Advances in Cancer Drug Targets

Volume: 1

Indexed in: EBSCO, Scopus

Advances in Cancer Drug Targets is an e-book series that brings together recent expert reviews published on the subject with a focus on strategies for synthesizing and isolating organic compounds and ...
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The PIK3CA Gene as a Mutated Target for Cancer Therapy

Pp. 3-21 (19)

DOI: 10.2174/9781608054749113010003

Author(s): Sarah Croessmann, Justin Cidado, John P. Gustin, David Cosgrove, Ben Ho Park


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. 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 p110α inhibitors and inhibitors of downstream effectors for potential use as targeted cancer therapeutics.


PIK3CA, mutation, oncogene, PI3 kinase, AKT, mTOR.