鞘氨醇激酶 1 选择性抑制剂的合成。
Synthesis of selective inhibitors of sphingosine kinase 1.
机构信息
Department of Chemistry and Biochemistry, Queens College of the City University of New York, Flushing, New York 11367-1597, USA.
出版信息
Chem Commun (Camb). 2013 Mar 14;49(21):2136-8. doi: 10.1039/c3cc00181d. Epub 2013 Feb 7.
Abstract
Sphingosine kinase isoform 1 (SK1) inhibitors may serve as therapeutic agents for proliferative diseases, including hypertension. We synthesized a series of sphingosine-based SK1-selective inhibitors, the most potent of which is RB-005 (IC(50) = 3.6 μM), which also induced proteasomal degradation of SK1 in human pulmonary arterial smooth muscle cells.
摘要
鞘氨醇激酶同工型 1（SK1）抑制剂可能作为治疗增殖性疾病（包括高血压）的药物。我们合成了一系列基于鞘氨醇的 SK1 选择性抑制剂，其中最有效的是 RB-005（IC50=3.6μM），它还能诱导人肺动脉平滑肌细胞中 SK1 的蛋白酶体降解。
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