PDBsum entry 4ghi

Transcription

PDB id: 4ghi

Contents

Protein chains

107 a.a.

110 a.a.

Ligands

0X3

Waters ×184

PDB id:

4ghi

Name:

Transcription

Title:

Crystal structure of the high affinity heterodimer of hif2 alpha and arnt c-terminal pas domains in complex with a benzoxadiazole antagonist

Structure:

Endothelial pas domain-containing protein 1. Chain: a. Fragment: c-terminal pas domain, unp residues 239-350. Synonym: 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. Engineered: yes. Mutation: yes.

Source:

Homo sapiens. Human. Organism_taxid: 9606. Gene: bhlhe73, epas1, hif2a, mop2, pasd2. Expressed in: escherichia coli. Expression_system_taxid: 469008. Gene: arnt, bhlhe2.

Resolution:

1.50Å R-factor: 0.170 R-free: 0.196

Authors:

T.H.Scheuermann,J.Key,U.K.Tambar,R.K.Bruick,K.H.Gardner

Key ref:

T.H.Scheuermann et al. (2013). Allosteric inhibition of hypoxia inducible factor-2 with small molecules. Nat Chem Biol, 9, 271-276. PubMed id: 23434853 DOI: 10.1038/nchembio.1185

Date:

07-Aug-12 Release date: 27-Feb-13

Protein chain

Q99814  (EPAS1_HUMAN) -  Endothelial PAS domain-containing protein 1 from Homo sapiens

Seq: 870 a.a.

Struc: 107 a.a.*

Protein chain

P27540  (ARNT_HUMAN) -  Aryl hydrocarbon receptor nuclear translocator from Homo sapiens

Seq: 789 a.a.

Struc: 110 a.a.*

* PDB and UniProt seqs differ at 5 residue positions (black crosses)

DOI no: 10.1038/nchembio.1185

Nat Chem Biol 9:271-276 (2013)

PubMed id: 23434853

Allosteric inhibition of hypoxia inducible factor-2 with small molecules.

T.H.Scheuermann, Q.Li, H.W.Ma, J.Key, L.Zhang, R.Chen, J.A.Garcia, J.Naidoo, J.Longgood, D.E.Frantz, U.K.Tambar, K.H.Gardner, R.K.Bruick.

ABSTRACT

No abstract given.