Phosphatidylinositol 3-Kinase (PI3K) Inhibitors as Cancer Therapeutics

Authors

Akintunde Akinleye
Parthu Avvaru
Muhammad Furqan
Yongping Song
Delong Liu, Division of Hematology/Oncology, Department of Medicine, New York Medical College and Westchester Medical Center, Valhalla, NY 10595, USA. DELONG_LIU@NYMC.EDU.

Author Type(s)

Faculty

DOI

10.1186/1756-8722-6-88

Journal Title

Journal of Hematology & Oncology

First Page

88

Document Type

Article

Publication Date

11-22-2013

Abstract

Phosphatidylinositol 3-kinases (PI3Ks) are lipid kinases that regulate diverse cellular processes including proliferation, adhesion, survival, and motility. Dysregulated PI3K pathway signaling occurs in one-third of human tumors. Aberrantly activated PI3K signaling also confers sensitivity and resistance to conventional therapies. PI3K has been recognized as an attractive molecular target for novel anti-cancer molecules. In the last few years, several classes of potent and selective small molecule PI3K inhibitors have been developed, and at least fifteen compounds have progressed into clinical trials as new anticancer drugs. Among these, idelalisib has advanced to phase III trials in patients with advanced indolent non-Hodgkin's lymphoma and mantle cell lymphoma. In this review, we summarized the major molecules of PI3K signaling pathway, and discussed the preclinical models and clinical trials of potent small-molecule PI3K inhibitors.

Recommended Citation

Akinleye, A., Avvaru, P., Furqan, M., Song, Y., & Liu, D. (2013). Phosphatidylinositol 3-Kinase (PI3K) Inhibitors as Cancer Therapeutics. Journal of Hematology & Oncology, 6 (1), 88. https://doi.org/10.1186/1756-8722-6-88