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Structure determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin and staurosporine

X-ray diffraction
2.7Å resolution
PDB entry 1e90 coloured by chain, front view.
PDB entry 1e90 coloured by chain, side view.
PDB entry 1e90 coloured by chain, top view.
Source organism: Sus scrofa
Assembly composition:
monomeric (preferred)
Entry contents: 1 distinct polypeptide molecule

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Assemblies

Assembly 1 (preferred)
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Assembly Name: Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
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Multimeric state: monomeric
Accessible surface area: 37355.74 Å2
Buried surface area: 672.95 Å2
Dissociation area: 336.48 Å2
Dissociation energy (ΔGdiss): 11.03 kcal/mol
Dissociation entropy (TΔSdiss): 4.3 kcal/mol
Symmetry number: 1
PDBe Complex ID: PDB-CPX-126424

Macromolecules

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
Chain: A
Length: 961 amino acids
Theoretical weight: 109.95 KDa
Source organism: Sus scrofa
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: O02697 (Residues: 142-142, 144-1102; Coverage: 87%)
Gene name: PIK3CG
Pfam:
InterPro:
CATH:
SCOP:
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in PDB entry 1e90, assembly 1, front view.
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in PDB entry 1e90, assembly 1, side view.
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in PDB entry 1e90, assembly 1, top view.
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