Article: Take your PIK: phosphatidylinositol 3-kinase inhibitors race through the clinic and toward cancer therapy.
2009 Volume 8, Issue 1, Page(s) 1–9
Abstract: The phosphatidylinositol 3-kinase (PI3K)/Akt signaling pathway is currently one of the most ... to the four PI3K class I isoforms would be too toxic for use in cancer therapy due to effects on physiologic ... proved to be tolerable and therapeutically beneficial in animal studies, and a number are in clinical ...
| Abstract | The phosphatidylinositol 3-kinase (PI3K)/Akt signaling pathway is currently one of the most exciting drug targets in oncology. However, only a short time ago, the paradigm existed that drugs targeted to the four PI3K class I isoforms would be too toxic for use in cancer therapy due to effects on physiologic signaling. Since that time, studies have delineated the roles of these four isoforms in nonpathologic signaling as well as their roles in cancer. An extensive effort has gone into developing agents that inhibit one or more PI3K isoforms, as well as closely related proteins implicated in cancer. These agents have proved to be tolerable and therapeutically beneficial in animal studies, and a number are in clinical testing. The agents, their properties, and their molecular targets are discussed in this review. |
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| MeSH term(s) | Animals ; Drug Discovery ; Humans ; Isoenzymes/antagonists & inhibitors ; Isoenzymes/classification ; Isoenzymes/metabolism ; Neoplasms/drug therapy ; Neoplasms/enzymology ; Phosphatidylinositol 3-Kinases/classification ; Phosphatidylinositol 3-Kinases/metabolism ; Phosphoinositide-3 Kinase Inhibitors ; Protein Kinase Inhibitors/chemistry ; Protein Kinase Inhibitors/therapeutic use ; Signal Transduction | |||||
| Chemical Substances | Isoenzymes ; Phosphoinositide-3 Kinase Inhibitors ; Protein Kinase Inhibitors | |||||
| Language | English | |||||
| Publishing date | 2009-01-12 | |||||
| Publishing country | United States | |||||
| Document type | Journal Article ; Research Support, N.I.H., Extramural ; Review | |||||
| ZDB-ID | 2063563-1 | |||||
| ISSN | 1538-8514 ; 1535-7163 | |||||
| ISSN (online) | 1538-8514 | |||||
| ISSN | 1535-7163 | |||||
| DOI | 10.1158/1535-7163.MCT-08-0801 | |||||
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| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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