Pachastrissamine (jaspine B) and its stereoisomers inhibit sphingosine kinases and atypical protein kinase C.
スポンサーリンク
概要
- 論文の詳細を見る
Sphingosine kinases (SphKs) are oncogenic enzymes that regulate the critical balance between ceramide and sphingosine-1-phosphate. Much effort has been dedicated to develop inhibitors against these enzymes. Naturally occurring pachastrissamine (jaspine B) and all its stereoisomers were prepared and evaluated for their inhibitory effects against SphKs. All eight stereoisomers exhibited moderate to potent inhibitory activity against SphK1 and SphK2. Inhibitory effects were profiled against protein kinase C (PKC) isoforms by in vitro experiments. Atypical PKCs (PKCζ and PKCι) were inhibited by several pachastrissamine stereoisomers. The improved activity over N,N-dimethylsphingosine suggests that the cyclic scaffold in pachastrissamines facilitates potential favorable interactions with SphKs and PKCs.
- 2011-09-15
論文 | ランダム
- 複数のボーリングコアの高精度解析にもとづく濃尾平野における沖積層の研究
- 高密度ボーリングデータ解析にもとづく濃尾平野沖積層の三次元構造
- ボーリングコアの粒度組成と堆積速度からみた木曽川デルタの微地形と堆積過程
- 完新世浅海堆積物の堆積速度の変化から見た桑名断層の活動間隔
- 高密度ボーリングデータ解析にもとづく木曽川デルタの前進過程