Towards the development of activity-based probes for detection of lysine-specific demethylase-1 activity

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• 作者：Maria E. Ourailidou^a ; Alessia Lenoci^b ; Clemens Zwergel^b ; Dante Rotili^b ; Antonello Mai^b ; ^c ; ^{antonello.mai@uniroma1.it} ; Frank J. Dekker^a ; ^{f.j.dekker@rug.nl}
• 关键词：Lysine demethylation ; Tumorigenesis ; Tranylcypromine ; Irreversible inhibition ; Enzyme labeling
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2017
• 出版时间：1 February 2017
• 年：2017
• 卷：25
• 期：3
• 页码：847-856
• 全文大小：1182 K
• 卷排序：25

文摘

Lysine-specific demethylase 1 (LSD1) can be covalently labeled using tranylcypromine (TCP) based molecules. LSD1 labeling is specific for non-denatured enzymes. Further investigation of the inhibition mechanism of TCP based inhibitors for LSD1 is needed.