Selective inhibition of TRPM2 channel by two novel synthesized ADPR analogues,Chemical Biology & Drug Design

当前位置： X-MOL 学术 › Chem. Bio. Drug Des. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

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，7I和8a中，被确定为TRPM2抑制剂与IC ₅₀的5.7和5.4μ米，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

点击分享查看原文

点击收藏

公开下载

阅读更多本刊最新论文本刊介绍/投稿指南11