Recent progress in understanding the molecular mechanisms of receptor signal transduction is continuously highlighting new unforeseen potential drug targets for yet unmet therapeutic needs. While the large number of different cell surface receptors challenge the concept of antagonists development, the finding of signal transduction platforms common to multiple receptor families has boosted the development of new therapeutic approaches. The identification of the role of phosphoinositide 3-kinase family members downstream receptors as directors of multiple cellular responses ranging from cell proliferation and survival to immunity and cardiovascular control, is an example of successful drug target validation studies. This review will focus on these findings and on the ongoing efforts to tame this family of enzymes to beat inflammation and cancer.
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