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Crystal structure of PI3K p110gamma catalytical domain in complex with organoruthenium inhibitor E5E2

Source organism: Homo sapiens
Biochemical function: kinase activity
Biological process: phosphatidylinositol phosphate biosynthetic process
Cellular component: not assigned

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EC 2.7.11.1: Non-specific serine/threonine protein kinase

Reaction catalysed:
ATP + a protein = ADP + a phosphoprotein
Systematic name:
ATP:protein phosphotransferase (non-specific)
Alternative Name(s):
  • A-kinase
  • AP50 kinase
  • ATP-protein transphosphorylase
  • Beta-IIPKC
  • Beta-adrenergic receptor kinase
  • CK-2
  • CKI
  • CKII
  • Calcium-dependent protein kinase C
  • Calcium/phospholipid-dependent protein kinase
  • Casein kinase
  • Casein kinase (phosphorylating)
  • Casein kinase 2
  • Casein kinase I
  • Casein kinase II
  • Cyclic AMP-dependent protein kinase
  • Cyclic AMP-dependent protein kinase A
  • Cyclic monophosphate-dependent protein kinase
  • Cyclic nucleotide-dependent protein kinase
  • Cyclin-dependent kinase
  • Cytidine 3',5'-cyclic monophosphate-responsive protein kinase
  • Dsk1
  • Epsilon PKC
  • Glycogen synthase A kinase
  • Glycogen synthase a kinase
  • Glycogen synthase kinase
  • HIPK2
  • Hpr kinase
  • Hydroxyalkyl-protein kinase
  • M phase-specific cdc2 kinase
  • MAPK
  • Mitogen-activated S6 kinase
  • Mitogen-activated protein kinase
  • P82 kinase
  • PKA
  • PKC
  • Phosphorylase B kinase kinase
  • Phosphorylase b kinase kinase
  • Phosphorylase b kinase kinase
  • Protein glutamyl kinase
  • Protein kinase (phosphorylating)
  • Protein kinase A
  • Protein kinase CK2
  • Protein kinase p58
  • Protein phosphokinase
  • Protein serine kinase
  • Protein serine-threonine kinase
  • Protein-aspartyl kinase
  • Protein-cysteine kinase
  • Protein-serine kinase
  • Prp4 protein kinase
  • Raf kinase
  • Raf-1
  • Ribosomal S6 protein kinase
  • Ribosomal protein S6 kinase II
  • STK32
  • Serine kinase
  • Serine protein kinase
  • Serine(threonine) protein kinase
  • Serine-specific protein kinase
  • Serine/threonine protein kinase
  • T-antigen kinase
  • Threonine-specific protein kinase
  • Twitchin kinase
  • Type-2 casein kinase
  • WEE1Hu
  • Wee 1-like kinase
  • Wee-kinase
  • cAMP-dependent protein kinase
  • cAMP-dependent protein kinase A
  • cGMP-dependent protein kinase

EC 2.7.1.154: Phosphatidylinositol-4-phosphate 3-kinase

Reaction catalysed:
ATP + 1-phosphatidyl-1D-myo-inositol 4-phosphate = ADP + 1-phosphatidyl-1D-myo-inositol 3,4-bisphosphate
Systematic name:
ATP:1-phosphatidyl-1D-myo-inositol-4-phosphate 3-phosphotransferase
Alternative Name(s):
  • C2-domain-containing phosphoinositide 3-kinase
  • Phosphoinositide 3-kinase
  • Type II phosphoinositide 3-kinase

EC 2.7.1.153: Phosphatidylinositol-4,5-bisphosphate 3-kinase

Reaction catalysed:
ATP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate = ADP + 1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate
Systematic name:
ATP:1-phosphatidyl-1D-myo-inositol-4,5-bisphosphate 3-phosphotransferase
Alternative Name(s):
  • Type I phosphoinositide 3-kinase

EC 2.7.1.137: Phosphatidylinositol 3-kinase

Reaction catalysed:
ATP + 1-phosphatidyl-1D-myo-inositol = ADP + 1-phosphatidyl-1D-myo-inositol 3-phosphate
Systematic name:
ATP:1-phosphatidyl-1D-myo-inositol 3-phosphotransferase
Alternative Name(s):
  • 1-phosphatidylinositol 3-kinase
  • PI3-kinase
  • PtdIns-3-kinase
  • Type I phosphatidylinositol kinase
  • Type III phosphoinositide 3-kinase
  • Vps34p

GO terms

Biochemical function:
Biological process:
Cellular component:
  • not assigned

Sequence families

Pfam Protein families (Pfam)
PF00454
Domain description: Phosphatidylinositol 3- and 4-kinase
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
The deposited structure of PDB entry 3cst contains 1 copy of Pfam domain PF00454 (Phosphatidylinositol 3- and 4-kinase) in Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform. Showing 1 copy in chain A.

