Role of the second transmembrane domain of rat adenosine A(1) receptor in ligand-receptor interaction
文献类型：期刊论文
| 作者 | Xie, KQ; Cao, Y; Zhu, XZ |
| 刊名 | BIOCHEMICAL PHARMACOLOGY
 |
| 出版日期 | 2006-03-14 |
| 卷号 | 71期号:6页码:865-871 |
| 关键词 | adenosine A(1) receptor transmembrane domain hydrophobic hydrophilic mutagenesis ribose group |
| ISSN号 | 0006-2952 |
| DOI | 10.1016/j.bcp.2005.12.013 |
| 文献子类 | Article |
| 英文摘要 | Initial mutagenesis studies exploring the ligand recognition model of A(1) adenosine receptor (A(1)R) mainly focused on the residues in the 5th-7th transmembrane domains (TMs5-7). Little is known about the role of residues in TM2. To explore the importance of reserved hydrophobic region in TM2 of AIR, we mutated the hydrophobic residues at positions 65 and 69 to hydrophilic residues (L65T, Leu-65 to Thr-65; 169T, Ile-69 to Thr-69; 169S, Ile-69 to Ser-69) to change the hydrophobicity at the outer end of TM2. Binding assays showed that the affinities of mutant receptors were significantly decreased for ribose group-containing agonists (2-chloro-N-6-cyclopentyladenosine (CCPA) and 5'-N-ethyl-carboxamidoadenosine (NECA)) but not for antagonists, N-6-cyclopentyl-9-methyladenine (N-0840), an adenine derivative lacking ribose group, and 8-cyclopentyl-1, 3-dipropylxanthine (DPCPX), a xanthine derivative. This observation suggests that the hydrophobic region at the outer end of TM2 may mediate the recognition of the ribose group of CCPA and NECA. (c) 2005 Elsevier Inc. All rights reserved. |
| WOS关键词 | SITE-DIRECTED MUTAGENESIS ; SPECIES-DIFFERENCES ; BINDING-SITE ; A(1) ; INHIBITION ; ADENOSINE-A1-RECEPTORS ; DESENSITIZATION |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000235723100017 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273646]  |
| 专题 | 药理学第二研究室 |
| 通讯作者 | Zhu, XZ |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, Dept Pharmacol, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Xie, KQ,Cao, Y,Zhu, XZ. Role of the second transmembrane domain of rat adenosine A(1) receptor in ligand-receptor interaction[J]. BIOCHEMICAL PHARMACOLOGY,2006,71(6):865-871. |
| APA | Xie, KQ,Cao, Y,&Zhu, XZ.(2006).Role of the second transmembrane domain of rat adenosine A(1) receptor in ligand-receptor interaction.BIOCHEMICAL PHARMACOLOGY,71(6),865-871. |
| MLA | Xie, KQ,et al."Role of the second transmembrane domain of rat adenosine A(1) receptor in ligand-receptor interaction".BIOCHEMICAL PHARMACOLOGY 71.6(2006):865-871. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。