Internalization and recycling of human mu opioid receptors expressed in Sf9 insect cells
文献类型:期刊论文
作者 | Chen, LW; Gao, C; Chen, J![]() ![]() |
刊名 | LIFE SCIENCES
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出版日期 | 2003-05-23 |
卷号 | 73期号:1页码:115-128 |
关键词 | G protein coupled receptors mu-opioid receptor internalization recycling Sf9 insect cells |
ISSN号 | 0024-3205 |
DOI | 10.1016/S0024-3205(03)00250-9 |
文献子类 | Article |
英文摘要 | Internalization and recycling of G protein-coupled receptors (GPCRs), such as the mu-opioid receptor, largely depend on agonist stimulation. Agonist-promoted internalization of some GPCRs has been shown to mediate receptor desensitization, resensitization, and down-regulation. In this study, we investigated whether different mu opioid agonists displayed different effects in receptor internalization and recycling, the potential mechanisms involved in ohmefentanyl-induced internalization process. In transfected SO insect cells expressing 6His-tagged wild type mu opioid receptor, exposure to 100 nM ohmefentanyl caused a maximum internalization of the receptor at 30 min and receptors seemed to reappear at the cell membrane after 60 min as determined by radioligand binding assay. Ohmefentanyl-induced human mu opioid receptor internalization was concentration-dependent, with about 40% of the receptors internalized following a 30-min exposure to 1 muM ohmefentanyl. 10 muM morphine and 1 muM DAMGO could also induce about 40% internalization. The antagonist naloxone and pretreatment with pertussis toxin both blocked ohmefentanyl-induced internalization without affecting internalization themselves. Incubation with sucrose 0.45 M significantly inhibited ohmefentanyl-induced internalization of the mu receptor. The removal of agonists ohmefentanyl and morphine resulted in the receptors gradually returning to the cell surface over a 60 min period, while the removal of agonist DAMGO only partly resulted in the receptor recycling. The results of this study suggest that ohmefentanyl-induced internalization of human mu opioid receptor in Sf9 insect cells occurs via Gi/o protein-dependent process that likely involves clathrin-coated pits. In addition, the recycling process displays the differential modes of action of different agonists. (C) 2003 Published by Elsevier Science Inc. |
WOS关键词 | AGONIST-MEDIATED INTERNALIZATION ; MORPHINE-INDUCED ANALGESIA ; OPIATE RECEPTOR ; DESENSITIZATION ; MICE ; TRAFFICKING ; ENDOCYTOSIS ; AFFINITY ; KNOCKOUT ; DOMAIN |
WOS研究方向 | Research & Experimental Medicine ; Pharmacology & Pharmacy |
语种 | 英语 |
WOS记录号 | WOS:000182775600011 |
出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
源URL | [http://119.78.100.183/handle/2S10ELR8/274234] ![]() |
专题 | 院士及顾问专家 |
通讯作者 | Chi, ZQ |
作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Shanghai 200031, Peoples R China |
推荐引用方式 GB/T 7714 | Chen, LW,Gao, C,Chen, J,et al. Internalization and recycling of human mu opioid receptors expressed in Sf9 insect cells[J]. LIFE SCIENCES,2003,73(1):115-128. |
APA | Chen, LW,Gao, C,Chen, J,Xu, XJ,Zhou, DH,&Chi, ZQ.(2003).Internalization and recycling of human mu opioid receptors expressed in Sf9 insect cells.LIFE SCIENCES,73(1),115-128. |
MLA | Chen, LW,et al."Internalization and recycling of human mu opioid receptors expressed in Sf9 insect cells".LIFE SCIENCES 73.1(2003):115-128. |
入库方式: OAI收割
来源:上海药物研究所
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