Nitroreductase-Mediated Release of Inhibitors of Lysine-Specific Demethylase 1 (LSD1) from Prodrugs in Transfected Acute Myeloid Leukaemia Cells.,ChemBioChem

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Nitroreductase-Mediated Release of Inhibitors of Lysine-Specific Demethylase 1 (LSD1) from Prodrugs in Transfected Acute Myeloid Leukaemia Cells.
ChemBioChem ( IF 3.2 ) Pub Date : 2020-03-30 , DOI: 10.1002/cbic.202000138
Eva-Maria Herrlinger ₁ , Mirjam Hau _{1,

2} , Desiree Melanie Redhaber ₃ , Gabriele Greve ₃ , Dominica Willmann ₄ , Simon Steimle ₁ , Michael Müller ₁ , Michael Lübbert _{3,

5,

6} , Christoph Cornelius Miething ₃ , Roland Schüle _{2,

4} , Manfred Jung _{1,

2,

5,

6}

Affiliation

Site‐specific targeting: Nitroaromatic prodrugs were activated by the bacterial nitroreductase NfsB (NTR) to selectively inhibit lysine‐specific demethylase 1 (LSD1) in transfected leukaemic cells. The effects of LSD1 inhibition and cytotoxicity of the side products were distinguished by negative controls. This system may be applied in targeting approaches to reach site‐specific LSD1 inhibition.

中文翻译：

转染的急性髓性白血病细胞中硝基还原酶介导的赖氨酸特异性脱甲基酶 1 (LSD1) 抑制剂从前药中的释放。

位点特异性靶向：硝基芳香族前药被细菌硝基还原酶 NfsB (NTR) 激活，选择性抑制转染白血病细胞中的赖氨酸特异性去甲基酶 1 (LSD1)。LSD1 抑制作用和副产物的细胞毒性通过阴性对照来区分。该系统可应用于靶向方法以实现位点特异性 LSD1 抑制。

更新日期：2020-03-30

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