5-Lipoxygenase (human, recombinant)

5-Lipoxygenase (5-LO) is an enzyme encoded by ALOX5 in humans that is involved in leukotriene biosynthesis.¹ It is composed of an N-terminal regulatory domain and a C-terminal catalytic domain and is primarily expressed in leukocytes. Increases in intracellular calcium levels or cellular stress induce translocation of 5-LO from the cytosol or nucleoplasm, depending on the cell type and 5-LO phosphorylation status, to the nuclear envelope, where it interacts with 5-LO-activating protein (FLAP), which transfers arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) to 5-LO.^1,2 5-LO catalyzes the conversion of arachidonic acid to 5(S)-HpETE (Item No. 44230) and then to leukotriene A₄ (LTA₄).³ Other substrates of 5-LO include 5,8,11,14,17-eicosapentaenoic acid, 5,8,11-eicosatrienoic acid, 5,8-eicosadienoic acid, 12-HpETE, and 15-HpETE. Alox5 knockout mice are protected against arthritis and pulmonary inflammation.² Knockout of Alox5 also protects apolipoprotein E-deficient hyperlipidemic mice from high-fat diet-induced hepatic injury and inflammation.⁴ Levels of 5-LO are elevated in postmortem hippocampus and cortex of patients with Alzheimer's disease.⁵ Cayman's 5-Lipoxygenase (human, recombinant) can be used for enzyme activity assays.

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1. Rådmark, O., Werz, O., Steinhilber, D., et al. 5-Lipoxygenase, a key enzyme for leukotriene biosynthesis in health and disease. Biochim. Biophys. Acta 1851(4), 331-339 (2015).

2. Martínez-Clemente, M., Clària, J., and Titos, E. The 5-lipoxygenase/leukotriene pathway in obesity, insulin resistance, and fatty liver disease. Curr. Opin. Clin. Nutr. Metab. Care 14(4), 347-353 (2011).

3. Rådmark, O. Arachidonate 5-lipoxygenase. Prostaglandins Other Lipid Mediat. 68-69, 211-234 (2002).

4. Martínez-Clemente, M., Ferré, N., González-Périz, A., et al. 5-lipoxygenase deficiency reduces hepatic inflammation and tumor necrosis factor ɑ-induced hepatocyte damage in hyperlipidemia-prone ApoE-null mice. Hepatology 51(3), 817-827 (2010).

5. Firuzi, O., Zhuo, J., Chinnici, C.M., et al. 5-Lipoxygenase gene disruption reduces amyloid-beta pathology in a mouse model of Alzheimer’s disease. FASEB J. 22(4), 1169-1178 (2008).

Xie, L., Lee, D.Y.-W., Shang, Y., et al. Characterization of spirostanol glycosides and furostanol glycosides from anemarrhenae rhizoma as dual targeted inhibitors of 5-lipoxygenase and Cyclooxygenase-2 by employing a combination of affinity ultrafiltration and HPLC/MS. Phytomedicine 77, 153284 (2020).

Perez, C., Li, J., Parlati, F., et al. Discovery of an inhibitor of the proteasome subunit Rpn11. J. Med. Chem. 60(4), 1343-1361 (2017).

Zhao, X., Lu, W., Song, C., et al. Detection of mammalian 5-lipoxygenase activity using the fluorescent probe dihydrorhodamine 123. Eur. J. Lipid Sci. Technol. 116, 119-125 (2014).