終更新日2024-03-27
実験手法X-RAY DIFFRACTION (2.32 Å)
主引用文献Development and Structural Evaluation of N-Alkylated trans-2-Phenylcyclopropylamine-Based LSD1 Inhibitors.
Chemmedchem, 15, 2020
6KGQ
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LSD1-FCPA-MPE five-membered ring adduct model
分子名称: (4S)-2-METHYL-2,4-PENTANEDIOL, 3-[4-[5-fluoranyl-2-(trifluoromethyl)phenyl]phenyl]propanal, FLAVIN-ADENINE DINUCLEOTIDE, ...
著者Niwa, H, Sato, S, Handa, N, Umehara, T.
登録日2019-07-12
公開日2020-03-25
最終更新日2024-03-27
実験手法X-RAY DIFFRACTION (2.32 Å)
主引用文献Development and Structural Evaluation of N-Alkylated trans-2-Phenylcyclopropylamine-Based LSD1 Inhibitors.
Chemmedchem, 15, 2020
7W3L
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Crystal structure of LSD1 in complex with cis-4-Br-2,5-F2-PCPA (S1024)
分子名称: 3-[4-bromanyl-2,5-bis(fluoranyl)phenyl]propanal, FLAVIN-ADENINE DINUCLEOTIDE, GLYCEROL, ...
著者Niwa, H, Sato, S, Umehara, T.
登録日2021-11-25
公開日2022-09-14
最終更新日2023-11-29
実験手法X-RAY DIFFRACTION (2.51 Å)
主引用文献Structure-Activity Relationship and In Silico Evaluation of cis- and trans-PCPA-Derived Inhibitors of LSD1 and LSD2
Acs Med.Chem.Lett., 13, 2022
5H6Q
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Crystal structure of LSD1-CoREST in complex with peptide 11
分子名称: FLAVIN-ADENINE DINUCLEOTIDE, GLYCEROL, Lysine-specific histone demethylase 1A, ...
著者Kikuchi, M, Amano, Y, Sato, S, Yokoyama, S, Umezawa, N, Higuchi, T, Umehara, T.
登録日2016-11-14
公開日2017-04-12
最終更新日2023-11-08
実験手法X-RAY DIFFRACTION (2.53 Å)
主引用文献Development and crystallographic evaluation of histone H3 peptide with N-terminal serine substitution as a potent inhibitor of lysine-specific demethylase 1.
Bioorg. Med. Chem., 25, 2017
2IW5
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Structural Basis for CoREST-Dependent Demethylation of Nucleosomes by the Human LSD1 Histone Demethylase
分子名称: AMMONIUM ION, CHLORIDE ION, FLAVIN-ADENINE DINUCLEOTIDE, ...
著者Yang, M, Gocke, C.B, Luo, X, Borek, D, Tomchick, D.R, Machius, M, Otwinowski, Z, Yu, H.
登録日2006-06-26
公開日2006-08-09
最終更新日2024-05-08
実験手法X-RAY DIFFRACTION (2.57 Å)
主引用文献Structural Basis for Corest-Dependent Demethylation of Nucleosomes by the Human Lsd1 Histone Demethylase
Mol.Cell, 23, 2006
5L3D
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Human LSD1/CoREST: LSD1 Y761H mutation
分子名称: FLAVIN-ADENINE DINUCLEOTIDE, Lysine-specific histone demethylase 1A, REST corepressor 1
著者Pilotto, S, Speranzini, V, Marabelli, C, Mattevi, A.
登録日2016-04-06
公開日2016-05-04
最終更新日2024-05-08
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献LSD1/KDM1A mutations associated to a newly described form of intellectual disability impair demethylase activity and binding to transcription factors.
