Abstract
The phosphatidylinositol 3-kinase (PI3K)/AKT signaling pathway regulates multiple cellular processes. An overactivation of the pathway is frequently present in human malignancies and plays a key role in cancer progression. Hence, its inhibition has become a promising approach in cancer therapy. However, the development of resistances, such as the abrogation of negative feedback mechanisms or the activation of other proliferative signaling pathways, has considerably limited the anticancer efficacy of PI3K/AKT inhibitors. In addition, emerging evidence points out that although AKT is acknowledged as the major downstream effector of PI3K, both PI3K and AKT can operate independently of each other in cancer, revealing another level of complexity in this pathway. Here, we highlight the complex relationship between PI3K and AKT in cancer and further discuss the consequences of this relationship for cancer therapy.
Highlights
Targeting signaling pathways that are deregulated in human cancer has been a promising approach in cancer therapy [1]
The phosphatidylinositol 3-kinase (PI3K)/AKT signaling pathway is frequently deregulated in cancer and represents an important anticancer target [5]
Class I PI3Ks generate PIP3 at the plasma membrane, which will induce the recruitment of proteins that have a pleckstrin homology (PH) domain such as PDK1 and AKT (Figure 1) [17]
Summary
Targeting signaling pathways that are deregulated in human cancer has been a promising approach in cancer therapy [1]. The phosphatidylinositol 3-kinase (PI3K)/AKT signaling pathway is frequently deregulated in cancer and represents an important anticancer target [5]. The PI3K/AKT signaling pathway plays a major role in regulating cellular processes that are features of cancer such as cell proliferation, survival or migration. Over the last years, drugs that target PI3K or AKT have been extensively developed and are being tested in clinical trials (Supplementary Tables S1 and S2) [6,7]. After describing the major features of this pathway in cancer, we will review the complex relationship between PI3K and AKT in cancer and its relevance for cancer therapy
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