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Selective inhibition of TRPM2 channel by two novel synthesized ADPR analogues
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2017-11-15 00:11:47 , DOI: 10.1111/cbdd.13119
Xiao Luo 1 , Meng Li 2 , Kaiyu Zhan 3 , Wei Yang 3 , Lihe Zhang 1 , KeWei Wang 2, 4 , Peilin Yu 5 , Liangren Zhang 1
Affiliation  

A series of adenosine 5′-diphosphoribose (ADPR) analogues were synthesized for discovering novel and selective TRPM2 inhibitors. Two compounds, 7i and 8a, were identified as TRPM2 inhibitors with IC50 of 5.7 and 5.4 μm, respectively, selective against TRPM7, TRPM8, TRPV1 and TRPV3. These two novels and TRP-subtype selective TRPM2 inhibitors can be used as tool for further investigation of the channel pharmacology.

中文翻译:

两种新型合成ADPR类似物对TRPM2通道的选择性抑制

合成了一系列腺苷5'-二磷酸核糖(ADPR)类似物,用于发现新型的选择性TRPM2抑制剂。两种化合物,7I8a中,被确定为TRPM2抑制剂与IC 50的5.7和5.4μ,分别针对TRPM7,TRPM8,TRPV1和TRPV3选择性。这两种新型药物和TRP亚型选择性TRPM2抑制剂可用作进一步研究通道药理学的工具。
更新日期:2017-11-15
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