Aminoglycoside antibiotics induce pH-sensitive activation of the calcium-sensing receptor

Aminoglycoside antibiotics induce pH-sensitive activation of the calcium-sensing receptor
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DOI:
10.1016/s0006-291x(02)02133-2
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发表时间:
2002-09-13
影响因子:
3.1
通讯作者:
Riccardi, D
Riccardi, D
中科院分区:
生物学4区
文献类型:
--
作者:
McLarnon, SJ;Holden, D;Riccardi, D

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氨基糖苷类抗生素 (AGA) 新霉素是一种已知的细胞外钙敏感受体 (CaR) 激动剂。为了测试其他 AGA 药物是否刺激 Calk,我们使用 CaR 转染的人胚肾 (HEK)-293 细胞研究了四种 AGA 对细胞内 Ca2+ 浓度 ([Ca2+](i)) 的相对影响。庆大霉素、妥布霉素和新霉素在 CaR 转染细胞中引起剂量依赖性的 [Ca2+](i) 增加,EC50 值分别为 258、177 和 43 muM,但在未转染细胞中则不然。卡那霉素在一定剂量下无效
The aminoglycoside antibiotic (AGA) neomycin is a known agonist of the extracellular calcium-sensing receptor (CaR). To test whether other AGA drugs stimulate the Calk, we studied the relative effects of four AGAs on intracellular Ca2+ concentration ([Ca2+](i)) using CaR-transfected human embryonic kidney (HEK)-293 cells. Gentamicin, tobramycin, and neomycin evoked dose-dependent increases in [Ca2+](i) with EC50 values of 258, 177, and 43 muM, respectively, in CaR-transfected, but not in non-transfected cells. Kanamycin was ineffective at doses