title: 5-Lipoxygenase inhibitors: a review of recent developments and patents.
abstract: BACKGROUND
  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.
  
  
  METHODS
  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.
  
  
  RESULTS
  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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: Eberhard-Karls-University Tuebingen, Pharmaceutical Institute, Department of Pharmaceutical Analytics, Auf der Morgenstelle 8, 72076 Tuebingen, Germany.
authors.forename: Carlo
authors.initials: C
authors.lastname: Pergola
authors.forename: Oliver
authors.initials: O
authors.lastname: Werz
mesh_terms: D000818:Animals; D002318:Cardiovascular Diseases / Q000188:drug therapy / Q000503:physiopathology; D016503:Drug Delivery Systems; D015195:Drug Design; D006801:Humans; D016859:Lipoxygenase Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D009369:Neoplasms / Q000188:drug therapy / Q000503:physiopathology; D010024:Osteoporosis / Q000188:drug therapy / Q000503:physiopathology; D010330:Patents as Topic
chemical_list: D016859:Lipoxygenase Inhibitors