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Title: G-protein Coupled Receptors: A Potential Candidate for Drug Discovery
Authors: Pranveer Singh
Journal: International Journal of Pharmacology
Publisher: Asian Network for Scientific Information
Country: Pakistan
Year: 2017
Volume: 13
Issue: 7
Language: English
Keywords: Signal transductionlipid bilayerdrug-targetmembrane proteinProtein-ligand
Protein-protein, protein-ligand and protein-lipid interactions are fundamental to most of the physiological processes. Membrane proteins are particularly very important in this regard as most of the marketed drugs and those under clinical trials target these proteins either activating or inhibiting their activity thus reflecting their importance in human health and disease. This perceived importance warrants the detailed analysis of the process to understand and elucidate the underlying mechanisms behind the process. However, there are significant constraints like lack of high resolution structure, difficulty in getting the sufficient amount of purified protein and crystallization. The advancement in surface chemistry, coupled with modified sensor chips with improvised surface chemistry where lipid bilayer can be created thus, mimicking the native membrane environment have greatly facilitated and revolutionized the kinetic and equilibrium analysis of such interactions. Additional advantages offered by plasmon resonance based techniques include, high sensitivity, accuracy, label free analysis, lesser protein requirement etc. This review highlights the membrane protein interactions with their specific ligands with special emphasis on G-Protein Coupled Receptors (GPCRs), optimized protocols to study such interactions, associated challenges and advantages and disadvantages of each protocols and finally future road map of such studies.
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