Article
Amino acid derivatives as bitter taste receptor (T2R) blockers.
The Journal of biological chemistry - 5 Sept 2014
Pydi Sai P, Sobotkiewicz Tyler, Billakanti Rohini, Bhullar Rajinder P, Loewen Michele C, Chelikani Prashen
Abstract excerpt
In humans, the 25 bitter taste receptors (T2Rs) are activated by hundreds of structurally diverse bitter compounds. However, only five antagonists or bitter blockers are known. In this study, using molecular modeling guided site-directed mutagenesis, we elucidated the ligand-binding pocket of T2R4. We found seven amino acids located in the extracellular side of transmembrane 3 (TM3), TM4, extracellular loop 2...
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