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. 2007 Aug;121(4):448–461. doi: 10.1111/j.1365-2567.2007.02663.x

Table 1.

Main characteristics of the members of the PI3K family

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
a

Receptor tyrosine kinase

b

phosphatidyl inositol-3-monophosphate

c

deletion associated with defective mouse embryonic proliferation and death

d

phosphatidyl inositol-3,4-bisphosphate

e

mutated/amplified in human cancer

f

phosphatidyl inositol 3,4,5-trisphosphate

g

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)

h

G-protein coupled receptors

i

mainly, but also expressed in endothelial cells and others

j

integrin receptors

k

Toll-like receptors.