Record Details

Structure and Ligand Based Drug Design Strategies in the Development of Novel 5-LOX Inhibitors
IR @ National Institute of Animal Biotechnology
Title
Structure and Ligand Based Drug Design Strategies in the Development of Novel 5-LOX Inhibitors
Creator
Aparoy, P. Reddy, K. K. Reddanna, P.
Description
"Lipoxygenases (LOXs) are non-heme iron containing dioxygenases involved in the oxygenation of polyunsaturated fatty acids (PUFAs) such as arachidonic acid (AA). Depending on the position of insertion of oxygen, LOXs are classified into 5-, 8-, 9-, 12- and 15-LOX. Among these, 5-LOX is the most predominant isoform associated with the formation of 5-hydroperoxyeicosatetraenoic acid (5-HpETE), the precursor of non-peptido (LTB4) and peptido (LTC4, LTD4, and LTE4) leukotrienes. LTs are involved in inflammatory and allergic diseases like asthma, ulcerative colitis, rhinitis and also in cancer. Consequently 5-LOX has become target for the development of therapeutic molecules for treatment of various inflammatory disorders. Zileuton is one such inhibitor of 5-LOX approved for the treatment of asthma. In the recent times, computer aided drug design (CADD) strategies have been applied successfully in drug development processes. A comprehensive review on structure based drug design strategies in the development of novel 5-LOX inhibitors is presented in this article. Since the crystal structure of 5-LOX has been recently solved, efforts to develop 5-LOX inhibitors have mostly relied on ligand based rational approaches. The present review provides a comprehensive survey on these strategies in the development of 5-LOX inhibitors."
Publisher
Date
2012
Type
Article PeerReviewed
Identifier
Aparoy, P. and Reddy, K. K. and Reddanna, P. (2012) Structure and Ligand Based Drug Design Strategies in the Development of Novel 5-LOX Inhibitors. Current Medicinal Chemistry, 19 (22). pp. 3763-3778.
Language