5LAT
 
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6YVZ
 | | HIF prolyl hydroxylase 2 (PHD2/ EGLN1) in complex with bicyclic JLS-367 | | Descriptor: | 4-[(5-bromanylisoquinolin-3-yl)amino]-4-oxidanylidene-butanoic acid, BICARBONATE ION, Egl nine homolog 1, ... | | Authors: | Chowdhury, R, Sorensen, J.L, Schofield, C.J. | | Deposit date: | 2020-04-29 | | Release date: | 2020-12-30 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.91 Å) | | Cite: | Use of cyclic peptides to induce crystallization: case study with prolyl hydroxylase domain 2.
Sci Rep, 10, 2020
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5L9B
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6YVW
 | | HIF prolyl hydroxylase 2 (PHD2/ EGLN1) in complex with monocyclic BB-328 | | Descriptor: | 4-[(5-bromanyl-4,6-dimethyl-pyridin-2-yl)amino]-4-oxidanylidene-butanoic acid, Egl nine homolog 1, FE (III) ION, ... | | Authors: | Chowdhury, R, Banerji, B, Schofield, C.J. | | Deposit date: | 2020-04-28 | | Release date: | 2020-12-30 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.97 Å) | | Cite: | Use of cyclic peptides to induce crystallization: case study with prolyl hydroxylase domain 2.
Sci Rep, 10, 2020
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5OX6
 | | HIF prolyl hydroxylase 2 (PHD2/ EGLN1) in complex with Vadadustat | | Descriptor: | Egl nine homolog 1, GLYCEROL, MANGANESE (II) ION, ... | | Authors: | Chowdhury, R, Zhang, D, Schofield, C.J. | | Deposit date: | 2017-09-06 | | Release date: | 2017-10-18 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (1.99 Å) | | Cite: | Molecular and cellular mechanisms of HIF prolyl hydroxylase inhibitors in clinical trials.
Chem Sci, 8, 2017
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3HQR
 | | PHD2:Mn:NOG:HIF1-alpha substrate complex | | Descriptor: | Egl nine homolog 1, Hypoxia-inducible factor 1 alpha, MANGANESE (II) ION, ... | | Authors: | Chowdhury, R, McDonough, M.A, Schofield, C.J. | | Deposit date: | 2009-06-08 | | Release date: | 2009-07-28 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Structural basis for binding of hypoxia-inducible factor to the oxygen-sensing prolyl hydroxylases
Structure, 17, 2009
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2Y33
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6ZBN
 | | HIF Prolyl Hydroxylase 2 (PHD2/EGLN1) in complex with tert-butyl 6-(5-hydroxy-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-1-yl)nicotinate (IOX4) | | Descriptor: | Egl nine homolog 1, GLYCEROL, MANGANESE (II) ION, ... | | Authors: | Figg Jr, W.D, McDonough, M.A, Nakashima, Y, Schofield, C.J. | | Deposit date: | 2020-06-08 | | Release date: | 2021-04-07 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (2.01 Å) | | Cite: | Structural Basis of Prolyl Hydroxylase Domain Inhibition by Molidustat.
Chemmedchem, 16, 2021
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2Y34
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5LAS
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4JZR
 | | Structure of Prolyl Hydroxylase Domain-containing Protein (PHD) with Inhibitors | | Descriptor: | 1,2-ETHANEDIOL, 2-(biphenyl-4-yl)-8-[(1-methyl-1H-imidazol-2-yl)methyl]-2,8-diazaspiro[4.5]decan-1-one, Egl nine homolog 1, ... | | Authors: | Ma, Y, Yang, L. | | Deposit date: | 2013-04-03 | | Release date: | 2013-10-30 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Novel complex crystal structure of prolyl hydroxylase domain-containing protein 2 (PHD2): 2,8-Diazaspiro[4.5]decan-1-ones as potent, orally bioavailable PHD2 inhibitors
Bioorg.Med.Chem., 21, 2013
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6YW2
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4KBZ
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5V18
 | | Structure of PHD2 in complex with 1,2,4-Triazolo-[1,5-a]pyridine | | Descriptor: | 4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile, Egl nine homolog 1, FE (II) ION, ... | | Authors: | Skene, R.J. | | Deposit date: | 2017-03-01 | | Release date: | 2017-06-21 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (2.15 Å) | | Cite: | 1,2,4-Triazolo-[1,5-a]pyridine HIF Prolylhydroxylase Domain-1 (PHD-1) Inhibitors With a Novel Monodentate Binding Interaction.
