TAS2R4

更新于：2025-05-07

基本信息

别名

T2R4、TAS2R4、taste 2 receptor member 4

+ [2]

简介

Gustducin-coupled receptor for denatonium and N(6)-propyl-2-thiouracil implicated in the perception of bitter compounds in the oral cavity and the gastrointestinal tract. Signals through PLCB2 and the calcium-regulated cation channel TRPM5. In airway epithelial cells, binding of denatonium increases the intracellular calcium ion concentration and stimulates ciliary beat frequency.

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100 项与 TAS2R4 相关的临床结果

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100 项与 TAS2R4 相关的转化医学

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0 项与 TAS2R4 相关的专利（医药）

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项与 TAS2R4 相关的文献（医药）

2025-08-01·Food Chemistry

Bitter peptides formed during in-vitro gastric digestion induce mechanisms of gastric acid secretion and release satiating serotonin via bitter taste receptors TAS2R4 and TAS2R43 in human parietal cells in culture

Article

作者: Richter, Phil ; Gradl, Katrin ; Somoza, Veronika

A key barrier in transitioning to plant-based, more satiating diets, is the bitter taste of plant proteins. We hypothesize that both, a more bitter tasting (MBT) and a less bitter tasting (LBT) pea protein hydrolysate (PPH) can be digested in the stomach into bitter tasting peptides that stimulate proton secretion (PS) and serotonin release, as two of the key gastric satiety signals, via the functional involvement of bitter taste receptors (TAS2Rs). Using a sensory-guided LC-MS approach, we identified six bitter peptides that were released from LBT-PPH and MBT-PPH during gastric digestion in vitro. TAS2R4 and TAS2R43 involvement in PS and serotonin release was confirmed via CRISPR-Cas9 knockout experiments. Our hypothesis was proven with all six peptides equally stimulating PS in immortalized human gastric HGT-1 cells, and LBT-PPH-derived peptides eliciting a higher serotonin release in HGT-1 cells than MBT-PPH peptides, indicating a satiating potential of less bitter tasting protein hydrolysates.

2025-07-01·Biochemical Pharmacology

Activation of bitter taste receptor TAS2R4 alleviates diabetic nephropathy in mice

Article

作者: Gu, Pan-Pan ; Gu, Yan-Ping ; Duan, Jing-Yu ; Zhang, Chun-Ping ; Tian, Sai ; Wang, Jiang-Meng ; An, Xiao-Fei ; Liu, Yao-Wu

Activation of bitter taste receptor member 4 (TAS2R4) signaling alleviates podocyte injury caused by chronic high glucose; however, whether TAS2R4 activation in podocytes can improve diabetic nephropathy (DN) is to be verified. This study aims to confirm the beneficial effects of quinine, a dual human and rodent TAS2R4 agonist, and matrine with a potent anti-inflammatory activity and binding with TAS2R4 via online prediction and receptor docking on DN in vivo and in vitro. In this study, we found that quinine and matrine markedly ameliorated renal dysfunction, as evidenced by decreases in creatinine and urea nitrogen levels in plasma as well as protein excretion in urine, increased podocyte slit diaphragm and adaptor proteins including Nephrin, Podocin, and Zonula occluden 1, and suppressed activations of NF-κB and the NLRP3 inflammasome in the kidney of DN mice. Meanwhile, quinine and matrine activated TAS2R4 signaling, as revealed by increased protein expressions of TAS2R4 and its key downstream molecule phospholipase C β2. Furthermore, quinine and matrine attenuated podocyte injury, activated TAS2R4 signaling, and suppressed the above inflammatory pathways in the high glucose-cultured MPC cells, a mouse podocyte cell line, while the effects of both quinine and matrine were eliminated when TAS2R4 signaling was inhibited by using either a TAS2R4 blocker abscisic acid or a Gβγ inhibitor Gallein. In summary, quinine and matrine alleviated DN in mice through activation of TAS2R4 signaling in podocytes, which was achieved by inhibiting the activation of NF-κB mediated NLRP3 inflammasome in the kidney. Moreover, TAS2R4 could be a drug target.

2025-01-01·Journal of Ethnopharmacology

Scutellaria baicalensis ameliorates allergic airway inflammation through agonism and transcriptional regulation of TAS2Rs

Article

作者: Zhang, Yanling ; Liu, Yanxia ; Liu, Kaiyang ; Qiao, Liansheng ; Xu, Zhenzhen ; Wang, Shifeng ; Ren, Yue

ETHNOPHARMACOLOGICAL RELEVANCEScutellaria baicalensis Georgi (SCB, Huangqin) is a traditional medicinal plant used to treat fever and respiratory diseases. SCB has a good therapeutic effect on asthma and anti-inflammation in traditional clinic use. However, the molecular mechanism and targets of SCB in treating asthma are still unclear.AIM OF THE STUDYCombining transcriptomic analysis and in vitro experimental validation, this study aimed to reveal the molecular mechanism and targets of SCB in treating asthma.MATERIALS AND METHODSThe anti-asthmatic effects of SCB and its active components, scutellarin and oroxylin A, were evaluated in ovalbumin (OVA)-induced rats by analysis of pulmonary function and pathology. The signaling pathways in rat pulmonary tissue were analyzed using transcriptomics and protein interaction network analysis. Calcium mobilization assay and molecular docking were utilized to discover the active compounds from SCB with agonism activity of type 2 taste receptors (TAS2Rs). The anti-asthmatic effect and transcriptional regulation of TAS2Rs regulated by SCB and its active components were analyzed in vitro.RESULTSExtracts of SCB (ESB), scutellarin, and oroxylin A ameliorated airway function and inflammation in OVA-induced rats. The anti-asthma mechanism of ESB, scutellarin and oroxylin A was highly related to immune and taste transduction pathways based on transcriptomic analysis, especially the TAS2Rs signaling pathway. ESB was the direct agonist of TAS2R4 and TAS2R14 with EC₅₀ of 209.1 and 217.2 μg/mL based on calcium mobilization assay, respectively. Baicalein was the main active component for TAS2R4 agonism activity, and scutellarin and oroxylin A had weak agonism activity of TAS2R4 and TAS2R14 through calcium mobilization assay and molecular docking. However, scutellarin and oroxylin A significantly upregulated the gene expression of Tas2r108 (the mouse ortholog of the TAS2R4) in lung tissue. ESB, scutellarin, and oroxylin A inhibited LPS-induced lactate dehydrogenase release and gene expression of TNF through transcriptional regulation of TAS2R4 and TAS2R14 on bronchial epithelial cells. ESB and oroxylin A ameliorated IgE-induced β-hexosaminidase release and gene expression of Il4 and Tnf and upregulated gene expression of Tas2r108.CONCLUSIONThese results provided new insight into the anti-asthmatic mechanism of SCB and active components, scutellarin and oroxylin A, through agonism and transcriptional regulation of TAS2Rs to ameliorate allergic airway inflammation.

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