PF00613
Domain description: Phosphoinositide 3-kinase family, accessory domain (PIK domain)
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
The deposited structure of PDB entry 3cst contains 1 copy of Pfam domain PF00613 (Phosphoinositide 3-kinase family, accessory domain (PIK domain)) in Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform. Showing 1 copy in chain A.

PF00792
Domain description: Phosphoinositide 3-kinase C2
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
The deposited structure of PDB entry 3cst contains 1 copy of Pfam domain PF00792 (Phosphoinositide 3-kinase C2) in Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform. Showing 1 copy in chain A.

PF00794
Domain description: PI3-kinase family, ras-binding domain
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
The deposited structure of PDB entry 3cst contains 1 copy of Pfam domain PF00794 (PI3-kinase family, ras-binding domain) in Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform. Showing 1 copy in chain A.

InterPro InterPro annotations
IPR000403
Domain description: Phosphatidylinositol 3-/4-kinase, catalytic domain
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
IPR001263
Domain description: Phosphoinositide 3-kinase, accessory (PIK) domain
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
IPR002420
Domain description: C2 phosphatidylinositol 3-kinase-type domain
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
IPR000341
Domain description: Phosphatidylinositol 3-kinase Ras-binding (PI3K RBD) domain
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
IPR018936
Domain description: Phosphatidylinositol 3/4-kinase, conserved site
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
IPR035892
Domain description: C2 domain superfamily
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
IPR036940
Domain description: Phosphatidylinositol 3-/4-kinase, catalytic domain superfamily
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
IPR011009
Domain description: Protein kinase-like domain superfamily
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
IPR042236
Domain description: Phosphoinositide 3-kinase, accessory (PIK) domain superfamily
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
IPR016024
Domain description: Armadillo-type fold
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
IPR015433
Domain description: Phosphatidylinositol kinase
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
IPR029071
Domain description: Ubiquitin-like domain superfamily
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
IPR045580
Domain description: PIK3 catalytic subunit gamma, adaptor-binding domain
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform

Structure domains

CATH CATH domains
1.10.1070.11
Class: Mainly Alpha
Architecture: Orthogonal Bundle
Topology: Phosphatidylinositol 3-kinase Catalytic Subunit; Chain A, Domain 5
Homology: Phosphatidylinositol 3-/4-kinase, catalytic domain
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
The deposited structure of PDB entry 3cst contains 1 copy of CATH domain 1.10.1070.11 (Phosphatidylinositol 3-kinase Catalytic Subunit; Chain A, Domain 5) in Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform. Showing 1 copy in chain A.
3.30.1010.10
Class: Alpha Beta
Architecture: 2-Layer Sandwich
Topology: Phosphatidylinositol 3-kinase Catalytic Subunit; Chain A, domain 4
Homology: Phosphatidylinositol 3-kinase Catalytic Subunit; Chain A, domain 4
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
The deposited structure of PDB entry 3cst contains 1 copy of CATH domain 3.30.1010.10 (Phosphatidylinositol 3-kinase Catalytic Subunit; Chain A, domain 4) in Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform. Showing 1 copy in chain A.
1.25.40.70
Class: Mainly Alpha
Architecture: Alpha Horseshoe
Topology: Serine Threonine Protein Phosphatase 5, Tetratricopeptide repeat
Homology: Phosphatidylinositol 3-kinase, accessory domain (PIK)
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
The deposited structure of PDB entry 3cst contains 1 copy of CATH domain 1.25.40.70 (Serine Threonine Protein Phosphatase 5, Tetratricopeptide repeat) in Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform. Showing 1 copy in chain A.
2.60.40.150
Class: Mainly Beta
Architecture: Sandwich
Topology: Immunoglobulin-like
Homology: C2 domain
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
The deposited structure of PDB entry 3cst contains 1 copy of CATH domain 2.60.40.150 (Immunoglobulin-like) in Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform. Showing 1 copy in chain A.
3.10.20.90
Class: Alpha Beta
Architecture: Roll
Topology: Ubiquitin-like (UB roll)
Homology: Phosphatidylinositol 3-kinase Catalytic Subunit; Chain A, domain 1
Occurring in:
  1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
The deposited structure of PDB entry 3cst contains 1 copy of CATH domain 3.10.20.90 (Ubiquitin-like (UB roll)) in Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform. Showing 1 copy in chain A.

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