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Current Protein & Peptide Science


ISSN (Print): 1389-2037
ISSN (Online): 1875-5550

Recent Advances in Structure and Function Studies on Human Bitter Taste Receptors

Author(s): Sai Prasad Pydi, Jasbir Upadhyaya, Nisha Singh, Rajinder Pal Bhullar and Prashen Chelikani

Volume 13, Issue 6, 2012

Page: [501 - 508] Pages: 8

DOI: 10.2174/138920312803582942

Price: $65


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

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