STRUCTURAL BIOLOGY

5-LOX inhibition by natural products

The enzyme 5-lipoxygenase (5-LOX) initiates the biosynthesis of leukotrienes (LT), potent mediators of the inflammatory response. The first crystal structures of two complexes of inhibitor bound to 5-LOX reveal the functional consequences of the binding, including a change in the regiospecificity toward a 12/15-lipoxygenating enzyme.

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Fig. 1: 5-LOX catalyzes the conversion of AA to LT through the formation of 5-HETE as an intermediate.

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Correspondence to Homero Rubbo.

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Rubbo, H., Wood, I. 5-LOX inhibition by natural products. Nat Chem Biol 16, 714–715 (2020). https://doi.org/10.1038/s41589-020-0568-z

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