Description
Perifosine is an alkylphospholipid analog that exhibits anticancer chemotherapeutic and anti-inflammatory activities. Perifosine directly inhibits Akt by binding at multiple sites. In macrophages, perifosine inhibits LPS-induced increases in TNF-α and ERK activation and activates AMPK. In colorectal cancer, hepatocellular carcinoma, and multiple myeloma cells, perifosine induces apoptosis and inhibits growth; in clinical settings, perifosine enhances the anticancer activity of other chemotherapeutics.
References
Gradziel CS, Wang Y, Stec B, et al. Cytotoxic amphiphiles and phosphoinositides bind to two discrete sites on the Akt1 PH domain. Biochemistry. 2014 Jan 28;53(3):462-72. PMID: 24383815.
Shen J, Liang L, Wang C. Perifosine inhibits lipopolysaccharide (LPS)-induced tumor necrosis factor (TNF)-α production via regulation multiple signaling pathways: new implication for Kawasaki disease (KD) treatment. Biochem Biophys Res Commun. 2013 Jul 26;437(2):250-5. PMID: 23806687.
Richardson PG, Eng C, Kolesar J, et al. Perifosine, an oral, anti-cancer agent and inhibitor of the Akt pathway: mechanistic actions, pharmacodynamics, pharmacokinetics, and clinical activity. Expert Opin Drug Metab Toxicol. 2012 May;8(5):623-33. PMID: 22512706.
Fei HR, Chen G, Wang JM, et al. Perifosine induces cell cycle arrest and apoptosis in human hepatocellular carcinoma cell lines by blockade of Akt phosphorylation. Cytotechnology. 2010 Oct;62(5):449-60. PMID: 20842425.
