Project highlights: a small set of NOX-1 inhibitors were synthesized. Further screening and development for NOX-1 inhibitors will be pursued. Current efforts focused on developing more selective and potent 12-LOX inhibitors with improved ADME properties to use in in vivo models. During this period, the NCGC has fostered and maintained over 180 active collaborations with both NIH and extramural investigators, facilitating drug discovery efforts across the entire spectrum of human disease. These efforts have led to over 100 high-throughput screens and nearly 60 medicinal chemistry campaigns, providing our collaborators and the general research community a wealth of publications and promising small molecule leads. In addition, the NCGC has undertaken a number of informatic challenges to make better use of existing drug and disease target information and provide the general public with easily accessible resources, further catalyzing the development of new therapies for human disease.
| Armstrong, Michelle M; Freedman, Cody J; Jung, Joo Eun et al. (2016) A potent and selective inhibitor targeting human and murine 12/15-LOX. Bioorg Med Chem 24:1183-90 |
| Taylor-Fishwick, David A; Weaver, Jessica; Glenn, Lindsey et al. (2015) Selective inhibition of 12-lipoxygenase protects islets and beta cells from inflammatory cytokine-mediated beta cell dysfunction. Diabetologia 58:549-57 |
| Rai, Ganesha; Joshi, Netra; Jung, Joo Eun et al. (2014) Potent and selective inhibitors of human reticulocyte 12/15-lipoxygenase as anti-stroke therapies. J Med Chem 57:4035-48 |
