› 6cqf

X-ray diffraction
2.25Å resolution

Crystal structure of HPK1 in complex an inhibitor G1858

Released:
DOI: 10.2210/pdb6cqf/pdb
PDB entry 6cqf coloured by chain, front view.
PDB entry 6cqf coloured by chain, side view.
PDB entry 6cqf coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Hematopoietic Progenitor Kinase-1 Structure in a Domain-Swapped Dimer.
Wu P, Sneeringer CJ, Pitts KE, Day ES, Chan BK, Wei B, Lehoux I, Mortara K, Li H, Wu J, Franke Y, Moffat JG, Grogan JL, Heffron TP, Wang W
Structure 27 125-133.e4 (2019)
PMID: 30503777

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-187814 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Mitogen-activated protein kinase kinase kinase kinase 1 Chain: A
Molecule details ›
Chain: A
Length: 297 amino acids
Theoretical weight: 33.12 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: Q92918 (Residues: 2-293; Coverage: 35%)
Gene names: HPK1, MAP4K1
Sequence domains: Protein kinase domain

Ligands and Environments

1 bound ligand:
Ligand F97 1 x F97
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 21-ID-F
Spacegroup: C2221
Unit cell:
a: 91.868Å b: 98.803Å c: 77.1Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.21 0.208 0.255
Expression system: Spodoptera frugiperda

Quick links

Citations

1 review citation

A perspective on HPK1 as a novel immuno-oncology drug target.
Sawasdikosol et al. (2020)
9 other articles

2 mentions without citation

Multiple conformational states of the HPK1 kinase domain in complex with sunitinib reveal the structural changes accompanying HPK1 trans-regulation.
Johnson et al. (2019)
1 more