5UFP
 
 | | Crystal structure of PT2399 bound to HIF2a-B*:ARNT-B* complex | | Descriptor: | 3-({(1S)-7-[(difluoromethyl)sulfonyl]-2,2-difluoro-1-hydroxy-2,3-dihydro-1H-inden-4-yl}oxy)-5-fluorobenzonitrile, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | | Authors: | Du, X. | | Deposit date: | 2017-01-05 | | Release date: | 2017-01-25 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | On-target efficacy of a HIF-2 alpha antagonist in preclinical kidney cancer models.
Nature, 539, 2016
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7UJV
 | | Structure of PHD2 in complex with HIF2a-CODD | | Descriptor: | Egl nine homolog 1, Endothelial PAS domain-containing protein 1, FE (III) ION, ... | | Authors: | Ferens, F.G, Tarade, D, Lee, J.E, Ohh, M. | | Deposit date: | 2022-03-31 | | Release date: | 2023-04-05 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Deficiency in PHD2-mediated hydroxylation of HIF2 alpha underlies Pacak-Zhuang syndrome.
Commun Biol, 7, 2024
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7Q5X
 | | HIF PROLYL HYDROXYLASE 2 (PHD2/EGLN1) IN COMPLEX WITH 2-OXOGLUTARATE (2OG) AND HIF-2 ALPHA CODD (523-542) | | Descriptor: | 2-OXOGLUTARIC ACID, CHLORIDE ION, DI(HYDROXYETHYL)ETHER, ... | | Authors: | Figg Jr, W.D, McDonough, M.A, Chowdhury, R, Nakashima, Y, Schofield, C.J. | | Deposit date: | 2021-11-04 | | Release date: | 2022-11-16 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (1.21 Å) | | Cite: | Structural basis for binding of the renal carcinoma target hypoxia-inducible factor 2 alpha to prolyl hydroxylase domain 2.
Proteins, 91, 2023
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7Q5V
 | | HIF PROLYL HYDROXYLASE 2 (PHD2/EGLN1) IN COMPLEX WITH N-OXALYLGLYCINE (NOG) AND HIF-2 ALPHA CODD (523-542) | | Descriptor: | CHLORIDE ION, DI(HYDROXYETHYL)ETHER, Egl nine homolog 1, ... | | Authors: | Figg Jr, W.D, McDonough, M.A, Chowdhury, R, Nakashima, Y, Schofield, C.J. | | Deposit date: | 2021-11-04 | | Release date: | 2022-11-16 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (1.17 Å) | | Cite: | Structural basis for binding of the renal carcinoma target hypoxia-inducible factor 2 alpha to prolyl hydroxylase domain 2.
Proteins, 91, 2023
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5KIZ
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1P97
 | | NMR structure of the C-terminal PAS domain of HIF2a | | Descriptor: | Endothelial PAS domain protein 1 | | Authors: | Erbel, P.J, Card, P.B, Karakuzu, O, Bruick, R.K, Gardner, K.H. | | Deposit date: | 2003-05-09 | | Release date: | 2004-01-13 | | Last modified: | 2022-02-23 | | Method: | SOLUTION NMR | | Cite: | Structural basis for PAS domain heterodimerization in the basic helix-loop-helix-PAS transcription factor hypoxia-inducible factor.
Proc.Natl.Acad.Sci.USA, 100, 2003
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5TBM
 | | Crystal structure of PT2385 bound to HIF2a-B*:ARNT-B* complex | | Descriptor: | 3-{[(1S)-2,2-difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1H-inden-4-yl]oxy}-5-fluorobenzonitrile, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | | Authors: | Du, X. | | Deposit date: | 2016-09-12 | | Release date: | 2016-09-21 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | A Small-Molecule Antagonist of HIF2 alpha Is Efficacious in Preclinical Models of Renal Cell Carcinoma.
Cancer Res., 76, 2016
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7W80
 | | Crystal Structure of the Heterodimeric HIF-2 in Complex with Antagonist Belzutifan | | Descriptor: | 3-{[(1S,2S,3R)-2,3-difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1H-inden-4-yl]oxy}-5-fluorobenzonitrile, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | | Authors: | Ren, X, Diao, X, Zhuang, J, Wu, D. | | Deposit date: | 2021-12-07 | | Release date: | 2022-09-21 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.754 Å) | | Cite: | Structural basis for the allosteric inhibition of hypoxia-inducible factor (HIF)-2 by belzutifan.
