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Trends Biochem Sci. 2007 Oct;32(10):450-6.

The PI3K inhibitor arsenal: choose your weapon!

Author information

1
UCB-Celltech, Slough, UK.

Abstract

Owing to its widespread activation in inflammation and cancer, a growing appreciation of the therapeutic potential of inhibitors of the phosphoinositide 3-kinase (PI3K) pathway has stimulated intense interest in compounds with suitable pharmacological profiles. These are primarily directed toward PI3K itself. However, as class I PI3Ks are also essential for a range of normal physiological processes, broad spectrum PI3K inhibition could be poorly tolerated. In recent years, patents describing a new generation of PI3K inhibitors have started to appear, with a particular focus on the development of compounds with enhanced isoform selectivity for use as anti-cancer and anti-inflammatory therapies. However, challenges remain for the efforts to pharmacologically target this enzyme family in a successful manner.

PMID:
17920279
DOI:
10.1016/j.tibs.2007.09.001
[Indexed for MEDLINE]

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