4BQY
 
 | | HIF prolyl hydroxylase 2 (PHD2/ EGLN1) in complex with Fe(II) and N-[(1-chloro-4-hydroxyisoquinolin-3-yl)carbonyl]alanine | | 分子名称: | (2S)-2-{[(1-chloro-4-hydroxyisoquinolin-3-yl)carbonyl]amino}propanoic acid, EGL NINE HOMOLOG 1, FE (II) ION | | 著者 | Chowdhury, R, McDonough, M.A, Yeoh, K.K, Schofield, C.J. | | 登録日 | 2013-06-03 | | 公開日 | 2013-06-19 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (1.53 Å) | | 主引用文献 | Selective small molecule probes for the hypoxia inducible factor (HIF) prolyl hydroxylases.
ACS Chem. Biol., 8, 2013
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4UWD
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6YVT
 | | HIF prolyl hydroxylase 2 (PHD2/ EGLN1) in complex with MD-253 | | 分子名称: | 2-[[5-(6-methoxynaphthalen-2-yl)-3-oxidanyl-pyridin-2-yl]carbonylamino]ethanoic acid, Egl nine homolog 1, GLYCEROL, ... | | 著者 | Chowdhury, R, Demetriades, M, Schofield, C.J. | | 登録日 | 2020-04-28 | | 公開日 | 2020-05-20 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.847 Å) | | 主引用文献 | Dynamic combinatorial chemistry employing boronic acids/boronate esters leads to potent oxygenase inhibitors.
Angew.Chem.Int.Ed.Engl., 51, 2012
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5OX6
 | | HIF prolyl hydroxylase 2 (PHD2/ EGLN1) in complex with Vadadustat | | 分子名称: | Egl nine homolog 1, GLYCEROL, MANGANESE (II) ION, ... | | 著者 | Chowdhury, R, Zhang, D, Schofield, C.J. | | 登録日 | 2017-09-06 | | 公開日 | 2017-10-18 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.99 Å) | | 主引用文献 | Molecular and cellular mechanisms of HIF prolyl hydroxylase inhibitors in clinical trials.
Chem Sci, 8, 2017
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5OX5
 | | HIF prolyl hydroxylase 2 (PHD2/ EGLN1) in complex with CCT6, a GSK1278863-related compound | | 分子名称: | (6-hydroxy-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carbonyl)glycine, BICARBONATE ION, Egl nine homolog 1, ... | | 著者 | Chowdhury, R, Thinnes, C.C, Schofield, C.J. | | 登録日 | 2017-09-06 | | 公開日 | 2017-10-18 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.251 Å) | | 主引用文献 | Molecular and cellular mechanisms of HIF prolyl hydroxylase inhibitors in clinical trials.
Chem Sci, 8, 2017
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2YBP
 | | JMJD2A COMPLEXED WITH R-2-HYDROXYGLUTARATE AND HISTONE H3K36me3 PEPTIDE (30-41) | | 分子名称: | (2R)-2-hydroxypentanedioic acid, GLYCEROL, HISTONE H3.1T, ... | | 著者 | Chowdhury, R, McDonough, M.A, Schofield, C.J. | | 登録日 | 2011-03-09 | | 公開日 | 2011-03-30 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (2.02 Å) | | 主引用文献 | The oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylases.
EMBO Rep., 12, 2011
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2YC0
 | | FACTOR INHIBITING HIF-1 ALPHA IN COMPLEX WITH R-2-HYDROXYGLUTARATE | | 分子名称: | (2R)-2-hydroxypentanedioic acid, FE (II) ION, GLYCEROL, ... | | 著者 | Chowdhury, R, Clifton, I.J, Schofield, C.J. | | 登録日 | 2011-03-10 | | 公開日 | 2011-03-30 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (2.15 Å) | | 主引用文献 | The oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylases.
EMBO Rep., 12, 2011
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2YBS
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2YDE
 | | FACTOR INHIBITING HIF-1 ALPHA IN COMPLEX WITH S-2-HYDROXYGLUTARATE | | 分子名称: | (2S)-2-HYDROXYPENTANEDIOIC ACID, FE (III) ION, GLYCEROL, ... | | 著者 | Chowdhury, R, Clifton, I.J, Schofield, C.J. | | 登録日 | 2011-03-18 | | 公開日 | 2011-03-30 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (2.28 Å) | | 主引用文献 | The oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylases.
