Identification of indole scaffold-based dual inhibitors of NOD1 and NOD2
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- 作者：Kaja Keček Ple&scaron ; ec ; Dunja Urbančič ; Martina Gobec ; Aleksandra Peko&scaron ; ak ; Tihomir Toma&scaron ; ič ; Marko Anderluh ; Irena Mlinarič-Ra&scaron ; čan ; Žiga Jakopin ; ziga.jakopin@ffa.uni-lj.si" class="auth_mail" title="E-mail the corresponding author
- 关键词：C12-iE-DAP ; lauroyl-γ-d-glutamyl-meso-diaminopimelic acid ; iE-DAP ; γ-d-glutamyl-meso-diaminopimelic acid ; IL ; interleukin ; MAPK ; mitogen-activated protein kinase ; NF-κB ; nuclear factor κB ; NOD ; nucleotide-binding oligomerization domain protein ; PAMP ; pathogen-associated molecular pattern ; RA ; residual activity ; RIP2 ; receptor-interacting serine&ndash ; threonine protein kinase ; SAR ; structure&ndash ; activity relationship ; SEAP ; secreted embryonic alkaline phosphatase
- 刊名：Bioorganic & Medicinal Chemistry
- 出版年：2016
- 出版时间：1 November 2016
- 年：2016
- 卷：24
- 期：21
- 页码：5221-5234
- 全文大小：1263 K
文摘
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Structurally novel inhibitors of NOD proteins were discovered using ligand-based design.
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2-Ethoxycarbonylindoles were identified as potent mixed inhibitors of NOD1 and NOD2.
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Results enable a deeper understanding of the structural requirements for NOD1 and NOD2 inhibition.