Synthesis and biological activity of optically active NCL-1, a lysine-specific demethylase 1 selective inhibitor
Synthesis and biological activity of optically active NCL-1, a lysine-specific demethylase 1 selective inhibitor
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DOI：
10.1016/j.bmc.2010.12.024
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发表时间：
2011-06-15
影响因子：
3.5
通讯作者：
Miyata, Naoki
中科院分区：
文献类型：
--
作者：
Ogasawara, Daisuke;Suzuki, Takayoshi;Miyata, Naoki
合成了光学活性的（1 S，2 R）-NCL-1和（1 R，2S）-NCL-1，并评价了它们的赖氨酸特异性脱甲基酶1抑制活性和细胞生长抑制活性。在酶测定中，（1 S，2 R）-异构体的效力约为（1 R，2S）-异构体的4倍。在细胞生长抑制试验中，这两种异构体在HEK 293细胞和SH-SY 5 Y细胞中显示出相似的活性，而在HeLa细胞中，（1 S，2 R）-异构体显示出比（1 R，2S）-异构体强约4倍的活性。(C)2010爱思唯尔有限公司保留所有权利。
Optically active (1S,2R)-NCL-1 and (1R,2S)-NCL-1 were synthesized and evaluated for their lysine-specific demethylase 1 inhibitory activity and cell growth inhibitory activity. In enzyme assays, the (1S,2R)-isomer was approximately four times more potent than the (1R, 2S)-isomer. In cell growth inhibition assays, the two isomers showed similar activity in HEK293 cells and SH-SY5Y cells, whereas the (1S, 2R)-isomer showed approximately four times more potent activity than the (1R, 2S)-isomer in HeLa cells. (C) 2010 Elsevier Ltd. All rights reserved.