J. Med. Chem., 60, 2017
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2G1M
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6YW0
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5OX5
 | | HIF prolyl hydroxylase 2 (PHD2/ EGLN1) in complex with CCT6, a GSK1278863-related compound | | Descriptor: | (6-hydroxy-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carbonyl)glycine, BICARBONATE ION, Egl nine homolog 1, ... | | Authors: | Chowdhury, R, Thinnes, C.C, Schofield, C.J. | | Deposit date: | 2017-09-06 | | Release date: | 2017-10-18 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.251 Å) | | Cite: | Molecular and cellular mechanisms of HIF prolyl hydroxylase inhibitors in clinical trials.
Chem Sci, 8, 2017
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6YW3
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3HQU
 | | PHD2:Fe:UN9:partial HIF1-alpha substrate complex | | Descriptor: | Egl nine homolog 1, FE (II) ION, Hypoxia-inducible factor 1 alpha, ... | | Authors: | Chowdhury, R, McDonough, M.A, Schofield, C.J. | | Deposit date: | 2009-06-08 | | Release date: | 2009-07-28 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Structural basis for binding of hypoxia-inducible factor to the oxygen-sensing prolyl hydroxylases
Structure, 17, 2009
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3OUJ
 | | PHD2 with 2-Oxoglutarate | | Descriptor: | 2-OXOGLUTARIC ACID, Egl nine homolog 1, FE (II) ION, ... | | Authors: | Staker, B.L, Arakaki, T.L. | | Deposit date: | 2010-09-14 | | Release date: | 2010-12-01 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Benzimidazole-2-pyrazole HIF Prolyl 4-Hydroxylase Inhibitors as Oral Erythropoietin Secretagogues.
ACS Med Chem Lett, 1, 2010
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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 | | Descriptor: | 4-oxidanyl-~{N}-[(4-phenoxyphenyl)methyl]-2-pyrazol-1-yl-pyrimidine-5-carboxamide, Egl nine homolog 1, FORMIC ACID, ... | | Authors: | Chowdhury, R, Holt-Martyn, J.P, Schofield, C.J. | | Deposit date: | 2019-09-10 | | Release date: | 2019-12-04 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (2.426 Å) | | Cite: | Structure-Activity Relationship and Crystallographic Studies on 4-Hydroxypyrimidine HIF Prolyl Hydroxylase Domain Inhibitors.
Chemmedchem, 15, 2020
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8J1K
 | | co-crystal structure of non-carboxylic acid inhibitor with PHD2 | | Descriptor: | Egl nine homolog 1, MANGANESE (II) ION, N-[(6-cyanopyridin-3-yl)methyl]-5-oxidanyl-2-[(3R)-3-oxidanylpyrrolidin-1-yl]-1,7-naphthyridine-6-carboxamide | | Authors: | Xu, J, Fu, Y, Ding, X, Meng, Q, Wang, L, Zhang, M, Ding, X, Ren, F, Zhavoronkov, A. | | Deposit date: | 2023-04-13 | | Release date: | 2024-04-17 | | Method: | X-RAY DIFFRACTION (2.451 Å) | | Cite: | co-crystal structure of non-carboxylic acid inhibitor with PHD2
To Be Published
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3OUH
 | | PHD2-R127 with JNJ41536014 | | Descriptor: | 1-(5-chloro-6-fluoro-1H-benzimidazol-2-yl)-1H-pyrazole-4-carboxylic acid, Egl nine homolog 1, FE (II) ION, ... | | Authors: | Kim, H, Clark, R. | | Deposit date: | 2010-09-14 | | Release date: | 2010-12-01 | | Last modified: | 2018-04-18 | | Method: | X-RAY DIFFRACTION (2.51 Å) | | Cite: | Benzimidazole-2-pyrazole HIF Prolyl 4-Hydroxylase Inhibitors as Oral Erythropoietin Secretagogues.
ACS Med Chem Lett, 1, 2010
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5LA9
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6YVT
 | | HIF prolyl hydroxylase 2 (PHD2/ EGLN1) in complex with MD-253 | | Descriptor: | 2-[[5-(6-methoxynaphthalen-2-yl)-3-oxidanyl-pyridin-2-yl]carbonylamino]ethanoic acid, Egl nine homolog 1, GLYCEROL, ... | | Authors: | Chowdhury, R, Demetriades, M, Schofield, C.J. | | Deposit date: | 2020-04-28 | | Release date: | 2020-05-20 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (2.847 Å) | | Cite: | Dynamic combinatorial chemistry employing boronic acids/boronate esters leads to potent oxygenase inhibitors.
Angew.Chem.Int.Ed.Engl., 51, 2012
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