中文摘要：

在人的癌症的 phosphatidylinositol 3-kinases (PI3Ks ) 的枢轴的角色启发了小分子的活跃开发禁止这些类脂化合物 kinases。然而，归化为美国人的 pan-PI3K 和 dual-PI3K/mTOR 禁止者在临床的试用遇到了问题，与象一个 monotherapeutic 代理人以及副作用的相对高的率的有限功效。不同 PI3K isoforms 特别地起非冗余的作用，这逐渐地被认出当减少时，肿瘤打字，它为改进功效与目的为预先选择的病人推动了 isoform 选择的禁止者的发展不受欢迎的副作用。PI3K isoform 选择的禁止者的成功被 CAL101 (Idelalisib ) 代表， first-in-class PI3Kδ；被 FDA 为长期的淋巴球的白血病，懒惰 B 房间 non-Hodgkin 的淋巴瘤和 relapsed 的治疗同意了的选择小分子的禁止者小淋巴球的淋巴瘤。指向另外的 PI3K isoforms 的禁止者广泛地也正在被开发。这评论为癌症治疗在 PI3K isoform 选择的禁止者的开发集中于最近的进步。新奇 PI3K isoform 选择的禁止者的行动模式的更深的理解将提供珍贵信息进一步验证指向特定的 PI3K isoforms 的概念，当对可能的病人从治疗有益于成层的 biomarkers 的鉴定将为这些代理人的成功是必要的时。

英文摘要：

The pivotal roles of phosphatidylinositol 3-kinases （PI3Ks） in human cancers have inspired active development of small molecules to inhibit these lipid kinases. However, the first-generation pan-PI3K and dual-PI3K/mTOR inhibitors have encountered problems in clinical trials, with limited efficacies as a monotherapeutic agent as well as a relatively high rate of side effects. It is increasingly recognized that different PI3K isoforms play non-redundant roles in particular tumor types, which has prompted the development of isoform-selective inhibitors for pre-selected patients with the aim for improving efficacy while decreasing undesirable side effects. The success of PI3K isoform-selective inhibitors is represented by CAL101 （Idelalisib）, a first-in-class PI3Kδ-selective small-molecule inhibitor that has been approved by the FDA for the treatment of chronic lymphocytic leukemia, indolent B-cell non-Hodgkin’s lymphoma and relapsed small lymphocytic lymphoma. Inhibitors targeting other PI3K isoforms are also being extensively developed. This review focuses on the recent progress in development of PI3K isoform-selective inhibitors for cancer therapy. A deeper understanding of the action modes of novel PI3K isoform-selective inhibitors will provide valuable information to further validate the concept of targeting specific PI3K isoforms, while the identification of biomarkers to stratify patients who are likely to benefit from the therapy will be essential for the success of these agents.