3F1P
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![BU of 3f1p by Molmil](/molmil-images/mine/3f1p) | Crystal structure of a high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains | Descriptor: | Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | Authors: | Scheuermann, T.H, Tomchick, D.R, Machius, M, Guo, Y, Bruick, R.K, Gardner, K.H. | Deposit date: | 2008-10-28 | Release date: | 2009-01-20 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (1.17 Å) | Cite: | Artificial ligand binding within the HIF2alpha PAS-B domain of the HIF2 transcription factor. Proc.Natl.Acad.Sci.USA, 106, 2009
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7Q5V
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![BU of 7q5v by Molmil](/molmil-images/mine/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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7Q5X
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![BU of 7q5x by Molmil](/molmil-images/mine/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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3F1N
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![BU of 3f1n by Molmil](/molmil-images/mine/3f1n) | Crystal structure of a high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains, with internally bound ethylene glycol. | Descriptor: | 1,2-ETHANEDIOL, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | Authors: | Scheuermann, T.H, Tomchick, D.R, Machius, M, Guo, Y, Bruick, R.K, Gardner, K.H. | Deposit date: | 2008-10-28 | Release date: | 2009-01-20 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (1.479 Å) | Cite: | Artificial ligand binding within the HIF2alpha PAS-B domain of the HIF2 transcription factor. Proc.Natl.Acad.Sci.USA, 106, 2009
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3H82
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![BU of 3h82 by Molmil](/molmil-images/mine/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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6D0C
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![BU of 6d0c by Molmil](/molmil-images/mine/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
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![BU of 4ghi by Molmil](/molmil-images/mine/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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6X21
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![BU of 6x21 by Molmil](/molmil-images/mine/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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3F1O
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![BU of 3f1o by Molmil](/molmil-images/mine/3f1o) | Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains, with an internally-bound artificial ligand | Descriptor: | 1,2-ETHANEDIOL, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1, ... | Authors: | Scheuermann, T.H, Tomchick, D.R, Machius, M, Guo, Y, Bruick, R.K, Gardner, K.H. | Deposit date: | 2008-10-28 | Release date: | 2009-01-20 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (1.598 Å) | Cite: | Artificial ligand binding within the HIF2alpha PAS-B domain of the HIF2 transcription factor. Proc.Natl.Acad.Sci.USA, 106, 2009
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6CZW
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![BU of 6czw by Molmil](/molmil-images/mine/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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6D0B
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![BU of 6d0b by Molmil](/molmil-images/mine/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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3H7W
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![BU of 3h7w by Molmil](/molmil-images/mine/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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4XT2
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![BU of 4xt2 by Molmil](/molmil-images/mine/4xt2) | Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains in complex with a tetrazole-containing antagonist | Descriptor: | (5S,7R)-5,7-bis(3-bromophenyl)-4,5,6,7-tetrahydrotetrazolo[1,5-a]pyrimidine, Aryl hydrocarbon receptor nuclear translocator, Endothelial PAS domain-containing protein 1 | Authors: | Scheuermann, T.H, Gardner, K.H. | Deposit date: | 2015-01-22 | Release date: | 2015-12-09 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.698 Å) | Cite: | Isoform-Selective and Stereoselective Inhibition of Hypoxia Inducible Factor-2. J.Med.Chem., 58, 2015
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8CK3
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![BU of 8ck3 by Molmil](/molmil-images/mine/8ck3) | STRUCTURE OF HIF2A-ARNT HETERODIMER IN COMPLEX WITH (S)-1-(3,5-Difluoro-phenyl)-5,5-difluoro-3-methanesulfonyl-5,6-dihydro-4H-cyclopenta[c]thiophen-4-ol | Descriptor: | (4~{S})-1-[3,5-bis(fluoranyl)phenyl]-5,5-bis(fluoranyl)-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-4-ol, Aryl hydrocarbon receptor nuclear translocator, DIMETHYL SULFOXIDE, ... | Authors: | Musil, D, Lehmannn, M, Diehl, L. | Deposit date: | 2023-02-14 | Release date: | 2023-07-19 | Last modified: | 2024-06-19 | Method: | X-RAY DIFFRACTION (1.707 Å) | Cite: | Discovery of Cycloalkyl[ c ]thiophenes as Novel Scaffolds for Hypoxia-Inducible Factor-2 alpha Inhibitors. J.Med.Chem., 66, 2023
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4GS9
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![BU of 4gs9 by Molmil](/molmil-images/mine/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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6I7Q
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![BU of 6i7q by Molmil](/molmil-images/mine/6i7q) | |
7UJV
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![BU of 7ujv by Molmil](/molmil-images/mine/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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5TBM
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![BU of 5tbm by Molmil](/molmil-images/mine/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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6D09
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![BU of 6d09 by Molmil](/molmil-images/mine/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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5UFP
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![BU of 5ufp by Molmil](/molmil-images/mine/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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6X28
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![BU of 6x28 by Molmil](/molmil-images/mine/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
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![BU of 6x37 by Molmil](/molmil-images/mine/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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6I7R
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![BU of 6i7r by Molmil](/molmil-images/mine/6i7r) | |
6X2H
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![BU of 6x2h by Molmil](/molmil-images/mine/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
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![BU of 6x3d by Molmil](/molmil-images/mine/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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