Abstract
Humans are capable of sensing five basic tastes and of these, bitter taste sensation alone, is mediated by a large group of 25 cell surface proteins known as, bitter taste receptors (T2Rs). T2Rs belong to the G-protein coupled receptor (GPCR) superfamily. However, they share little homology with the large subfamily of Class A GPCRs. Very little progress has been made in understanding the dynamics of T2R activation, and in discovery of molecules that can block (bitter blockers) T2R activation. Only recently few structure-function studies focused on elucidating the ligand binding mechanisms of T2Rs have been published. Here we will discuss the roles of conserved amino acids in T2R structure-function, possible mechanisms of activation of T2Rs, and compare and contrast with the recent crystal structures of the Class A GPCRs.
Keywords: G-protein coupled receptors (GPCRs), bitter taste receptors (T2Rs), structure-function analysis, T2R heterologous expression, T2R ligand binding, T2R receptor activation mechanism(s), bitter blockers, receptor-expressing cells, Extra-Oral Tissues, GPCRs
Current Protein & Peptide Science
Title:Recent Advances in Structure and Function Studies on Human Bitter Taste Receptors
Volume: 13 Issue: 6
Author(s): Sai Prasad Pydi, Jasbir Upadhyaya, Nisha Singh, Rajinder Pal Bhullar and Prashen Chelikani
Affiliation:
Keywords: G-protein coupled receptors (GPCRs), bitter taste receptors (T2Rs), structure-function analysis, T2R heterologous expression, T2R ligand binding, T2R receptor activation mechanism(s), bitter blockers, receptor-expressing cells, Extra-Oral Tissues, GPCRs
Abstract: Humans are capable of sensing five basic tastes and of these, bitter taste sensation alone, is mediated by a large group of 25 cell surface proteins known as, bitter taste receptors (T2Rs). T2Rs belong to the G-protein coupled receptor (GPCR) superfamily. However, they share little homology with the large subfamily of Class A GPCRs. Very little progress has been made in understanding the dynamics of T2R activation, and in discovery of molecules that can block (bitter blockers) T2R activation. Only recently few structure-function studies focused on elucidating the ligand binding mechanisms of T2Rs have been published. Here we will discuss the roles of conserved amino acids in T2R structure-function, possible mechanisms of activation of T2Rs, and compare and contrast with the recent crystal structures of the Class A GPCRs.
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Cite this article as:
Prasad Pydi Sai, Upadhyaya Jasbir, Singh Nisha, Pal Bhullar Rajinder and Chelikani Prashen, Recent Advances in Structure and Function Studies on Human Bitter Taste Receptors, Current Protein & Peptide Science 2012; 13 (6) . https://dx.doi.org/10.2174/138920312803582942
DOI https://dx.doi.org/10.2174/138920312803582942 |
Print ISSN 1389-2037 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5550 |
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