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Title: Characterization of human bitter taste receptor T2R1
Authors: Upadhyaya, Jasbir Deol
Supervisor: Chelikani, Prashen (Oral Biology)
Examining Committee: Parkinson, Fiona (Pharmacology and Therapeutics) Bhullar, Raj (Oral Biology)
Graduation Date: October 2010
Keywords: T2R1
Molecular modeling
C6 glial cells
Issue Date: 10-Sep-2010
Citation: Upadhyaya, Jasbir (2010) BBRC 398 (2) : 331-335
Abstract: Bitter taste signaling in humans is mediated by a group of 25 bitter receptors (T2Rs) that belong to the G-protein coupled receptor (GPCR) family. Previously, several bitter peptides were isolated and characterized from bitter tasting food protein derived extracts, such as pea protein and soya bean extracts. However, their molecular targets in humans were poorly characterized. In this study, we tested the ability of the bitter tasting tri- and di-peptides to activate the human bitter receptor, T2R1. Using a heterologous expression system, T2R1 gene was transiently expressed in C6-glioma cells and changes in intracellular calcium were measured following addition of the peptides. We found that the bitter tasting tri-peptides are more potent in activating T2R1 than the di-peptides tested. Furthermore, to elucidate the potential ligand binding pocket of T2R1 we used homology molecular modeling. The ligand binding pocket in T2R1 is present on the extracellular surface of the receptor, and is formed by the transmembrane helices 1, 2, 3 and 7 and with extracellular loops 1 and 2.
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