EMBO Rep., 12, 2011
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2YBK
 | | JMJD2A COMPLEXED WITH R-2-HYDROXYGLUTARATE | | 分子名称: | (2R)-2-hydroxypentanedioic acid, CHLORIDE ION, LYSINE-SPECIFIC DEMETHYLASE 4A, ... | | 著者 | Chowdhury, R, McDonough, M.A, Schofield, C.J. | | 登録日 | 2011-03-08 | | 公開日 | 2011-04-06 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | The oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylases.
EMBO Rep., 12, 2011
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4AI9
 | | JMJD2A Complexed with Daminozide | | 分子名称: | CHLORIDE ION, DAMINOZIDE, GLYCEROL, ... | | 著者 | Chowdhury, R, Schofield, C.J. | | 登録日 | 2012-02-08 | | 公開日 | 2012-10-03 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (2.25 Å) | | 主引用文献 | Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases.
J. Med. Chem., 55, 2012
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4AI8
 | | FACTOR INHIBITING HIF-1 ALPHA IN COMPLEX WITH DAMINOZIDE | | 分子名称: | DAMINOZIDE, GLYCEROL, HYPOXIA-INDUCIBLE FACTOR 1-ALPHA INHIBITOR, ... | | 著者 | King, O.N.F, Chowdhury, R, Rose, N.R, McDonough, M.A, Clifton, I.J, Schofield, C.J, Kawamura, A. | | 登録日 | 2012-02-08 | | 公開日 | 2012-10-03 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases.
J. Med. Chem., 55, 2012
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4BIS
 | | JMJD2A COMPLEXED WITH 8-HYDROXYQUINOLINE-4-CARBOXYLIC ACID | | 分子名称: | 8-hydroxyquinoline-4-carboxylic acid, CHLORIDE ION, GLYCEROL, ... | | 著者 | Chowdhury, R, Thinnes, C, Schofield, C.J. | | 登録日 | 2013-04-12 | | 公開日 | 2014-02-05 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (2.493 Å) | | 主引用文献 | 5-Carboxy-8-hydroxyquinoline is a Broad Spectrum 2-Oxoglutarate Oxygenase Inhibitor which Causes Iron Translocation.
Chem Sci, 4, 2013
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4BIO
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4BQW
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4BQX
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4IE0
 | | Crystal structure of the human fat mass and obesity associated protein (FTO) in complex with pyridine-2,4-dicarboxylate (2,4-PDCA) | | 分子名称: | Alpha-ketoglutarate-dependent dioxygenase FTO, GLYCEROL, PYRIDINE-2,4-DICARBOXYLIC ACID, ... | | 著者 | Aik, W.S, McDonough, M.A, Schofield, C.J. | | 登録日 | 2012-12-13 | | 公開日 | 2013-04-03 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.53 Å) | | 主引用文献 | Structural basis for inhibition of the fat mass and obesity associated protein (FTO)
J.Med.Chem., 56, 2013
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4IE5
 | | Crystal structure of the human fat mass and obesity associated protein (FTO) in complex with N-[(3-hydroxypyridin-2-yl)carbonyl]glycine (MD6) | | 分子名称: | Alpha-ketoglutarate-dependent dioxygenase FTO, GLYCEROL, N-[(3-hydroxypyridin-2-yl)carbonyl]glycine, ... | | 著者 | Aik, W.S, McDonough, M.A, Schofield, C.J. | | 登録日 | 2012-12-13 | | 公開日 | 2013-04-03 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | | 主引用文献 | Structural basis for inhibition of the fat mass and obesity associated protein (FTO)
J.Med.Chem., 56, 2013
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4IE6
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4IE7
