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This Article Full Text Full Text (PDF) All Versions of this Article: 289/2/C483    most recent 00547.2004v1 Alert me when this article is cited Alert me if a correction is posted Citation Map Services Email this article to a friend Similar articles in this journal Similar articles in ISI Web of Science Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Citing Articles Citing Articles via HighWire Citing Articles via ISI Web of Science (4) Citing Articles via Google Scholar Google Scholar Articles by Zubare-Samuelov, M. Articles by Naim, M. Search for Related Content PubMed PubMed Citation Articles by Zubare-Samuelov, M. Articles by Naim, M.

RECEPTORS AND SIGNAL TRANSDUCTION

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

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

Submitted 10 November 2004 ; accepted in final form 21 March 2005

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 nonsugar sweeteners), may share the same or similar T1Rs, some nonsugar sweeteners and many bitter tastants are amphipathic and produce a significant delay in taste termination (lingering aftertaste). We report that such tastants may permeate rat taste bud cells rapidly in vivo and inhibit known signal termination-related kinases in vitro, such as GPCR kinase (GRK)2, 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 intracellularly with the receptors' downstream shutoff components to inhibit signal termination.

amphipathic tastants; tastant permeation; desensitization; lingering aftertaste

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