Bitter taste receptor T2R1 is activated by dipeptides and tripeptides

Upadhyaya, Jasbir; Pydi, Sai Prasad; Singh, Nisha; Aluko, Rotimi E.; Chelikani, Prashen

doi:10.1016/j.bbrc.2010.06.097

Cited by 72 publications

(77 citation statements)

References 23 publications

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“…Calcium Assays-Glial cells have comparatively lower basal calcium noise compared with HEK293 for DXM, and thus we were able to do a dose-response analysis for T2R1 activation by DXM in glial cells, according to previously published protocols (15). In addition, we have shown that glial cells do not expresses endogenous T2R1 (15).…”

Section: Methodsmentioning

confidence: 95%

“…Sensory analysis of the compounds tested shows that DXM has the most intense bitterness, with a predicted bitterness score of 12.87 (supplemental Table 1). In addition, our previous study on T2R1 using different ligands showed that DXM activates T2R1 with the highest potency (15). Based on the sensory analysis and EC 50 value for T2R1, DXM was selected as the ligand in the present study.…”

Section: Resultsmentioning

confidence: 99%

“…In addition, we have shown that glial cells do not expresses endogenous T2R1 (15). The measurement of intracellular calcium produced was carried out as follows.…”

Section: Methodsmentioning

confidence: 99%

“…Molecular Biology and Cell Culture-Amino acid substitutions were introduced into the synthetic T2R1-rho1D4 gene carried by the expression vector pcDNA3.1 (Invitrogen) as described previously (15,16) or synthesized commercially (GenScript USA Inc.). DNA sequences of all of the mutated genes were verified by automated DNA sequencing (MICB DNA Sequencing Facility, Winnipeg).…”

Section: Methodsmentioning

confidence: 99%

“…DNA sequences of all of the mutated genes were verified by automated DNA sequencing (MICB DNA Sequencing Facility, Winnipeg). The wild type and mutant T2R1 genes in pcDNA3.1 were transiently expressed in C6-glioma cells using Lipofectamine 2000 (Invitrogen) according to previously published methods (15).…”

Section: Methodsmentioning

confidence: 99%

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Structural Basis of Activation of Bitter Taste Receptor T2R1 and Comparison with Class A G-protein-coupled Receptors (GPCRs)

Singh

Pydi

Upadhyaya

et al. 2011

Journal of Biological Chemistry

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The human bitter taste receptors (T2Rs) are non-Class A members of the G-protein-coupled receptor (GPCR) superfamily, with very limited structural information. Amino acid sequence analysis reveals that most of the important motifs present in the transmembrane helices (TM1-TM7) of the well studied Class A GPCRs are absent in T2Rs, raising fundamental questions regarding the mechanisms of activation and how T2Rs recognize bitter ligands with diverse chemical structures. In this study, the bitter receptor T2R1 was used to systematically investigate the role of 15 transmembrane amino acids in T2Rs, including 13 highly conserved residues, by amino acid replacements guided by molecular modeling. form a putative LXXSL motif which performs predominantly a structural role by stabilizing the helical conformation of TM5 at the cytoplasmic end. This study provides for the first time mechanistic insights into the roles of the conserved transmembrane residues in T2Rs and allows comparison of the activation mechanisms of T2Rs with the Class A GPCRs.The mammalian taste sensation provides valuable information about the nature and quality of food. Taste transduction predominantly involves the interaction of molecules (i.e. tastants) with taste receptor-expressing cells that reside in the taste buds located on the papillae of the tongue. Taste buds relay information to the brain on the nutrient content of food.

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Section: Methodsmentioning

confidence: 95%

Section: Resultsmentioning

confidence: 99%

“…In addition, we have shown that glial cells do not expresses endogenous T2R1 (15). The measurement of intracellular calcium produced was carried out as follows.…”

Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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