The web-based teaching in the Institute of Structural and Molecular Biology, University of London

Abstract

Microsymposia increase enzymatic activity. The structure suggests that interaction with the membrane is mediated by one of the p85 domains (iSH2). The existence of p110alpha gain-of-function-mutants makes this protein an attractive therapeutic target. Since PI3Ks control a wide range of physiological functions, it would be desirable to inhibit only p110alpha, the isoform mutated in cancers. Structural differences among the isoforms can be exploited for that purpose. These findings may provide not only novel insight for the design of PI3K-isoformselective drugs but also help on the design of mutation-specific drugs.