受容体 / receptor-tas2r31

TAS2R31

Human bitter taste receptor (formerly TAS2R44) in the five-member TAS2R30-46 subfamily encoded in a high-linkage-disequilibrium cluster on chromosome 12; responds to saccharin, acesulfame K and quinine

感覚（1）

グレープフルーツジュースの嗜好と関連: TAS2R31支持あり

範囲: 246 adults (mostly European ancestry); remembered liking for unsweetened grapefruit juice on a bipolar hedonic scale

注記: Quinine bitterness showed the parallel association (21.5 versus 30.8 gLMS). Authors argue earlier TAS2R19 associations may reflect linkage disequilibrium with TAS2R31, whose validated agonist is quinine, not naringin or limonin.

Val240 homozygotes rated quinine less bitter (21.5 plus-minus 1.9 versus 30.8 plus-minus 3.1 for Ile240 homozygotes) and reported greater remembered liking for grapefruit juice (9.3 plus-minus 4.5 versus -16.53 plus-minus 7.1); the three TAS2R19/TAS2R31 SNPs formed a haploblock (D' 0.96 and 0.87) so earlier TAS2R19 associations may be LD artifacts.

限界: Remembered rather than tasted grapefruit liking; tag SNPs rather than suspected causal Arg35Trp; LD with unmeasured variants possible (authors' own limitations).

出典: Quinine Bitterness and Grapefruit Liking Associate with Allelic Variants in TAS2R31（Hayes JE; Feeney EL; Nolden AA; McGeary JE, 2015）・全文確認

文脈: The existence of high LD spanning functionally distinct TAS2R loci predicts that bitter taste responses to many compounds will be strongly correlated even when they are mediated by different genes, and haplotype analysis showed most single-marker associations in the TAS2R30-46 cluster to be spurious products of LD with TAS2R31.

限界: Provides the mechanistic backdrop for Hayes 2015's argument that earlier TAS2R19 grapefruit/quinine associations may be LD artifacts of TAS2R31; it does not itself test grapefruit liking.

出典: Genomic, genetic and functional dissection of bitter taste responses to artificial sweeteners（Roudnitzky N; Bufe B; Thalmann S; Kuhn C; Gunn HC; Xing C; Crider BP; Behrens M; Meyerhof W; Wooding SP, 2011）・抄録確認

データを表示

ingredient-grapefruit-juice —has_liking_associated_with→ receptor-tas2r31

claim: clm-grapefruit-liking-tas2r31 / type: sensory / 更新: 2026-08-30

機構・受容体（2）

TAS2R31はサッカリンの苦味の個人差を媒介する支持あり

範囲: Whole-gene sequencing of TAS2R30-46 in 60 Caucasian subjects, taste responses to both sweeteners, and in vitro assays of receptor alleles; 30 markers initially associated at P < 0.001

注記: クラスタ内の高 LD (D' と r2 > 0.95) のため単一 SNP 関連の大半が見かけ上という方法論的教訓つき。Hayes 2015 (src-hayes-2015-tas2r31-grapefruit) の TAS2R19 関連 = LD アーティファクト説と整合。

Thirty markers including non-synonymous variants in all five TAS2R30-46 genes were associated (P < 0.001) with responses to saccharin and acesulfame K, but linkage disequilibrium in the region was high (D prime and r2 > 0.95) and haplotype analyses revealed that most associations were spurious, arising from LD with variants in TAS2R31; in vitro assays confirmed the functional importance of four TAS2R31 mutations with independent effects on receptor response.

限界: Abstract-level: the identities of the four TAS2R31 mutations and effect sizes are in the full text, which was not retrieved. Single-ancestry sample.

データを表示

receptor-tas2r31 —mediates_variation_in_bitterness_of→ compound-saccharin

claim: clm-tas2r31-saccharin-bitterness / type: mechanism / 更新: 2026-08-30

GIV3727はTAS2R31を拮抗阻害する支持あり

範囲: Calcium imaging in HEK293 cells stably or transiently expressing single hTAS2Rs with the chimeric G-protein G16gust44; antagonist tested at 25 uM in the panel screen

注記: Identified from a 17,854-compound screen that yielded 139 candidate antagonists. Authors conclude it is likely an orthosteric, insurmountable antagonist: 25 uM GIV3727 shifted agonist EC50 3- to 10-fold and reduced maximal signal amplitude by 35-70%.

High-throughput calcium-imaging screening of 17,854 compounds against hTAS2R31 yielded 139 candidate antagonists, of which GIV3727 gave IC50 6.4 +/- 2.4 uM against acesulfame K and 7.9 +/- 6.1 uM against saccharin (n = 3). Inhibition was reversible on washout. Tested at 25 uM against 18 of the 25 hTAS2Rs with known agonists, GIV3727 significantly inhibited six receptors (hTAS2R4, 7, 40, 43, 31, 20) and not the remainder. Mutagenesis showed a basic residue at position 7.39 (Lys265) is a key contact point in the hTAS2R46 backbone.

限界: For four receptors (hTAS2R3/5/7/13) an accurate EC90 agonist concentration could not be established, so the maximal non-artifactual agonist concentration was used instead and hTAS2R7 inhibition at a true EC90 is therefore uncertain. Lysine at 7.39 is not sufficient for sensitivity, since hTAS2R50 also carries it but is insensitive.

出典: Modulation of bitter taste perception by a small molecule hTAS2R antagonist（Slack JP; Brockhoff A; Batram C; Menzel S; Sonnabend C; Born S; Galindo MM; Kohl S; Thalmann S; Ostopovici-Halip L; Simons CT; Ungureanu I; Duineveld K; Bologa CG; Behrens M; Furrer S; Oprea TI; Meyerhof W, 2010）・全文確認

データを表示

compound-giv3727 —antagonizes→ receptor-tas2r31

claim: clm-giv3727-tas2r-antagonism / type: mechanism / 更新: 2026-08-30

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