› 2b7a

X-ray diffraction
2Å resolution

The structural basis of Janus Kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor

Released:
DOI: 10.2210/pdb2b7a/pdb
PDB entry 2b7a coloured by chain, front view.
PDB entry 2b7a coloured by chain, side view.
PDB entry 2b7a coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor.
Lucet IS, Fantino E, Styles M, Bamert R, Patel O, Broughton SE, Walter M, Burns CJ, Treutlein H, Wilks AF, Rossjohn J
Blood 107 176-83 (2006)
PMID: 16174768

Function and Biology Details

Reaction catalysed: 
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
Biochemical function:
Biological process:
Cellular component:
  • not assigned
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-130063 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Tyrosine-protein kinase JAK2 Chains: A, B
Molecule details ›
Chains: A, B
Length: 293 amino acids
Theoretical weight: 34.59 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: O60674 (Residues: 840-1132; Coverage: 26%)
Gene name: JAK2
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

1 bound ligand:
Ligand IZA 2 x IZA
1 modified residue:
Ligand PTR 4 x PTR

Experiments and Validation Details

Entry percentile scores
X-ray source: RIGAKU RU300
Spacegroup: P41
Unit cell:
a: 111.273Å b: 111.273Å c: 70.577Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.211 0.209 0.249
Expression system: Spodoptera frugiperda

Quick links

Citations

47 review citations

The molecular details of cytokine signaling via the JAK/STAT pathway.
Morris et al. (2018)
46 more

40 mentions without citation

The molecular regulation of Janus kinase (JAK) activation.
Babon et al. (2014)
39 more