Abstract
The enzyme phospholipase A2 catalyzes the cleavage of the sn-2 acyl ester bond of phospholipids, leading to the production of free fatty acids and lysophospholipids, which leads to many inflammatory disorders. In view of its pharmaceutical interest, three phospholipase A2 + inhibitor (namely, (i) L-1-O-octyl-2-heptylphosphonyl-sn-glycero-3- phosphoethanolamine, Transition State Analogue, (ii) 1-Hexadecyl-3-(trifluoroethyl)-sn-glycero-2-phosphomethanol, MJ33 and (iii) p-methoxybenzoic acid, anisic acid) complex structures have already been solved and analysed, using the data obtained from X-ray diffraction. These structures provide insight on the mode of binding of the inhibitor molecules at the active site of phospholipase A2. The knowledge of the active site geometry in these inhibitor bound structures, yield valuable information in the design of more useful therapeutic agents. This report reviews only the inhibitor bound recombinant bovine pancreatic phospholipase A2 structures solved using X-ray crystallography.
Keywords: X-ray crystallography, phospholipase A2, extra cellular, drug/inhibitor molecules, surface loop, inflammation and rheumatoid arthritis
Current Topics in Medicinal Chemistry
Title: Structural Biology of Recombinant Bovine Pancreatic Phospholipase A2 and its Inhibitor Complexes
Volume: 7 Issue: 8
Author(s): K. Sekar
Affiliation:
Keywords: X-ray crystallography, phospholipase A2, extra cellular, drug/inhibitor molecules, surface loop, inflammation and rheumatoid arthritis
Abstract: The enzyme phospholipase A2 catalyzes the cleavage of the sn-2 acyl ester bond of phospholipids, leading to the production of free fatty acids and lysophospholipids, which leads to many inflammatory disorders. In view of its pharmaceutical interest, three phospholipase A2 + inhibitor (namely, (i) L-1-O-octyl-2-heptylphosphonyl-sn-glycero-3- phosphoethanolamine, Transition State Analogue, (ii) 1-Hexadecyl-3-(trifluoroethyl)-sn-glycero-2-phosphomethanol, MJ33 and (iii) p-methoxybenzoic acid, anisic acid) complex structures have already been solved and analysed, using the data obtained from X-ray diffraction. These structures provide insight on the mode of binding of the inhibitor molecules at the active site of phospholipase A2. The knowledge of the active site geometry in these inhibitor bound structures, yield valuable information in the design of more useful therapeutic agents. This report reviews only the inhibitor bound recombinant bovine pancreatic phospholipase A2 structures solved using X-ray crystallography.
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Cite this article as:
Sekar K., Structural Biology of Recombinant Bovine Pancreatic Phospholipase A2 and its Inhibitor Complexes, Current Topics in Medicinal Chemistry 2007; 7 (8) . https://dx.doi.org/10.2174/156802607780487632
DOI https://dx.doi.org/10.2174/156802607780487632 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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