5-Lipoxygenase Inhibitors: Bones, Cardio, and Cancer

Byron's Comments:

The importance of regulating the excess activity of the 5-Lipoxygenase enzyme to help prevent a variety of major health problems.

Study Title:

5-Lipoxygenase inhibitors: a review of recent developments and patents.

Study Abstract:

IMPORTANCE TO THE FIELD: Leukotrienes (LTs) are pivotal lipid mediators of inflammation and allergy and results from recent studies also suggest roles of LTs in cardiovascular diseases, cancer and osteoporosis. 5-Lipoxygenase (5-LO) catalyzes the first step in the biosynthesis of LTs from arachidonic acid, and based on the multiple potent pathophysiological actions of LTs, the pharmacological intervention with 5-LO is a challenge in the development of therapeutics.

AREAS COVERED IN THIS REVIEW: We first summarize the biochemical regulation of 5-LO and the general pharmacological concepts in 5-LO inhibition by currently available compounds, and subsequently we report recent developments deduced from recent scientific publications and patents.

WHAT THE READER WILL GAIN: A comprehensive overview about the different molecular pharmacological strategies to inhibit 5-LO and the most successful previous 5-LO inhibitors. The review also gives insights into novel concepts, for example, dual prostaglandin/LT synthesis inhibition and reveals novel compounds patented or developed within the past 5 years.

TAKE HOME MESSAGE: Despite the increasing therapeutic indications of anti-LT therapy, the progress in the development of novel 5-LO inhibitors is moderate. However, novel molecular concepts in the intervention with LT biosynthesis seem promising.

Study Information:

Pergola C, Werz O. 5-Lipoxygenase inhibitors: a review of recent developments and patents. Expert Opin Ther Pat. 2010 March 20(3):355-75.
Eberhard-Karls-University Tuebingen, Pharmaceutical Institute, Department of Pharmaceutical Analytics, Auf der Morgenstelle 8, 72076 Tuebingen, Germany.

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