Identification of novel small molecule activators of nuclear factor-κB with neuroprotective action via high-throughput screening.

ABSTRACT: Neuronal noncytokine-dependent p50/p65 nuclear factor-κB (the primary NF-κB complex in the brain) activation has been shown to exert neuroprotective actions. Thus neuronal activation of NF-κB could represent a viable neuroprotective target. We have developed a cell-based assay able to detect NF-κB expression enhancement, and through its use we have identified small molecules able to up-regulate NF-κB expression and hence trigger its activation in neurons. We have successfully screened approximately 300,000 compounds and identified 1,647 active compounds. Cluster analysis of the structures within the hit population yielded 14 enriched chemical scaffolds. One high-potency and chemically attractive representative of each of these 14 scaffolds and four singleton structures were selected for fo

SUBMITTER: Manuvakhova MS 

PROVIDER: S-EPMC3280078 | biostudies-literature | 2011 Jan

REPOSITORIES: biostudies-literature