5-Lipoxygenase (5-LO) is the key enzyme involved in the synthesis of pro-inflammatory leukotrienes (LTs)
and has become a prime target for new drug discovery research and development efforts by the pharmaceutical and biotech
industry. The pathophysiological effects of LTs can be modulated by the selective inhibition of 5-LO. In this review,
we summarize the established dogma and recent progress on the biochemical and pharmacological regulation of 5-LO and
its diverse cellular partners. In the last decade, significant research efforts have led to the exploitation of 5-LO pathway
for developing new drugs against inflammatory diseases. Despite few setbacks, a number of promising molecules have
moved into clinical development. These fundamental discoveries and proof-of-concept studies will ultimately be helpful
in delineating how 5-LO pathway participates in the development of disease phenotype and what are possible key biomarkers
of disease progression and regression. Elucidation of molecular mechanism-of-action of 5-LO in individual cell
types will pave the way for improving efficacy parameters. Taken together, this combined knowledge about the 5-LO
pathway would be helpful in planning collaborative and targeted R&D efforts, by the academic laboratories and pharmaceutical/
biotech industry, for the discovery and development of novel, efficacious and safer drugs against multiple diseases.
Keywords: Cytokines, 5-Lipoxygenase, leukotrienes, new drug discovery, small molecules.
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