1H NMR-based assay for lysine demethylase LSD1 and its application to inhibitor screening
Hui Wang , Minghui Shu , Xiaofan Li , Wei-Guo Zhu , He Wen , Zebin Mao
Genome Instability & Disease ›› 2021, Vol. 2 ›› Issue (5) : 302 -308.
1H NMR-based assay for lysine demethylase LSD1 and its application to inhibitor screening
Lysine-specific demethylase 1 (LSD1) with oxidation activity that relies on flavin adenine dinucleotide (FAD) to subsequently produce formaldehyde have been associated with various types of cancers. Here, we report an NMR-based assay for detecting the LSD1 enzyme activity. Our approach can be performed in a reaction buffer without any extraction step, achieve a time-dependent absolute quantification, and be useful for the enzyme inhibitor screening. This precise assay allows us to develop new inhibitors of the LSD1 as anticancer agents.
national natural science foundation of china(81530074)
science and technology program of guangdong province in china(2017B030301016)
shenzhen municipal commission of science and technology innovation(JCYJ20200109114214463)
science and technology foundation of shenzhen city(JCYJ20170302144650949)
natural science foundation of guangdong province(2017A030310459)
natural science foundation of szu(2017085)
national key r&d program of china(2017YFA0503900)
shenzhen bay laboratory(SZBL2019062801011)
discipline construction funding of shenzhen((2016)1452)
shenzhen peacock plan
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