title: Phosphatidylinositol 3-kinase (PI3K) inhibitors as cancer therapeutics.
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.
authors.forename: Akintunde
authors.initials: A
authors.lastname: Akinleye
authors.forename: Parthu
authors.initials: P
authors.lastname: Avvaru
authors.forename: Muhammad
authors.initials: M
authors.lastname: Furqan
authors.forename: Yongping
authors.initials: Y
authors.lastname: Song
authors.affiliation: Division of Hematology/Oncology, Department of Medicine, New York Medical College and Westchester Medical Center, Valhalla, NY 10595, USA. DELONG_LIU@NYMC.EDU.
authors.forename: Delong
authors.initials: D
authors.lastname: Liu
mesh_terms: D000818:Animals; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology*; D000081082:Phosphoinositide-3 Kinase Inhibitors; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use*; D015398:Signal Transduction
chemical_list: D000081082:Phosphoinositide-3 Kinase Inhibitors; D047428:Protein Kinase Inhibitors