Bitter Taste Receptor Activation by Flavonoids and Isoflavonoids: Modeled Structural Requirements for Activation of hTAS2R14 and hTAS2R39

2013 ◽  
Vol 61 (44) ◽  
pp. 10454-10466 ◽  
Author(s):  
Wibke S. U. Roland ◽  
Leo van Buren ◽  
Harry Gruppen ◽  
Marianne Driesse ◽  
Robin J. Gouka ◽  
...  
Keyword(s):  
Bitter Taste ◽  
Taste Receptor ◽  
Receptor Activation ◽  
Bitter Taste Receptor ◽  
Structural Requirements

scholarly journals Structural requirements of bitter taste receptor activation

2010 ◽  
Vol 107 (24) ◽  
pp. 11110-11115 ◽  
Author(s):  
A. Brockhoff ◽  
M. Behrens ◽  
M. Y. Niv ◽  
W. Meyerhof
Keyword(s):  
Bitter Taste ◽  
Taste Receptor ◽  
Receptor Activation ◽  
Bitter Taste Receptor ◽  
Structural Requirements

scholarly journals Dextromethorphan Mediated Bitter Taste Receptor Activation in the Pulmonary Circuit Causes Vasoconstriction

PLoS ONE ◽  
2014 ◽  
Vol 9 (10) ◽  
pp. e110373 ◽  
Author(s):  
Jasbir D. Upadhyaya ◽  
Nisha Singh ◽  
Anurag S. Sikarwar ◽  
Raja Chakraborty ◽  
Sai P. Pydi ◽  
...  
Keyword(s):  
Bitter Taste ◽  
Taste Receptor ◽  
Receptor Activation ◽  
Bitter Taste Receptor

scholarly journals Structural basis for bitter taste receptor activation and its potential role in targeting diabetes

2015 ◽  
Vol 5 (3) ◽  
pp. 117 ◽  
Author(s):  
Ravinder Abrol ◽  
Jun Tan ◽  
Hongxiang Hui ◽  
William A. Goddard III ◽  
Stephen J. Pandol
Keyword(s):  
Structure Prediction ◽  
Potential Role ◽  
Bitter Taste ◽  
Taste Receptor ◽  
Receptor Activation ◽  
Structural Basis ◽  
Gut Peptides ◽  
Bitter Taste Receptor ◽  
L Cells

Background: Taste receptors are G protein-coupled receptors that, besides being present in the taste buds, have also been shown to be present in the gastrointestinal (GI) system, respiratory system, and brain, though their function at these locations is not well understood.Objective: To understand the nutrient mediated release of gut peptides like GLP-1 from enteroendocrine L-cells of the GI system, we focused on a bitter taste receptor TAS2R38 (based on animal models) to investigate the structural basis of its potential role in the release of gut peptides. Methods: The atomic-level structure of bitter taste receptor TAS2R38 was predicted using GEnSeMBLE, a first-principle based GPCR structure prediction method. These structures were obtained for the dominant taster haplotype (PAV) as well as for the nontaster haplotype (AVI) of the receptor. The known ligands phenylthiocarbamide (PTC) and 6-n-propylthiouracil (PTU) were docked to these structures to provide a structural basis for the taster and nontaster haplotypes.Results: Docking of known ligands PTU and PTC to taster and nontaster haplotypes of the bitter taste receptor showed a backbone hydrogen bond to residue 262 in taster but not in nontaster haplotype, suggesting a potential mode of action of these molecules in the activation of the bitter taste receptor. Conclusion: These results, combined with the ability of PTC to release gut peptides from in vitro models of the enteroendocrine L-cells, suggest a potential structural basis for TAS2R38 activation that can lead to the release of those peptides. This release has a therapeutic benefit for type 2 diabetes and implies a role for bitter tasting (but safe) natural compounds targeting TAS2R38 as potential drug candidates for curing type 2 diabetes.Key words: TAS2R38, GLP-1 release, PYY release, CCK release, enteroendocrine L cell, GPCR, protein structure prediction, GEnSeMBLE

scholarly journals Intestinal bitter taste receptor activation alters hormone secretion and imparts metabolic benefits

2018 ◽  
Vol 16 ◽  
pp. 76-87 ◽  
Author(s):  
Bernard P. Kok ◽  
Andrea Galmozzi ◽  
Nicole K. Littlejohn ◽  
Verena Albert ◽  
Cristina Godio ◽  
...  
Keyword(s):  
Bitter Taste ◽  
Hormone Secretion ◽  
Taste Receptor ◽  
Receptor Activation ◽  
Bitter Taste Receptor

scholarly journals The third intracellular loop plays a critical role in bitter taste receptor activation

2014 ◽  
Vol 1838 (1) ◽  
pp. 231-236 ◽  
Author(s):  
Sai Prasad Pydi ◽  
Nisha Singh ◽  
Jasbir Upadhyaya ◽  
Rajinder Pal Bhullar ◽  
Prashen Chelikani
Keyword(s):  
Bitter Taste ◽  
Critical Role ◽  
Taste Receptor ◽  
Receptor Activation ◽  
Bitter Taste Receptor ◽  
Intracellular Loop ◽  
The Third ◽  
Third Intracellular Loop

scholarly journals Effects Of Dextromethorphan Mediated Bitter Taste Receptor Activation In Pulmonary Artery Smooth Muscle Cells

2013 ◽  
Vol 27 (S1) ◽  
Author(s):  
Jasbir Deol Upadhyaya ◽  
Nisha Singh ◽  
Anurag Singh Sikarwar ◽  
Rajinder Pal Bhullar ◽  
Shyamala Dakshinamurti ◽  
...  
Keyword(s):  
Smooth Muscle ◽  
Pulmonary Artery ◽  
Smooth Muscle Cells ◽  
Bitter Taste ◽  
Taste Receptor ◽  
Muscle Cells ◽  
Receptor Activation ◽  
Bitter Taste Receptor ◽  
Pulmonary Artery Smooth Muscle
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