Table 1.
Class | Subclass | Catalytic subunit | Adaptor/ Regulatory subunits | Regulated by | Distribution | In vitro lipid products | Functions for selective inhibitors | Organization with licences |
---|---|---|---|---|---|---|---|---|
I | A | p110α | p85α, p85β, | RTKa | Ubiquitous | PI(3)Pb, | Developmentc14, | Eli Lilly |
p55α, p55γ, p50α | PI(3,4)P2d, | Human cancere116, | Iconix | |||||
PI(3,4,5)P3f | Myocardial contractility117 | Echelon | ||||||
Astra Zeneca | ||||||||
Wyeth | ||||||||
PIramed | ||||||||
Moreg | ||||||||
p110β | p85α, p85β, | RTKa, | Ubiquitous | PI(3)Pb, | Developmentc15, | Kinacia | ||
p55α, p55γ, p50α | GPCRh | PI(3,4)P2d | Insulin signalling118, | |||||
PI(3,4,5)P3f | Motility119, | |||||||
Phagocytosis120, | ||||||||
Thrombus formation121, | ||||||||
p110δ | p85α, p85β, | RTKa | Leucocytesi | PI(3)Pb, | Immunity24, | ICOS | ||
p55α, p55γ, p50α | PI(3,4)P2d, | Cytokine receptor signalling122, | PIramed | |||||
PI(3,4,5)P3f | B-cell development24, | |||||||
B-cell migration38, | ||||||||
T-cell development123, | ||||||||
Cell proliferation124, | ||||||||
B- and T-cell antigenreceptor signalling24, | ||||||||
Smooth muscle tone andhypertension125, | ||||||||
Neutrophil migration and burst40 | ||||||||
B | p110γ | p101, p87PIKAP | GPCRh | Myeloidi | PI(3)Pb, | Thymocyte development126, | Novartis | |
PI(3,4)P2d, | T cell development123, | Bayer | ||||||
PI(3,4,5)P3f | T cell migration38, | Pfizer | ||||||
Neutrophil migration126, | Serono | |||||||
Macrophage and dendritic cell migration37, | Targegen | |||||||
Mast cell degranulation29, | Calbiochem | |||||||
Neutrophil burst40, | ||||||||
Insulin secretion127, | ||||||||
Myocardial contractility117 | ||||||||
II | C2α | Clathrin | RTKa | Widespread | PI(3)Pb, | Vesicle trafficking9, | ||
GPCRh, IRj | PI(3,4)P2d | Insulin signalling128, | ||||||
Cell survival129, | ||||||||
Vascular smooth musclecontraction130 | ||||||||
C2β | Clathrin | RTKa, | Widespread | PI(3)Pb, | Vesicle trafficking131, | |||
GPCRh, IRj | PI(3,4)P2d | Cell migration132,133, | ||||||
Liver growth134 | ||||||||
C2γ | Clathrin | ? | Hepatic | PI(3)Pb, | Liver regeneration135 | |||
PI(3,4)P2d | ||||||||
III | Vps34p | Vps15p | TLRk, constitutive | Ubiquitous | PI(3)Pb | Toll-like receptor signalling136, | ||
Receptor-independent membranetrafficking137 |
Receptor tyrosine kinase
phosphatidyl inositol-3-monophosphate
deletion associated with defective mouse embryonic proliferation and death
phosphatidyl inositol-3,4-bisphosphate
mutated/amplified in human cancer
phosphatidyl inositol 3,4,5-trisphosphate
due to the high frequency of PIK3CA mutations in human cancer, extensive research into selective inhibitors for this isoform have been carried out by many other institutions (Yamanouchi, Xinxiang Medical College, Semafore, Chiron, Zenyaku Kogyo, Boehringer, University of British Columbia)
G-protein coupled receptors
mainly, but also expressed in endothelial cells and others
integrin receptors
Toll-like receptors.