› 3hhm

X-ray diffraction
2.8Å resolution

Crystal structure of p110alpha H1047R mutant in complex with niSH2 of p85alpha and the drug wortmannin

Released:
DOI: 10.2210/pdb3hhm/pdb
PDB entry 3hhm coloured by chain, front view.
PDB entry 3hhm coloured by chain, side view.
PDB entry 3hhm coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
A frequent kinase domain mutation that changes the interaction between PI3Kalpha and the membrane.
Mandelker D, Gabelli SB, Schmidt-Kittler O, Zhu J, Cheong I, Huang CH, Kinzler KW, Vogelstein B, Amzel LM
Proc Natl Acad Sci U S A 106 16996-7001 (2009)
PMID: 19805105

Function and Biology Details

Reactions catalysed: 
ATP + 1-phosphatidyl-1D-myo-inositol = ADP + 1-phosphatidyl-1D-myo-inositol 3-phosphate
ATP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate = ADP + 1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate
ATP + a protein = ADP + a phosphoprotein
Biochemical function:
Biological process:
Cellular component:
Sequence domains:

Structure analysis Details

Assembly composition:
hetero dimer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-151133 (preferred)
Entry contents:
2 distinct polypeptide molecules
Macromolecules (2 distinct):
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Chain: A
Molecule details ›
Chain: A
Length: 1091 amino acids
Theoretical weight: 127.29 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P42336 (Residues: 1-1068; Coverage: 100%)
Gene name: PIK3CA
Sequence domains:
Structure domains:
Phosphatidylinositol 3-kinase regulatory subunit alpha Chain: B
Molecule details ›
Chain: B
Length: 373 amino acids
Theoretical weight: 44.26 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P27986 (Residues: 322-694; Coverage: 52%)
Gene names: GRB1, PIK3R1
Sequence domains:
Structure domains:

Ligands and Environments

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

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 31-ID
Spacegroup: P212121
Unit cell:
a: 115.312Å b: 121.453Å c: 152.494Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.243 0.223 0.307
Expression system: Spodoptera frugiperda

Quick links

Citations

48 review citations

The emerging mechanisms of isoform-specific PI3K signalling.
Vanhaesebroeck et al. (2010)
47 more

62 mentions without citation

KDM1 class flavin-dependent protein lysine demethylases.
Burg et al. (2015)
61 more