Brand  (β version)

PDB ID: 4GS9

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Ligands
Code Name Style Show Link
0XB N-(3-fluorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine PoSSuM
PE8 3,6,9,12,15,18,21-heptaoxatricosane-1,23-diol PoSSuM
Non-standard Residues
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Structure summary

Code : 4GS9   PDBj   RCSB PDB   PDBe
Header : TRANSCRIPTION
Title : Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains in complex with an inactive benzoxadiazole antagonist
Release Data : 2013-04-03
Compound :
mol_id molecule chains synonym
1 Endothelial PAS domain-containing protein 1 A EPAS-1, Basic-helix-loop-helix-PAS protein MOP2, Class E basic helix-loop-helix protein 73, bHLHe73, HIF-1-alpha-like factor, HLF, Hypoxia-inducible factor 2-alpha, HIF-2-alpha, HIF2-alpha, Member of PAS protein 2, PAS domain-containing protein 2
fragment: HIF2 PAS-B domain, UNP residues 239-350
mutation: R247E
mol_id molecule chains synonym
2 Aryl hydrocarbon receptor nuclear translocator B ARNT protein, Class E basic helix-loop-helix protein 2, bHLHe2, Dioxin receptor, nuclear translocator, Hypoxia-inducible factor 1-beta, HIF-1-beta, HIF1-beta
fragment: ARNT PAS-B domain, UNP residues 356-470
mutation: E362R
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Escherichia coli  (taxid:469008)
gene: BHLHE73, EPAS1, HIF2, HIF2A, MOP2, PASD2
expression_system_strain: BL21(DE3) CondonPlus
expression_system_vector_type: plasmid
expression_system_plasmid: pHIS-GB1
mol_id organism_scientific organism_common expression_system
2 Homo sapiens  (taxid:9606) Human Escherichia coli  (taxid:469008)
gene: ARNT, BHLHE2
expression_system_strain: BL21(DE3) CondonPlus
expression_system_vector_type: plasmid
expression_system_plasmid: pHIS-GB1
Authors : Scheuermann, T.H., Gardner, K.H.
Keywords : PAS fold, Transcription, protein-protein interactions, nucleus
Exp. method : X-RAY DIFFRACTION ( 1.72 Å )
Citation :

Development of Inhibitors of the PAS-B Domain of the HIF-2 alpha Transcription Factor

Rogers, J.L.,Bayeh, L.,Scheuermann, T.H.  et al.
(2013)  J.Med.Chem.  56 : 1739 - 1747

PubMed: 23363003
DOI: 10.1021/jm301847z

Reaction

Chain : A
UniProt : Q99814 (EPAS1_HUMAN)
Reaction : -
Chain : B
UniProt : P27540 (ARNT_HUMAN)
Reaction : -