Anti-inflammatory Molecules: Enzyme Inhibitors
Structure/receptor-based drug design, a new approach of drug discovery, has become a fascinating area of drug discovery/development. This rational approach of drug discovery may lead to the production of many drugs, and some products developed based on th
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Anti-inflammatory Molecules: Enzyme Inhibitors C.S. Sharanya and Madathilkovilakath Haridas
Abstract
Structure/receptor-based drug design, a new approach of drug discovery, has become a fascinating area of drug discovery/development. This rational approach of drug discovery may lead to the production of many drugs, and some products developed based on this approach are presently available in the market. Examples of some of these drugs include saquinavir for the treatment of AIDS, captopril against hypertension, dorzolamide for glaucoma and Zanamivir against influenza. Many molecules are designed based on their structure or receptors and are under different stages of clinical trials. For applying rational approach, we have to first identify the pathway of pathogenesis and the target proteins related to the specific disease. After the identification of the specific protein, the compound which inhibits the target protein may be designed to fit into the binding site of the protein most appropriately. Compounds from natural sources are tested first, taking cues from various kinds of information. Such compounds may form a basic structure which could be appropriated to the binding site of the target protein. This chapter has been devoted to the inhibitors of the enzymes in the arachidonic acid pathway which may serve as anti-inflammatory compounds. Target enzymes of inflammatory pathway include isozymes of phospholipase A2 (PLA2), cyclooxygenase (COX) and lipoxygenase (LOX). Keywords
Inflammation • Phospholipase A2 inhibitors • Cyclooxygenase inhibitors • Lipoxygenase inhibitors
C.S. Sharanya • M. Haridas (*) Inter University Centre for Bioscience, Department of Biotechnology and Microbiology, Kannur University, Thalassery Campus, Kannur, Kerala 670661, India e-mail: [email protected] © Springer Nature Singapore Pte Ltd. 2017 S. Sugathan et al. (eds.), Bioresources and Bioprocess in Biotechnology, DOI 10.1007/978-981-10-4284-3_9
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C.S. Sharanya and M. Haridas
Introduction
The most general and fundamental indicator of all pathological conditions initiates with inflammation, a general form of resistance broadly defined as a non-specific response to tissue malfunction, and it is employed by immune systems to combat pathogenic invaders (Ashley 2012).The Roman encyclopaedist Aulus Cornelius Celsus described four principal effects of inflammation which were rubor, tumor, calor and dolor and finally loss of function which was added by Virchow. Inflammation is initiated by the presence of physical agents, chemicals, microorganisms, inappropriate immunological responses and tissue death. An important stimulus of inflammation is caused by the endotoxins of bacteria and viruses. Viruses mediate inflammation by entering and destroying the cells of the body. Loss of blood flow causes tissue death due to lack of oxygen or nutrients, which also results in inflammation. Inflammation is a major problem associated with diseases like rheumatoid arthritis, cancer, obesity, neurodegenerative diseases, type 2 diab
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