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High Throughput Screening Assays for NOD1 Inhibitors - Probe 2.


Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Feb 28 [updated 2010 Oct 4].


The modulation of immune response activity is one of the major goals in the development of novel therapeutics for human immune or inflammatory diseases. The innate system resides at the intersection of the pathways of microbial recognition, inflammation, and cell death, thereby offering various therapeutic targets. In this context, NOD1 and NOD2 are of particular interest, since they recognize distinct structures derived from bacterial peptidoglycans and directly activate the NF-κB pathway, which controls the production of proinflammatory molecules. Mutations in the NOD1 and NOD2 genes are associated with a number of human inflammatory disorders, including Crohn's disease (CD), Blau syndrome, early-onset sarcoidosis, and atopic diseases, which characteristically cause constitutive NF-κB activation. Thus, small molecule inhibitors of NOD1 would provide powerful research tools for elucidating the roles of these proteins in modulating immune response in primary cultured cells from humans and in animal models. This probe report describes ML146 (CID-5310346), a second specific inhibitor of the NOD1-mediated activation of NF-κB of a new chemical class (purine-2,6-dione) compared to the previously submitted NOD1 specific inhibitor, ML130 (CID-1088438). While this probe is not as potent or selective as the first probe, CID-1088438, it does meet probe criteria and represents a second bona fide scaffold for a NOD1 selective probe.

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