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oai:kinjo.repo.nii.ac.jp:02000030 2025-09-23T06:01:21Z 113 113:18 113:18:1701331345768

ブラジキニンB2受容体C末端のリン酸化が アゴニストによる脱感作に与える影響 Effect of phosphorylation of the bradykinin B2 receptor C-terminus on agonist-induced desensitization 小崎, 康子 KOZAKI, Yasuko 服部, あみ HATTORI, Ami 小須田, 幸江 KOSUDA, Yukie 尾内, 彩乃 ONOUCHI, Ayano 鈴木, 義明 SUZUKI, Yoshiaki Bradykinin（ BK） is an endogenous pain substance, and desensitization by repeated administration of BK is a well-known phenomenon. In the present study, we observed that pretreatment with BK reduced BK binding and pretreatment with concanavalin A, a receptor internalization inhibitor, inhibited BK internalization in Chinese hamster ovary （CHO） cells stably expressing the mouse BK B2 receptor（ wild type）. It has been reported that BK-induced receptor internalization is mediated by tandem phosphorylation of the BK receptor C-terminus. Therefore, we introduced point mutations at the candidate phosphorylation sites to obtain B2 receptor mutations 1（ Ser367Ala, Thr370Ala）, 2 （Ser374Ala, Ser376Ala） and 3（ Ser367Ala, Thr370Ala, Ser374Ala, Ser376Ala）. We then observed ［3 H］BK binding and internalization in CHO cells stably expressing wild-type and B2 receptor mutations 1, 2, and 3. The ［3 H］BK internalization was found to be most reduced in cells expressing mutation 3. This suggests that phosphorylation of amino acid residues at all four sites is involved in B2 receptor internalization, namely, desensitization to BK. 金城学院大学 2023-03-30 jpn departmental bulletin paper https://kinjo.repo.nii.ac.jp/records/2000030 18800378 金城学院大学論集. 自然科学編 Treatises and Studies by the Faculty of Kinjo Gakuin University. Studies in Natural Sciences 19 2 1 7 https://kinjo.repo.nii.ac.jp/record/2000030/files/01_Yasuko KOZAKI,Ami HATTORI,Yukie KOSUDA,Ayano ONOUCHI,Yoshiaki SUZUKI.pdf application/pdf 1.3 MB 2023-12-25