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Future Med Chem. 2011 Apr;3(5):549-65. doi: 10.4155/fmc.11.12.

Small-molecule inhibitors of the PI3K signaling network.

Author information

1
Department of biochemistry, Tufts University School of Medicine, 136 Harrison Ave., Boston, MA 02111, USA.

Abstract

The phosphoinositide 3-kinase (PI3K) signaling pathway controls a wide variety of cellular processes including cell death and survival, cell migration, protein synthesis and metabolism. Aberrant PI3K-dependent signaling, mediated by Akt kinase, has been implicated in many human diseases including cancer, inflammation, cardiovascular disease and metabolic diseases, making this pathway a principle target for drug development. In this article we will summarize the PI3K signaling network and discuss current strategies for pathway inhibition. We will also explore the importance and emerging relevance of Akt-independent PI3K signaling pathways and discuss attempts being made to harness these pathways by inhibiting the binding of a product of PI3K, phosphatidylinositol-(3,4,5)-trisphosphate, to effector pleckstrin homology domains.

PMID:
21526896
PMCID:
PMC3132554
DOI:
10.4155/fmc.11.12
[Indexed for MEDLINE]
Free PMC Article

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