Mol.Pharmacol., 2022
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4PKY
 | | ARNT/HIF transcription factor/coactivator complex | | Descriptor: | Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1, SULFATE ION, ... | | Authors: | Tomchick, D.R, Partch, C.L, Gardner, K.H. | | Deposit date: | 2014-05-15 | | Release date: | 2015-02-11 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Coiled-coil Coactivators Play a Structural Role Mediating Interactions in Hypoxia-inducible Factor Heterodimerization.
J.Biol.Chem., 290, 2015
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6CZW
 | | Crystal structure of PT1940 bound to HIF2a-B*:ARNT-B* complex | | Descriptor: | Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1, {2-bromo-3-(3-chloro-5-fluorophenoxy)-6-[(difluoromethyl)sulfonyl]phenyl}methanol | | Authors: | Du, X. | | Deposit date: | 2018-04-09 | | Release date: | 2018-10-31 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | Crystal structure of PT1940 bound to HIF2a-B*:ARNT-B* complex
To Be Published
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6D09
 | | Crystal structure of PT2440 bound to HIF2a-B*:ARNT-B* complex | | Descriptor: | 3-{[(3R)-4-(difluoromethyl)-2,2-difluoro-3-hydroxy-1,1-dioxo-2,3-dihydro-1H-1-benzothiophen-5-yl]oxy}-5-fluorobenzonitrile, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | | Authors: | Du, X. | | Deposit date: | 2018-04-10 | | Release date: | 2018-10-31 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | Crystal structure of PT1940 bound to HIF2a-B*:ARNT-B* complex
To Be Published
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6D0B
 | | Crystal structure of PT1614 bound to HIF2a-B*:ARNT-B* complex | | Descriptor: | Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1, N-(3-chloro-5-fluorophenyl)-2-nitro-4-[(trifluoromethyl)sulfonyl]aniline | | Authors: | Du, X. | | Deposit date: | 2018-04-10 | | Release date: | 2018-10-31 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | Crystal structure of PT1614 bound to HIF2a-B*:ARNT-B* complex
To Be Published
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6D0C
 | | Crystal structure of HIF2a-B*:ARNT-B* complex | | Descriptor: | Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | | Authors: | Du, X. | | Deposit date: | 2018-04-10 | | Release date: | 2018-10-31 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | Crystal structure of PT1940 bound to HIF2a-B*:ARNT-B* complex
To Be Published
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4GHI
 | | Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains in complex with a benzoxadiazole antagonist | | Descriptor: | Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1, N-(3-chloro-5-fluorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine | | Authors: | Scheuermann, T.H, Key, J, Tambar, U.K, Bruick, R.K, Gardner, K.H. | | Deposit date: | 2012-08-07 | | Release date: | 2013-02-27 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | Allosteric inhibition of hypoxia inducible factor-2 with small molecules.
Nat.Chem.Biol., 9, 2013
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3H82
 | | Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains with the artificial ligand THS020 | | Descriptor: | Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1, N-(furan-2-ylmethyl)-2-nitro-4-(trifluoromethyl)aniline | | Authors: | Key, J.M, Scheuermann, T.H, Anderson, P.C, Daggett, V, Gardner, K.H. | | Deposit date: | 2009-04-28 | | Release date: | 2010-01-12 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | Principles of ligand binding within a completely buried cavity in HIF2alpha PAS-B
J.Am.Chem.Soc., 131, 2009
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3H7W
 | | Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains with the artificial ligand THS017 | | Descriptor: | 2-nitro-N-(thiophen-3-ylmethyl)-4-(trifluoromethyl)aniline, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | | Authors: | Key, J.M, Scheuermann, T.H, Anderson, P.C, Daggett, V, Gardner, K.H. | | Deposit date: | 2009-04-28 | | Release date: | 2010-01-12 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (1.65 Å) | | Cite: | Principles of ligand binding within a completely buried cavity in HIF2alpha PAS-B
J.Am.Chem.Soc., 131, 2009
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4GS9
 | | Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains in complex with an inactive benzoxadiazole antagonist | | Descriptor: | 3,6,9,12,15,18,21-HEPTAOXATRICOSANE-1,23-DIOL, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1, ... | | Authors: | Scheuermann, T.H, Gardner, K.H. | | Deposit date: | 2012-08-27 | | Release date: | 2013-04-03 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (1.72 Å) | | Cite: | Development of Inhibitors of the PAS-B Domain of the HIF-2 alpha Transcription Factor
