A high-throughput mass spectrometric assay for discovery of human lipoxygenase inhibitors and allosteric effectors.

ABSTRACT: Lipoxygenases (LOXs) regulate inflammation through the production of a variety of molecules whose specific downstream effects are not entirely understood due to the complexity of the inflammation pathway. The generation of these biomolecules can potentially be inhibited and/or allosterically regulated by small synthetic molecules. The current work describes the first mass spectrometric high-throughput method for identifying small molecule LOX inhibitors and LOX allosteric effectors that change the substrate preference of human lipoxygenase enzymes. Using a volatile buffer and an acid-labile detergent, enzymatic products can be directly detected using high-performance liquid chromatography-mass spectrometry (HPLC-MS) without the need for organic extraction. The method also reduces the requi

SUBMITTER: Jameson JB 

PROVIDER: S-EPMC4398643 | biostudies-literature | 2015 May

REPOSITORIES: biostudies-literature