Development ofNovel Phospholipase A2 Inhibitors Using Molecular and Computational Techniques
Journal Title: IOSR Journal of Pharmacy and Biological Sciences (IOSR-JPBS) - Year 2018, Vol 13, Issue 2
Abstract
Phospholipase A2 Enzymesare Basically Of Three Types i.e The Cytosolic PLA2, Secretory Phospholipase A2And Lipoprotein Associated PLA2. There Is Growing Interest In Developing Novel And Potent PLA2Inhibitors For Various Therapeutic Purposes E.G Alzheimer’s Disease, Allergic Conditons, Arthritis And Cancer, Cardiovascular Disorders And To Counter The Envenomation By Bee, Spider And Snake Bites. One Of The Excellent Example Is Darapladib Which Is An Effective And Potent Inhibitor Of The Lipoprotein Associated PLA2and Is Used For Clinical Conditions. On The Other Hand Computational Studies Conducted On The Numerous Snake Species Having Endogenous Phospholipase A2Inhibitors, Can Be Exploited For Therapeutic Purposes. This Inhibitor Type Is Generally Known As Snake Blood Phospholipase A2 Inhibitors (Sbplis). Most, If Not All Sbplis Are Oligomeric Glycosylated Proteins, Although The Carbohydrate Moiety May Not Be Important For PLA2Inhibition In Most Cases.Western Blot Analysis After Partial Purification With SPLA2-IB-Affinity Column Has Confirmed The Identity Of Serum Spla2 Binding Protein As A Soluble Form Of PLA2R (SPLA2r) That Retained All Of The Extracellular Domains Of The Membrane-Bound Receptor. This Review Article Has Tried To Encompass The Recent Advances In The Development Of Novel And Potent PLA2 Inhibitors, Both Endogenous And Synthetic In Nature.
Authors and Affiliations
Manoj G Tyagi, Dinesh J Vyas, Vinita Ernest, Debjyoti Mukherjee
Keywords
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- EP ID EP394491
- DOI 10.9790/3008-1302020512
- Views 50
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