J.Med.Chem., 56, 2013
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6X28
 | | Crystal structure of PT2243 bound to HIF2a-B*:ARNT-B* complex | | Descriptor: | (1R)-4-(3,5-difluorophenoxy)-7-(trifluoromethyl)-2,3-dihydro-1H-inden-1-ol, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | | Authors: | Du, X. | | Deposit date: | 2020-05-20 | | Release date: | 2021-05-26 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.92 Å) | | Cite: | Crystal structure of PT2243 bound to HIF2-PasB*:ARNT-PasB* complex
To Be Published
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6X37
 | | Crystal structure of PT3245 bound to HIF2a-B*:ARNT-B* complex | | Descriptor: | 3-fluoro-5-{[(7R)-7-hydroxy-1-(trifluoromethyl)-6,7-dihydro-5H-cyclopenta[c]pyridin-4-yl]oxy}benzonitrile, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | | Authors: | Du, X. | | Deposit date: | 2020-05-21 | | Release date: | 2021-05-26 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.94 Å) | | Cite: | Crystal structure of PT3245 bound to HIF2a-B*:ARNT-B* complex
To Be Published
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6X2H
 | | Crystal structure of PT2863 bound to HIF2a-B*:ARNT-B* complex | | Descriptor: | Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1, cis-3-({(1S)-7-[dihydroxy(trifluoromethyl)-lambda~4~-sulfanyl]-2,2-difluoro-1-hydroxy-2,3-dihydro-1H-inden-4-yl}oxy)cyclobutane-1-carbonitrile | | Authors: | Du, X. | | Deposit date: | 2020-05-20 | | Release date: | 2021-05-26 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Crystal structure of PT2863 bound to HIF2a-B*:ARNT-B* complex
To Be Published
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6X3D
 | | Crystal structure of PT3388 bound to HIF2a-B*:ARNT-B* complex | | Descriptor: | (6R,7S)-4-[(3,3-difluorocyclobutyl)oxy]-6-fluoro-1-(trifluoromethyl)-6,7-dihydro-5H-cyclopenta[c]pyridin-7-ol, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | | Authors: | Du, X. | | Deposit date: | 2020-05-21 | | Release date: | 2021-05-26 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Crystal structure of PT3388 bound to HIF2a-B*:ARNT-B* complex
To Be Published
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6X21
 | | Crystal structure of PT1673 bound to HIF2a-B*:ARNT-B* complex | | Descriptor: | 1-(3-bromo-5-fluorophenoxy)-4-[(difluoromethyl)sulfonyl]-2-nitrobenzene, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | | Authors: | Du, X. | | Deposit date: | 2020-05-19 | | Release date: | 2021-05-26 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.54 Å) | | Cite: | Crystal structure of PT1673 bound to HIF2a-B*:ARNT-B* complex
To Be Published
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6E3S
 | | Crystal Structure of the Heterodimeric HIF-2 Complex with Antagonist PT2385 | | Descriptor: | 3-{[(1S)-2,2-difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1H-inden-4-yl]oxy}-5-fluorobenzonitrile, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | | Authors: | Wu, D, Su, X, Lu, J, Li, S, Hood, B, Vasile, S, Potluri, N, Diao, X, Kim, Y, Khorasanizadeh, S, Rastinejad, F. | | Deposit date: | 2018-07-15 | | Release date: | 2019-02-13 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Bidirectional modulation of HIF-2 activity through chemical ligands.
Nat. Chem. Biol., 15, 2019
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6E3T
 | | Crystal Structure of the Heterodimeric HIF-2 Complex with Antagonist T1001 | | Descriptor: | (6S)-6-(4-bromophenyl)-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | | Authors: | Wu, D, Su, X, Lu, J, Li, S, Hood, B, Vasile, S, Potluri, N, Diao, X, Kim, Y, Khorasanizadeh, S, Rastinejad, F. | | Deposit date: | 2018-07-15 | | Release date: | 2019-02-13 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Bidirectional modulation of HIF-2 activity through chemical ligands.
Nat. Chem. Biol., 15, 2019
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6E3U
 | | Crystal Structure of the Heterodimeric HIF-2 Complex with Agonist M1001 | | Descriptor: | 3-{[2-(pyrrolidin-1-yl)phenyl]amino}-1H-1lambda~6~,2-benzothiazole-1,1-dione, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | | Authors: | Wu, D, Su, X, Lu, J, Li, S, Hood, B, Vasile, S, Potluri, N, Diao, X, Kim, Y, Khorasanizadeh, S, Rastinejad, F. | | Deposit date: | 2018-07-15 | | Release date: | 2019-02-13 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.85 Å) | | Cite: | Bidirectional modulation of HIF-2 activity through chemical ligands.
Nat. Chem. Biol., 15, 2019
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