The DOI matches its Crossref record; 12 of the 12 references it cites were found in a registry or an index.
MK886, a potent and specific leukotriene biosynthesis inhibitor blocks and reverses the membrane association of 5-lipoxygenase in ionophore-challenged leukocytes.
Open accessAbstract
Recently, we have shown that ionophore activation of human leukocytes results in leukotriene synthesis and a translocation of 5-lipoxygenase from the cytosol to cellular membrane. This membrane translocation was postulated to be an important early activation step for the enzyme. 3-[1-(p-Chlorobenzyl)-5-(isopropyl)-3-tert-butylthioindol-2-yl]-2, 2- dimethylpropanoic acid (MK886) is a potent and specific inhibitor of leukotriene biosynthesis in vivo and in intact cells, but has no direct effect on 5-lipoxygenase activity in cell-free systems. In this report, we show that MK886 can both prevent and reverse the membrane translocation of 5-lipoxygenase, in conjunction with the inhibition of leukotriene synthesis. Similar compounds of the indole class could also inhibit the membrane translocation of 5-lipoxygenase in a rank order of potency that correlated with their potencies for leukotriene synthesis inhibition. In contrast L-656,224, a direct 5-lipoxygenase inhibitor, had no effect on the translocation of the enzyme. Attempts to demonstrate the effects of MK886 on the association of 5-lipoxygenase with membrane in cell-free preparations failed due to a nonspecific Ca2+-dependent sedimentation of the enzyme. The mechanism of action of MK-886 is therefore to block translocation, prevent subsequent activation of 5-lipoxygenase, and hence block cellular leukotriene biosynthesis.
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Cites
Leukotrienes: Mediators of Immediate Hypersensitivity Reactions and Inflammation
Samuelsson, B. (1983) · Science · doi:10.1126/science.6301011 · Cited by 2,843
Borgeat, P., & Samuelsson, B. (1979) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.76.7.3213 · Cited by 470
Gillard, J. W., Ford‐Hutchinson, A. W., Chan, C.-C., Charleson, S. E., Denis, D., Foster, A., Fortin, R., Léger, S., McFarlane, C. S., Morton, H. E., et al. (1989) · Canadian Journal of Physiology and Pharmacology · doi:10.1139/y89-073 · Cited by 324
Self-citationRouzer, C. A., & Kargman, S. (1988) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(18)38066-9 · Cited by 319
Self-citationRouzer, C. A., Matsumoto, T., & Samuelsson, B. (1986) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.83.4.857 · Cited by 305
Self-citationPharmacology of L-660,711 (MK-571): a novel potent and selective leukotriene D4 receptor antagonist
Jones, T. R., Zamboni, R., Belley, M., Champion, E., Charette, L., Ford-Hutchinson, A. W., Frenette, R., Gauthier, J.-Y., Leger, S., Masson, P., et al. (1989) · Canadian Journal of Physiology and Pharmacology · doi:10.1139/y89-004 · Cited by 270
Self-citationRouzer, C. A., & Samuelsson, B. O. (1985) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.82.18.6040 · Cited by 253
Self-citationUeda, N., Kaneko, S., Yoshimoto, T., & Yamamoto, S. (1986) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(19)57499-3 · Cited by 189
Shimizu, T., Izumi, T., Seyama, Y., Tadokoro, K., Rådmark, O., & Samuelsson, B. (1986) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.83.12.4175 · Cited by 173
Rouzer, C. A., Shimizu, T., & Samuelsson, B. O. (1985) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.82.22.7505 · Cited by 101
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Lewis (1990) · doi:10.1056/nejm199009063231006 · Cited by 1,200
Lipoxygenase and leukotriene pathways: biochemistry, biology, and roles in disease
Haeggström, J. Z., & Funk, C. D. (2011) · Chemical Reviews · doi:10.1021/cr200246d · Cited by 875
Role of ABCC1 in export of sphingosine-1-phosphate from mast cells
Mitra, P., Oskeritzian, C. A., Payne, S. G., Beaven, M. A., Milstien, S., & Spiegel, S. (2006) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0603734103 · Cited by 407
Metadata
- Authors
- Rouzer, C. A., Ford-Hutchinson, A. W., Morton, H. E., & Gillard, J. W.
- Venue
- Journal of Biological Chemistry
- Publisher
- Elsevier BV
- Published
- 1990-01
- Volume
- 265
- Issue
- 3
- Pages
- 1436-1442
- ISSN
- 0021-9258 (ISSN-L)
- OpenAlex
- W1520264805
- Cited by
- 314
- References
- 12
- FWCI
- 33.83
- Type
- journal article
- Language
- en
- Open access
- hybrid
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- Rouzer, C. A., Ford-Hutchinson, A. W., Morton, H. E., & Gillard, J. W. (1990). MK886, a potent and specific leukotriene biosynthesis inhibitor blocks and reverses the membrane association of 5-lipoxygenase in ionophore-challenged leukocytes. Journal of Biological Chemistry. https://doi.org/10.1016/s0021-9258(19)40034-3
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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