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Identification of indole scaffold-based dual inhibitors of NOD1 and NOD2Keček, Kaja, [1987-] ...NOD1 and NOD2 are important members of the pattern recognition receptor family and play a crucial role within the context of innate immunity. However, overactivation of NODs, especially of NOD1, has ... also been implicated in a number of diseases. Surprisingly, NOD1 remains a virtually unexploited target in this respect. To gain additional insight into the structure-activity relationships of NOD1 inhibitors, a series of novel analogs has been designed and synthesized and then screened for their NOD1-inhibitory activity. Selected compounds were also investigated for their NOD2-inhibitory activity. Two compounds 4 and 15, were identified as potent mixed inhibitors of NOD1 and NOD2, displaying a balanced inhibitory activity on both targets in the low micromolar range. The results obtained have enabled a deeper understanding of the structural requirements for NOD1 and NOD2 inhibition.Source: Bioorganic & Medicinal Chemistry. - ISSN 0968-0896 (Vol. 24, iss 21, 2016, str. 5221-5234)Type of material - article, component part ; adult, seriousPublish date - 2016Language - englishCOBISS.SI-ID - 4145009
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Keček, Kaja, [1987-] | |
Urbančič, Dunja, farmacevtka | 34512 |
Gobec, Martina, 1983- | 32034 |
Pekošak, Aleksandra, farmacevtka | |
Tomašič, Tihomir | 28334 |
Anderluh, Marko | 21456 |
Mlinarič-Raščan, Irena | 12443 |
Jakopin, Žiga | 26496 |
Source: Personal bibliographies
and: SICRIS
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