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Discovery of 2,3-diaminoindole derivatives as a novel class of NOD antagonists [Elektronski vir]Russo, Camilla ...NOD1 and NOD2 are members of the pattern recognition receptors involved in the innate immune response. Overactivation of NOD1 is implicated in inflammatory disorders, multiple sclerosis, and cancer ... cell metastases. NOD1 antagonists would represent valuable pharmacological tools to gain further insight into protein roles, potentially leading to new therapeutic strategies. We herein report the expansion of the chemical space of NOD1 antagonists via a multicomponent synthetic approach affording a novel chemotype, namely, 2,3-diaminoindoles. These efforts resulted in compound 37, endowed with low micromolar affinity toward NOD1. Importantly, a proof-of-evidence of direct binding to NOD1 of Noditinib-1 and derivative 37 is provided here for the first time. Additionally, the combination of computational studies and NMR-based displacement assays enabled the characterization of the binding modality of 37 to NOD1, thus providing key unprecedented knowledge for the design of potent and selective NOD1 antagonists.Type of material - e-article ; adult, seriousPublish date - 2024Language - englishCOBISS.SI-ID - 183800579
Author
Russo, Camilla |
Russomanno, Pasquale |
D’Amore, Vincenzo Maria |
Alfano, Antonella Ilenia |
Santoro, Federica |
Guzelj, Samo |
Gobec, Martina, 1983- |
Amato, Jussara |
Pagano, Bruno |
Jakopin, Žiga
Topics
Peptidi |
Proteini |
Imunski odziv |
antagonists |
assays |
indoles |
peptides |
proteins |
reaction products |
antagonisti |
testi |
indoli |
reakcijski produkti
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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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Russo, Camilla | |
Russomanno, Pasquale | |
D’Amore, Vincenzo Maria | |
Alfano, Antonella Ilenia | |
Santoro, Federica | |
Guzelj, Samo | 52379 |
Gobec, Martina, 1983- | 32034 |
Amato, Jussara | |
Pagano, Bruno | |
Jakopin, Žiga | 26496 |
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