From humble beginnings over 25 years ago as a lipid kinase activity associated with certain oncoproteins, PI3K (phosphoinositide 3-kinase) has been catapulted to the forefront of drug development in cancer, immunity and thrombosis, with the first clinical trials of PI3K pathway inhibitors now in progress. Here the authors give a brief overview of some key discoveries in the PI3K area and their impact, and include thoughts on the current state of the field, and where it could go from here.

PI3K - From the Bench to the Clinic and Back

PI3K Book Introduction
PDK1: The major transducer of PI 3-Kinase actions
Protein Kinase B (PKB/Akt), a key mediator of the PI3K signaling pathway
Regulatory subunits of class IA PI3K
The Regulation of Class IA PI 3-kinases by Inter-Subunit Interactions
Phosphoinositide signalling pathways in metabolic regulation
Role of RAS in the regulation of PI 3-kinase
More than just kinases: The scaffolding function of PI3K
PI3K signalling in neutrophils
PI 3-kinase p110beta regulation of platelet integrin alphaIIbbeta3
PI3Ks in lymphocyte signalling and development
PI3 kinase regulation of skeletal muscle hypertrophy and atrophy
Taking PI3Kdelta and PI3Kgamma one step ahead - Dual active PI3Kdelta/gamma inhibitors for the treatment of immune-mediated inflammatory diseases
Oncogenic Mutations of PIK3CA in Human Cancers
Structural Effects of Oncogenic PI3Kalpha Mutations
Comparing the roles of the p110alpha and p110beta isoforms of PI3K in signaling and cancer
Phosphatidylinositol 3-kinase (PI3K): The oncoprotein
AKT Signaling in Physiology and Disease
Faithfull modeling of PTEN loss driven diseases in the mouse
PI3K as a target for therapy in haematological malignancies
Clinical development of Phosphatidylinositol-3 kinase pathway inhibitors
New inhibitors of the PI3K-Akt-mTOR pathway: Insights into mTOR signaling from a new generation of Tor kinase domain inhibitors (TORKinibs)
Small molecule inhibitors of the PI3-kinase family
Targeting the RTK-PI3K-mTOR axis in malignant glioma: overcoming resistance
Subject index.