 | | Crystal structure of the human fat mass and obesity associated protein (FTO) in complex with citrate and rhein (RHN) | | 分子名称: | 4,5-dihydroxy-9,10-dioxo-9,10-dihydroanthracene-2-carboxylic acid, Alpha-ketoglutarate-dependent dioxygenase FTO, CITRATE ANION, ... | | 著者 | Aik, W.S, McDonough, M.A, Schofield, C.J. | | 登録日 | 2012-12-13 | | 公開日 | 2013-04-03 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.6004 Å) | | 主引用文献 | Structural basis for inhibition of the fat mass and obesity associated protein (FTO)
J.Med.Chem., 56, 2013
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4IDZ
 | | Crystal structure of the human fat mass and obesity associated protein (FTO) in complex with N-oxalylglycine (NOG) | | 分子名称: | Alpha-ketoglutarate-dependent dioxygenase FTO, GLYCEROL, N-OXALYLGLYCINE, ... | | 著者 | Aik, W.S, McDonough, M.A, Schofield, C.J. | | 登録日 | 2012-12-13 | | 公開日 | 2013-04-03 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.46 Å) | | 主引用文献 | Structural basis for inhibition of the fat mass and obesity associated protein (FTO)
J.Med.Chem., 56, 2013
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4IE4
 | | Crystal structure of the human fat mass and obesity associated protein (FTO) in complex with 5-carboxy-8-hydroxyquinoline (IOX1) | | 分子名称: | 8-hydroxyquinoline-5-carboxylic acid, Alpha-ketoglutarate-dependent dioxygenase FTO, GLYCEROL, ... | | 著者 | Aik, W.S, McDonough, M.A, Schofield, C.J. | | 登録日 | 2012-12-13 | | 公開日 | 2013-04-03 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.5048 Å) | | 主引用文献 | Structural basis for inhibition of the fat mass and obesity associated protein (FTO)
J.Med.Chem., 56, 2013
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4JHT
 | | Crystal Structure of AlkB in complex with 5-carboxy-8-hydroxyquinoline (IOX1) | | 分子名称: | 8-hydroxyquinoline-5-carboxylic acid, ACETATE ION, Alpha-ketoglutarate-dependent dioxygenase AlkB, ... | | 著者 | Aik, W.S, McDonough, M.A, Schofield, C.J. | | 登録日 | 2013-03-05 | | 公開日 | 2013-06-26 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (1.18 Å) | | 主引用文献 | 5-Carboxy-8-hydroxyquinoline is a Broad Spectrum 2-Oxoglutarate Oxygenase Inhibitor which Causes Iron Translocation.
Chem Sci, 4, 2013
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6QGV
 | | HIF prolyl hydroxylase 2 (PHD2/ EGLN1) in complex with a Spiro[4.5]decanone inhibitor (JPHM-2-167) | | 分子名称: | 8-[(3-methylpyridin-2-yl)methyl]-3-(4-phenylphenyl)-1-pyrimidin-2-yl-1,3,8-triazaspiro[4.5]decane-2,4-dione, Egl nine homolog 1, GLYCEROL, ... | | 著者 | Chowdhury, R, Holt-Martyn, J.P, Rahman, M.Z, Schofield, C.J. | | 登録日 | 2019-01-13 | | 公開日 | 2020-02-05 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (1.4 Å) | | 主引用文献 | Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors.
Medchemcomm, 10, 2019
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6ST3
 | | HIF prolyl hydroxylase 2 (PHD2/ EGLN1) in complex with 4-hydroxy-N-(4-phenoxybenzyl)-2-(1H-pyrazol-1-yl)pyrimidine-5-carboxamide | | 分子名称: | 4-oxidanyl-~{N}-[(4-phenoxyphenyl)methyl]-2-pyrazol-1-yl-pyrimidine-5-carboxamide, Egl nine homolog 1, FORMIC ACID, ... | | 著者 | Chowdhury, R, Holt-Martyn, J.P, Schofield, C.J. | | 登録日 | 2019-09-10 | | 公開日 | 2019-12-04 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.426 Å) | | 主引用文献 | Structure-Activity Relationship and Crystallographic Studies on 4-Hydroxypyrimidine HIF Prolyl Hydroxylase Domain Inhibitors.
Chemmedchem, 15, 2020
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