Abstract
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.
Current Drug Targets
Title:5-Lipoxygenase: A Promising Drug Target Against Inflammatory Diseases-Biochemical and Pharmacological Regulation
Volume: 15 Issue: 4
Author(s): Yasir Anwar, Jamal S.M. Sabir, Muhammad I. Qureshi and Kulvinder S. Saini
Affiliation:
Keywords: Cytokines, 5-Lipoxygenase, leukotrienes, new drug discovery, small molecules.
Abstract: 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.
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Cite this article as:
Anwar Yasir, Sabir S.M. Jamal, Qureshi I. Muhammad and Saini S. Kulvinder, 5-Lipoxygenase: A Promising Drug Target Against Inflammatory Diseases-Biochemical and Pharmacological Regulation, Current Drug Targets 2014; 15 (4) . https://dx.doi.org/10.2174/1389450114666131209110745
DOI https://dx.doi.org/10.2174/1389450114666131209110745 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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