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Drugs of the Future
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Drugs Fut 2007, 32(6): 537
ISSN 0377-8282
e-ISSN 2013-0368
Copyright 2007 Clarivate
CCC: 0377-8282
DOI: 10.1358/dof.2007.032.06.1107995
 
 
Phosphatidylinositol 3-kinase (PI3K) inhibitors as anticancer drugs
Verheijen, J.C., Zask, A.
 
 
The phosphatidylinositol 3-kinases (PI3Ks) are members of a family of lipid kinases that regulate cellular metabolism and growth by phosphorylation of the 3-position of phosphatidylinositol to generate phosphatidylinositol triphosphate (PIP3). The PI3K pathway is one of the most frequently mutated in human cancer, leading to amplification of signaling, and as such is a promising target for small-molecule inhibition, with exciting therapeutic opportunities for the treatment of cancer. The last several years have seen an explosive increase in publications and patents concerning inhibition of PI3K. This paper summarizes recent developments in the discovery of PI3K inhibitors as anticancer drugs. We describe representative examples of seven structurally diverse classes of PI3K inhibitors. These compounds represent a large arsenal of potent enzyme inhibitors (single-digit nanomolar IC50 values) with a variety of isoform specificity profiles. Currently, the first PI3K inhibitors are making their way into the clinic and we eagerly await data that will help address questions regarding the contribution of inhibition of various PI3K isoforms to tumor suppression and the associated side effect profiles.


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