Recent advances in the search for novel 5-lipoxygenase inhibitors.
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| Abstract |
5-Lipoxygenase (5-LO) is an important enzyme of the arachidonic acid cascade and catalyses with the help of FLAP, the 5-LO-activating protein, the formation of bioactive leukotrienes (LTs). LTs are inflammatory mediators playing a pathophysiological role in different diseases such as asthma, allergic rhinitis as well as cardiovascular diseases and certain types of cancer. Up to now, only one 5-LO inhibitor is on the market, zileuton for the treatment of asthma. With the rising number of indications for anti-LT therapy, 5-LO inhibitor drug development becomes more and more important. This MiniReview gives an update on 5-LO inhibitors currently under clinical development. Furthermore, the recent advances in the search for novel 5-lipoxygenase inhibitors with a focus on computational methods are summarized. Currently, licofelone is the compound with the highest clinical development status (completed phase III trials). 5-LO inhibitor screening programmes based on computational methods could deliver several promising drug-like new molecules. These activities can be expected to be driven by the newly resolved structure of human 5-LO in the future, enabling structure-based drug design. For the prospective drugs in late-stage clinical development, the future will show their clinical safety and efficacy in the particular diseases.
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| Authors | Dieter Steinhilber, Bettina Hofmann |
| Journal | Basic & clinical pharmacology & toxicology (Basic Clin Pharmacol Toxicol) Vol. 114 Issue 1 Pg. 70-7 (Jan 2014) ISSN: 1742-7843 [Electronic] England |
| PMID | 23953428 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review) |
| Copyright | © 2013 Nordic Pharmacological Society. Published by John Wiley & Sons Ltd. |
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