› 3gcv

X-ray diffraction
2.3Å resolution

Human P38 MAP Kinase in Complex with RL62

Released:
DOI: 10.2210/pdb3gcv/pdb
PDB entry 3gcv coloured by chain, front view.
PDB entry 3gcv coloured by chain, side view.
PDB entry 3gcv coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Development of a fluorescent-tagged kinase assay system for the detection and characterization of allosteric kinase inhibitors.
Simard JR, Getlik M, Grütter C, Pawar V, Wulfert S, Rabiller M, Rauh D
J Am Chem Soc 131 13286-96 (2009)
PMID: 19572644

Function and Biology Details

Reaction catalysed: 
ATP + a protein = ADP + a phosphoprotein
Biochemical function:
Biological process:
Cellular component:
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-556911 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Mitogen-activated protein kinase 14 Chain: A
Molecule details ›
Chain: A
Length: 360 amino acids
Theoretical weight: 41.23 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: Q16539 (Residues: 2-360; Coverage: 100%)
Gene names: CSBP, CSBP1, CSBP2, CSPB1, MAPK14, MXI2, SAPK2A
Sequence domains: Protein kinase domain
Structure domains:

Ligands and Environments

2 bound ligands:
Ligand SS6 1 x SS6
Ligand BOG 2 x BOG
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: BRUKER AXS MICROSTAR
Spacegroup: P212121
Unit cell:
a: 67.785Å b: 70.003Å c: 74.513Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.199 0.196 0.254
Expression system: Escherichia coli

Quick links

Citations

10 review citations

FDA-approved small-molecule kinase inhibitors.
Wu et al. (2015)
9 more

4 mentions without citation

p38α Mitogen-Activated Protein Kinase Is a Druggable Target in Pancreatic Adenocarcinoma.
Yang et al. (2019)
3 more