BitterDB

hTAS2R46 - Taste receptor type 2 member 46 help

hTAS2R46 is a bitter receptor broadly tuned to sesquiterpene lactones, related clerodane diterpenoids,labdane diterpenes and more.

Properties help

  • Human
  • chr12:11,213,964-11,214,893 UCSC
  • 28
  • 35,523 (Da)


  • MITFLPIIFSILIVVTFVIGNFANGFIALVNSIEWFKRQK ISFADQILTALAVSRVGLLWVLVLNWYATELNPAFNSIEV RITAYNVWAVINHFSNWLATSLSIFYLLKIANFSNLIFLH LKRRVKSVVLVILLGPLLFLVCHLFVINMNQIIWTKEYEG NMTWKIKLRSAMYLSNTTVTILANLVPFTLTLISFLLLIC SLCKHLKKMQLHGKGSQDPSMKVHIKALQTVTSFLLLCAI YFLSIIMSVWSFESLENKPVFMFCEAIAFSYPSTHPFILI WGNKKLKQTFLSVLWHVRYWVKGEKPSSS

Known Ligands help

Please scroll down to see the rest of the ligands.

Protein Diagram help

Receptor snake diagram

When using this 2D protein diagram,please cite us:
Ayana Wiener; Marina Shudler; Anat Levit; Masha Y. Niv. BitterDB: a database of bitter compounds. Nucleic Acids Res 2012, 40(Database issue):D413-419.
Click here to view the paper: BitterDB paper

Known Mutations Table help

Residue Location Ballesteros-Weinstein: Mutation Experimental data Inferred role
E70 EL1 E70K Strong reduction in two agonist responsiveness agonist specificity
E70Q Minor reduction in responsiveness to agonist
E70A Minor reduction in responsiveness to agonist
E70V Exhibited agonist-selective reductions of responses
L71 EL1 L71F Showed decreased receptor activation by all agonists
N76 EL1 N76I No obvious differences compared with hTAS2R46 WT
I82 EL1 I82T exhibited agonist-selective reductions of responses
I91 TM3 3.35 I91T no obvious differences compared with hTAS2R46 WT
N92 TM3 3.36 N92G showed decreased receptor activation by all agonists
N150 EL2 N150K showed decreased receptor activation by all agonists
W154 EL2 W154R no obvious differences compared with hTAS2R46WT
N176 EL2 N176D exhibited agonist-selective reductions of responses
Y241 TM6 6.5 Y241F significant reduction in agonist (strychnine) responsiveness agonist-induced activation?
E253 EL3 E253G exhibited agonist-selective reductions of responses
E265 TM7 7.39 E265K Sufficient to confer sensitivity to the antagonist that was indistinguishable from the double mutant (with7.42) [1]. Strong reduction or loss-of-responsiveness toward the original agonist [2] basic residues in these positions important for antagonist binding agonist specificity (with 7.42), agonist specificity (with 7.42)
E265D No antagonist sensitivity observed. compared with hTAS2R46 WT [1] Reduced the EC50 value for strychnine activation [2]
E265Q No antagonist sensitivity observed. compared with hTAS2R46 WT [1] Reduced receptor responsiveness [2]
E265K/A268R Double mutant Increase in antagonist activity [1] Switching of receptor ligand specificities [2]
A268 TM7 7.42 A268R No antagonist sensitivity observed. like hTAS2R46 WT. [1] Strong reduction or loss-of-responsiveness toward the original agonists [2] basic residues in these positions important for antagonist binding agonist specificity (with 7.39), agonist specificity (with 7.39)
A268G No antagonist sensitivity observed like hTAS2R46 WT [1]

[1] Slack, J. P., et al. (2010) Modulation of bitter taste perception by a small molecule hTAS2R antagonist, Curr Biol 20, 1104-1109.

[2] Brockhoff, A., et al. (2010) Structural requirements of bitter taste receptor activation, Proc Natl Acad Sci U S A 107 , 11110-11115.

Links:

P59540
TAS2R46