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Am J Physiol Cell Physiol (April 13, 2005). doi:10.1152/ajpcell.00547.2004
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Submitted on November 10, 2004
Accepted on April 6, 2005

Inhibition of signal-termination-related kinases by membrane-permeant bitter and sweet tastants: potential role in taste-signal termination

Meirav Zubare-Samuelov1, Merav E Shaul1, Irena Peri1, Alexander Aliluiko1, Oren Tirosh1, and Michael Naim1*

1 Institute of Biochemistry, Food science and Nutrition, The Hebrew University of Jerusalem, Rehovot, Israel

* To whom correspondence should be addressed. E-mail: Naim{at}agri.huji.ac.il.

Sweet and bitter taste sensations are believed to be initiated by the tastant-stimulated T1R and T2R G-protein-coupled receptor (GPCR) subfamilies, respectively, which occur in taste cells. Although such tastants, with their significantly diverse chemical structures (e.g., sugar and non-sugar sweeteners), may share the same or similar T1Rs, some non-sugar sweeteners and many bitter tastants are amphipathic and produce a significant delay in taste termination (lingering aftertaste). We report that such tastants may rapidly permeate rat taste-bud cells in vivo and inhibit known signal-termination-related kinases in vitro, such as GRK2, GRK5 and PKA. GRK5, and perhaps GRK2 and GRK6 are present in taste cells. A new hypothesis is proposed in which membrane-permeant tastants not only interact with taste GPCRs, but also interact intracellulary with the receptor's downstream shut-off components to inhibit signal termination.




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