The PIK3CA gene as a mutated target for cancer therapy.
The PIK3CA gene as a mutated target for cancer therapy.
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DOI：
10.2174/156800908786733504
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发表时间：
2008-12
影响因子：
3
通讯作者：
Park BH
中科院分区：
文献类型：
--
作者：
Gustin JP;Cosgrove DP;Park BH
针对癌症的真正特异性靶向治疗的发展依赖于利用癌细胞和正常细胞之间的差异。包括体细胞突变、易位和扩增在内的遗传和基因组改变是如何利用这些差异作为有效药物靶点的最新例子。针对这些基因异常的蛋白质产物的小分子抑制剂和单克隆抗体已经导致具有高特异性和相对低毒性的癌症治疗。最近，我们的团队和其他人已经证明，PIK3CA基因的体细胞突变在乳腺癌和其他癌症中发生的频率很高。此外，大多数突变发生在三个热点，使它们成为治疗开发的理想靶点。在这里，我们回顾了关于癌症中PIK3CA突变的文献，以及关于PIK3CA抑制剂和下游效应物抑制剂的现有数据，这些抑制剂可能用作靶向癌症治疗药物。
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.
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影响因子：
11.4
作者：
Brunn, GJ;Williams, J;Abraham, RT
通讯作者：
Abraham, RT
影响因子：
6.2
作者：
Campistol, JM;Gutierrez-Dalmau, A;Torregrosa, JV
通讯作者：
Torregrosa, JV
影响因子：
45.3
作者：
Chan, S;Scheulen, ME;Moore, L
通讯作者：
Moore, L
影响因子：
3.6
作者：
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通讯作者：
Park, BH
影响因子：
45.3
作者：
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通讯作者：
Sherman, ML