During this period, the NCGC has worked to further advance the selective 12-LOX inhibitors identified previously through ADME characterization. As a center, the NCGC has fostered and maintained over 130 active collaborations with both NIH and extramural investigators, facilitating drug discovery efforts across the entire spectrum of human disease. These efforts have led to dozens of high-throughput screens and a number of medicinal chemistry campaigns to further improve on screening hits, providing our collaborators and the general research community with publications and a variety of promising small molecule probes and leads. In addition, the NCGC has worked to advance a number of informatic initiatives 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 |