title: Sphingosine kinase 2 inhibitor SG-12 induces apoptosis via phosphorylation by sphingosine kinase 2.
abstract: Sphingosine kinase (SPHK), which catalyzes the phosphorylation of sphingosine to generate sphingosine 1-phosphate, has two mammalian isotypes, SPHK1 and SPHK2. Both isozymes are promising anti-cancer therapeutic targets. In this report, we found that SG-12, a synthetic analogue of sphingosine that acts as a SPHK2 inhibitor, induces apoptosis via phosphorylation by SPHK2. The present results revealed the novel anti-cancer potential of a sphingosine analogue in the pathological setting where SPHK2 is upregulated.
authors: Section of Biochemistry, Department of Hard Tissue Engineering, Graduate School of Medical and Dental Sciences, Tokyo Medical and Dental University, 1-5-45 Yushima, Tokyo 113-8549, Japan. m.yokoyama.bch@tmd.ac.jp
authors: Miki
authors: M
authors: Hara-Yokoyama
authors: Kazue
authors: K
authors: Terasawa
authors: Shizuko
authors: S
authors: Ichinose
authors: Akihiko
authors: A
authors: Watanabe
authors: Katarzyna A
authors: KA
authors: Podyma-Inoue
authors: Kazunari
authors: K
authors: Akiyoshi
authors: Yasuyuki
authors: Y
authors: Igarashi
authors: Masaki
authors: M
authors: Yanagishita
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D051379:Mice; D010766:Phosphorylation / Q000187:drug effects; D017853:Phosphotransferases (Alcohol Group Acceptor) / Q000037:antagonists & inhibitors* / Q000378:metabolism; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013110:Sphingosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D000099157:Sphingosine Kinase
chemical_list: D000970:Antineoplastic Agents; D017853:Phosphotransferases (Alcohol Group Acceptor); D047428:Protein Kinase Inhibitors; D013110:Sphingosine; D000099157:Sphingosine Kinase; C583673:SG-12 compound