Hum.Mol.Genet., 25, 2016
7JJL
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Crystal structure of Importin Alpha 3 in complex with human LSD1 NLS
分子名称: Importin subunit alpha-3, Lysine-specific histone demethylase 1A
著者Tu, W.J, McCuaig, R, Tan, H.Y.A, Hardy, K, Seddiki, N, Ali, S, Dahlstrom, J.E, Bean, E.G, Dunn, J, Forwood, J.K, Tsimbalyuk, S, Smith, K, Yip, D, Malik, L, Prasana, T, Milburn, P, Rao, S.
登録日2020-07-27
公開日2020-08-05
最終更新日2023-10-18
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Targeting Nuclear LSD1 to Reprogram Cancer Cells and Reinvigorate Exhausted T Cells via a Novel LSD1-EOMES Switch.
Front Immunol, 11, 2020
8Q1G
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LSD1-CoREST bound to Acetylated K14 of Histone H3
分子名称: FLAVIN-ADENINE DINUCLEOTIDE, Histone H3.3C, Lysine-specific histone demethylase 1A, ...
著者Barone, M, Mattevi, A.
登録日2023-07-31
公開日2024-05-15
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Uncoupling Histone Modification Crosstalk by Engineering Lysine Demethylase LSD1
To Be Published
6TUY
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Human LSD1/CoREST bound to the quinazoline inhibitor MC4106
分子名称: CHLORIDE ION, DIMETHYL SULFOXIDE, FLAVIN-ADENINE DINUCLEOTIDE, ...
著者Mattevi, A, Marrocco, B.
登録日2020-01-08
公開日2021-07-21
最終更新日2024-01-24
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models.
Eur.J.Med.Chem., 237, 2022
5H6R
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Crystal structure of LSD1-CoREST in complex with peptide 13
分子名称: FLAVIN-ADENINE DINUCLEOTIDE, GLYCEROL, Lysine-specific histone demethylase 1A, ...
著者Kkuchi, M, Amano, Y, Sato, S, Yokoyama, S, Umezawa, N, Higuchi, T, Umehara, T.
登録日2016-11-14
公開日2017-04-12
最終更新日2023-11-15
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Development and crystallographic evaluation of histone H3 peptide with N-terminal serine substitution as a potent inhibitor of lysine-specific demethylase 1.
Bioorg. Med. Chem., 25, 2017
6KGN
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LSD1-CoREST-S2116 N5 adduct model
分子名称: 3-[3,5-bis(fluoranyl)-2-phenylmethoxy-phenyl]propanal, FLAVIN-ADENINE DINUCLEOTIDE, GLYCEROL, ...
著者Niwa, H, Sato, S, Umehara, T.
登録日2019-07-12
公開日2020-03-25
最終更新日2024-03-27
実験手法X-RAY DIFFRACTION (2.62 Å)
主引用文献Development and Structural Evaluation of N-Alkylated trans-2-Phenylcyclopropylamine-Based LSD1 Inhibitors.
Chemmedchem, 15, 2020
8INL
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LSD1 in complex with S2172
分子名称: 3-[3,5-bis(fluoranyl)-2-phenylmethoxy-phenyl]propanal, FLAVIN-ADENINE DINUCLEOTIDE, GLYCEROL, ...
著者Niwa, H, Sato, S, Umehara, T.
登録日2023-03-10
公開日2024-03-13
実験手法X-RAY DIFFRACTION (2.62 Å)
主引用文献LSD1 in complex with S2172
To Be Published
6KGM
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LSD1-CoREST-S2116 five-membered ring adduct model
分子名称: 3-[3,5-bis(fluoranyl)-2-phenylmethoxy-phenyl]propanal, FLAVIN-ADENINE DINUCLEOTIDE, GLYCEROL, ...
著者Niwa, H, Sato, S, Umehara, T.
登録日2019-07-12
公開日2020-03-25
最終更新日2024-03-27
実験手法X-RAY DIFFRACTION (2.62 Å)
主引用文献Development and Structural Evaluation of N-Alkylated trans-2-Phenylcyclopropylamine-Based LSD1 Inhibitors.
Chemmedchem, 15, 2020

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