Current Cancer Drug Targets

Ruiwen Zhang 
Texas Tech University Health Sciences Center
1300 Coulter Drive
Amarillo, TX 79106
USA

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The PIK3CA Gene as a Mutated Target for Cancer Therapy

Author(s): John P. Gustin, David P. Cosgrove, Ben Ho Park.

Abstract:

The development of targeted therapies with true specificity for cancer relies upon exploiting differences between cancerous and normal cells. Genetic and genomic alterations including somatic mutations, translocations, and amplifications have served as recent examples of how such differences can be exploited as effective drug targets. Small molecule inhibitors and monoclonal antibodies directed against the protein products of these genetic anomalies have led to cancer therapies with high specificity and relatively low toxicity. Recently, our group and others have demonstrated that somatic mutations in the PIK3CA gene occur at high frequency in breast and other cancers. Moreover, the majority of mutations occur at three hotspots, making these ideal targets for therapeutic development. Here we review the literature on PIK3CA mutations in cancer, as well as existing data on PIK3CA inhibitors and inhibitors of downstream effectors for potential use as targeted cancer therapeutics.

Keywords: PIK3CA, mutation, oncogene, PI3 kinase, AKT, mTOR

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Article Details

VOLUME: 8
ISSUE: 8
Year: 2008
Page: [733 - 740]
Pages: 8
DOI: 10.2174/156800908786733504
Price: $58