› 5ut5

X-ray diffraction
1.9Å resolution

JAK2 JH2 in complex with GLPG0634

Released:
DOI: 10.2210/pdb5ut5/pdb
PDB entry 5ut5 coloured by chain, front view.
PDB entry 5ut5 coloured by chain, side view.
PDB entry 5ut5 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules.
Newton AS, Deiana L, Puleo DE, Cisneros JA, Cutrona KJ, Schlessinger J, Jorgensen WL
ACS Med Chem Lett 8 614-617 (2017)
PMID: 28626520

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 Chain: A
Molecule details ›
Chain: A
Length: 289 amino acids
Theoretical weight: 33.12 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: O60674 (Residues: 536-812; Coverage: 25%)
Gene name: JAK2
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

4 bound ligands:
Ligand GOL 4 x GOL
Ligand 2HB 1 x 2HB
Ligand ACT 1 x ACT
Ligand DMS 1 x DMS
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: RIGAKU MICROMAX-007 HF
Spacegroup: P21
Unit cell:
a: 44.44Å b: 57.381Å c: 60.556Å
α: 90° β: 110.03° γ: 90°
R-values:
R R work R free
0.162 0.16 0.2
Expression system: Spodoptera frugiperda

Quick links

Citations

13 citation in other articles

Covalent inhibitors of EGFR family protein kinases induce degradation of human Tribbles 2 (TRIB2) pseudokinase in cancer cells.
Foulkes et al. (2018)
12 more

5 mentions without citation

Prospects for pharmacological targeting of pseudokinases.
Kung et al. (2019)
4 more