› 4equ

X-ray diffraction
2Å resolution

Human STK-10 (LOK) kinase domain in DFG-out conformation with inhibitor DSA-7

Released:
DOI: 10.2210/pdb4equ/pdb
PDB entry 4equ coloured by chain, front view.
PDB entry 4equ coloured by chain, side view.
PDB entry 4equ coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Affinity-Based Probes Based on Type II Kinase Inhibitors.
Ranjitkar P, Perera BG, Swaney DL, Hari SB, Larson ET, Krishnamurty R, Merritt EA, Villen J, Maly DJ
J. Am. Chem. Soc. (2012)
PMID: 23088519

Function and Biology Details

Reaction catalysed: 
ATP + a protein = ADP + a phosphoprotein
Biochemical function:
Biological process:
Cellular component:
  • not assigned
Sequence domains:

Structure analysis Details

Assembly composition:
homo dimer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-131760 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Serine/threonine-protein kinase 10 Chains: A, B
Molecule details ›
Chains: A, B
Length: 302 amino acids
Theoretical weight: 34.3 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: O94804 (Residues: 18-317; Coverage: 31%)
Gene names: LOK, STK10
Sequence domains: Protein kinase domain
Structure domains:

Ligands and Environments

3 bound ligands:
Ligand G6I 2 x G6I
Ligand CA 5 x CA
Ligand 1PE 1 x 1PE
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: SSRL BEAMLINE BL9-2
Spacegroup: P21
Unit cell:
a: 61.81Å b: 49.04Å c: 133.76Å
α: 90° β: 101.42° γ: 90°
R-values:
R R work R free
0.224 0.223 0.246
Expression system: Escherichia coli

Quick links

Citations

10 review citations

Enzyme inhibitor discovery by activity-based protein profiling.
Niphakis et al. (2014)
9 more

5 mentions without citation

Sequence determinants of a specific inactive protein kinase conformation.
Hari et al. (2013)
4 more