文献类型：会议

作　　者：赵文楠 Takao Yamori Shingo Dan 孔德新

作者单位：天津医科大学药学院生物制药教研室、基础医学研究中心分子靶向药物研究室 Division of Molecular Pharmacology,Japanese Foundation for Cancer Research

会议文献：2014医学科学前沿暨第三届个体化治疗与抗肿瘤药物研究新趋向研讨会论文集

会议名称：2014医学科学前沿暨第三届个体化治疗与抗肿瘤药物研究新趋向研讨会

会议日期：20141018

会议地点：深圳

主办单位：中国工程院医药卫生学部;广东省药理学会;中国医药生物技术协会

出版日期：20141018

语　　种：中文

摘　　要：As accumulating evidences suggest close involvement of phosphatidylinositol 3-kinase (PI3K) in cancer, novel PI3K inhibitors such as ZSTK474, GDC-0941,NVP-BEZ235 and BKM-120 have been developed for cancer therapy.A high frequency ofhotspot mutations known as E542K, E545K and H1047R in the PIK3CA gene, which encodes the catalytic subunit of PI3K, has been found in various types of human cancers.The hotspot PIK3CA mutations also lead to resistance to therapeutics targeting epidermal growth factor receptor (EGFR), further suggesting that inhibition of hotspot mutant PIK3CA be required for a PI3K inhibitor as anticancer drug.

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