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| Poster #187 Molecular basis for activation of the human bitter taste receptor TAS2R14 by Ritonavir |
| Jiao Wen, Xinyi Ma, Xinyi Zhou, Yongcheng Lu, Yukyoung Kim, Young Seo Lee, Alice Lee, Shurui Chen, Keman Xu, Meng Cui Northeastern University, Boston, MA, United States |
Ritonavir is a protease inhibitor used in combination with other antiretroviral medications to treat HIV, particularly in children. It increases the bioavailability of these medications by inhibiting the cytochrome P450-3A4 enzyme and is also being studied for cancer treatment due to its mechanism of action. However, its intense bitterness, especially in liquid formulations, may be intolerable for some children. This bitterness is attributed to its activation of bitter taste receptors, including TAS2R14, as demonstrated in our previous study. In this study, we utilized molecular modeling, site-directed mutagenesis, and cell-based calcium mobilization assays to characterize the key residues involved in TAS2R14 activation by ritonavir. These results are crucial for the design and screening of bitter taste inhibitors. |