| Item type |
学術雑誌論文 / Journal Article(1) |
| 公開日 |
2024-10-17 |
| タイトル |
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タイトル |
An aromatic amino acid within intracellular loop 2 of the prostaglandin EP2 receptor is a prerequisite for selective association and activation of Gαs |
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言語 |
en |
| 言語 |
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言語 |
eng |
| キーワード |
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主題 |
Eicosanoid, G protein-coupled receptor, Heterotrimeric G protein, Prostaglandin, Prostanoid receptor, Receptor structure-function |
| 資源タイプ |
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資源タイプ識別子 |
http://purl.org/coar/resource_type/c_6501 |
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資源タイプ |
journal article |
| アクセス権 |
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アクセス権 |
open access |
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アクセス権URI |
http://purl.org/coar/access_right/c_abf2 |
| 著者 |
Akiko, Yano
Yuko, Takahashi
Hiromi, Moriguchi
Tomoaki, Inazumi
Tomoaki, Koga
Akira, Otaka
Yukihiko, Sugimoto
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| 内容記述 |
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内容記述タイプ |
Abstract |
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内容記述 |
We previously demonstrated that the aromatic moiety of Tyr143 within the intracellular loop 2 (ICL2) region of the prostaglandin EP2 receptor plays a crucial role in Gs coupling. Here we investigated whether the ICL2 of the EP2 receptor directly binds to Gαs and whether an aromatic moiety affects this interaction. In Chinese hamster ovary cells, mutations of Tyr143 reduced the ability of the EP2 receptor to interact with G proteins as demonstrated by GTPγS sensitivity, as well as the ability of agonist-induced cAMP formation, with the rank order of Phe > Tyr (wild-type) = Trp > Leu > Ala (= 0). We found that the wild-type ICL2 peptide (i2Y) and its mutant with Phe at Tyr143 (i2F) inhibited receptor-G protein complex formation of wild-type EP2 in membranes, whereas the Ala-substituted mutant (i2A) did not. Specific interactions between these peptides and the Gαs protein were detected by surface plasmon resonance, but Gαs showed different association rates, with a rank order of i2F > i2Y ≫ i2A, with similar dissociation rates. Moreover, i2F and i2Y, but not i2A activated membrane adenylyl cyclase. These results indicate that the ICL2 region of the EP2 receptor is its potential interaction site with Gαs, and that the aromatic side chain moiety at position 143 is a determinant for the accessibility of the ICL2 to the Gαs protein. |
| bibliographic_information |
en : Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids
巻 1862,
号 6,
p. 615-622,
発行年 2017-06
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| item_16_source_id_7 |
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収録物識別子 |
1388-1981 |
| item_16_relation_11 |
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関連タイプ |
isVersionOf |
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関連識別子 |
https://doi.org/10.1016/j.bbalip.2017.03.006 |
| 権利 |
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権利情報 |
(C) 2017 Elsevier B.V. All rights reserved. |
| 権利 |
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権利情報 |
This manuscript version is made available under the CC-BY-NC-ND 4.0 license https://creativecommons.org/licenses/by-nc-nd/4.0/ |
| 出版タイプ |
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出版タイプ |
AM |
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出版タイプResource |
http://purl.org/coar/version/c_ab4af688f83e57aa |
| 出版者 |
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出版者 |
Elsevier |
10.1016_j.bbalip.2017.03.006.pdf (964 KB)
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