Identification of Novel Compounds for Human Bitter Taste Receptors
文献类型：期刊论文
| 作者 | Ji, Mingfei1; Su, Xubo2,3; Su, Xiaohong4; Chen, Yingyi2,3,5; Huang, Wenkang2,3; Zhang, Jian2,3; Gao, Zhaobin6; Li, Chuangang1; Lu, Xuefeng5 |
| 刊名 | CHEMICAL BIOLOGY & DRUG DESIGN
 |
| 出版日期 | 2014-07 |
| 卷号 | 84期号:1页码:63-74 |
| 关键词 | bitter compounds calcium imaging molecular descriptors TAS2Rs |
| ISSN号 | 1747-0277 |
| DOI | 10.1111/cbdd.12293 |
| 文献子类 | Article |
| 英文摘要 | The finely tuned bitter taste sensing in humans is orchestrated by a group of 25 bitter taste receptors (TAS2Rs), which belong to the G-protein-coupled receptor superfamily. TAS2Rs are expressed in the specialized taste bud cells of the gustatory system and perceive a plethora of bitter substances with versatile structures. To date, more than one hundred bitter ligands have been matched with their cognate receptors, but the understanding of the molecular mechanisms of TAS2Rs remains limited. Additionally, the extraoral expression of TAS2R genes was found in the gastrointestinal tract and respiratory system, which suggests other important physiological functions for TAS2Rs. To gain insight into the physiological functions of TAS2Rs, we established a heterologous expression system and characterized the response of 24 TAS2Rs against a library of potential bitter compounds. Among these bitter compounds of interest, 18 bitter compounds activated 16 TAS2Rs, representing 42 tastant-receptor pairs. We then calculated 14 descriptor properties for the 18 positive compounds. By comparison with 102 previously annotated bitter compounds in the database, we discovered common descriptor properties that may contribute to the discovery of additional bitter ligands and further expand the known molecular receptive ranges of human TAS2Rs. |
| WOS关键词 | MAMMALIAN ODORANT RECEPTORS ; DRUG-LIKE COMPOUNDS ; FUNCTIONAL EXPRESSION ; GENE FAMILY ; CELLS ; PERCEPTION ; ACTIVATION ; DISCOVERY ; DATABASES ; LIBRARIES |
| 资助项目 | National Natural Science Foundation of China[21102090] ; National Natural Science Foundation of China[81302698] ; Shanghai Rising-Star Program[13QA1402300] ; China Postdoctoral Science Foundation[2012M520046] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000337665900006 |
| 出版者 | WILEY |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277014]  |
| 专题 | 新药研究国家重点实验室 中科院受体结构与功能重点实验室 |
| 通讯作者 | Lu, Xuefeng |
| 作者单位 | 1.Dalian Med Univ, Dept Urol, Affiliated Hosp 2, Dalian 116023, Peoples R China; 2.Shanghai Jiao Tong Univ, Dept Pathophysiol, Sch Med, Chinese Minist Educ, Shanghai 200025, Peoples R China; 3.Shanghai Jiao Tong Univ, Key Lab Cell Differentiat & Apoptosis, Sch Med, Chinese Minist Educ, Shanghai 200025, Peoples R China; 4.Dalian Med Univ, Dept Pharmacol, Dalian 116023, Peoples R China; 5.Shanghai Jiao Tong Univ, Inst Obstet & Gynecol, Renji Hosp, Dept Obstet & Gynecol,Sch Med, Shanghai 200001, Peoples R China; 6.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ji, Mingfei,Su, Xubo,Su, Xiaohong,et al. Identification of Novel Compounds for Human Bitter Taste Receptors[J]. CHEMICAL BIOLOGY & DRUG DESIGN,2014,84(1):63-74. |
| APA | Ji, Mingfei.,Su, Xubo.,Su, Xiaohong.,Chen, Yingyi.,Huang, Wenkang.,...&Lu, Xuefeng.(2014).Identification of Novel Compounds for Human Bitter Taste Receptors.CHEMICAL BIOLOGY & DRUG DESIGN,84(1),63-74. |
| MLA | Ji, Mingfei,et al."Identification of Novel Compounds for Human Bitter Taste Receptors".CHEMICAL BIOLOGY & DRUG DESIGN 84.1(2014):63-74. |
入库方式： OAI收割
来源：上海药物研究所
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