Discovery of ML351, a Potent and Selective Inhibitor of Human 15-Lipoxygenase-1
Bethesda, United States. In Unknown Journal, 2013
Toward this end, we employed a quantitative high-throughput (qHTS) screen against ∼74,000 small molecules which led to the discovery of ML351, a novel chemotype for 15-LOX-1 inhibition, that displays nanomolar potency (IC50 = 200 nM) and excellent selectivity (>250-fold) versus the related isozymes, 5-LOX, platelet 12-LOX, 15-LOX-2, ovine COX-1, and human COX-2.
Tocotrienols: the lesser known form of natural vitamin E.
Columbus, United States. In Indian J Exp Biol, 2011
Tocotrienols have garnered much of this recent attention, and in particular alpha-tocotrienol has been shown to be the most potent neuroprotective form of vitamin E. Protection exclusively mediated through tocotrienols has been arbitrated to many mechanisms including inhibition of 12-LOX, c-Src, PLA2 and through up-regulation of MRP1.