期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 53, 期 2, 页码 911-915出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm9012505
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资金
- LOEWE Lipid Signaling Forschungszentrum Frankfurt (LiFF)
- Beilstein-Institut zur Forderung der Chemischen Wissenschaften
- Frankfurt am Main
- European Graduate School Roles of Eicosanoids in Biology and Medicine [DFG GRK 757/1]
Microsomal prostaglandin E-2-synthase (mPGES-1) is a target for future anti-inflammatory drugs. Inhibitors of mPGES-1 mimicking prostaglandin E-2 often interact with cyclooxygenases (COXs) 1 and 2, leading to unwanted side effects. Selective inhibitors of mPGES-1 can be obtained by deliberate abdication of the acidic groups, which are an important feature of COX inhibition. Here, we present it Successful virtual screening study that results in it potent nonacidic mPGES-1 inhibitor lacking COX Inhibition.
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