Role of the second transmembrane domain of rat adenosine A(1) receptor in ligand-receptor interaction

doi:10.1016/j.bcp.2005.12.013

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	Role of the second transmembrane domain of rat adenosine A(1) receptor in ligand-receptor interaction
	Xie, KQ; Cao, Y; Zhu, XZ
刊名	BIOCHEMICAL PHARMACOLOGY
	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
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000235723100017
内容类型	期刊论文
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.