Phosphoinositide 3-kinase (PI3K) was first identified as a lipid kinase activity associated with the products of viral oncogenes and with activated protein-tyrosine kinases. Since those early studies, the PI3K superfamily has grown to embrace at least 12 structurally and functionally related enzymes present in the human genome, some of which have protein kinase activity but not lipid kinase activity. Evidence is emerging that PI3K superfamily members, and components of PI3K signalling, play a role in the development of many human cancers. In this review, the PI3K family of enzymes and their signalling is reviewed, with particular reference to possible involvement in breast cancer.