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量调节的化物通道与人类多重耐药性P-糖蛋白相关
M A Valverde1, M Díaz, F V Sepúlveda
1AFRC Institute of Animal Physiology and Genetics Research, Babraham, Cambridge, UK.
Nature
|February 27, 1992
概括
与多种药物耐药性相关的载体P-糖蛋白形成了依赖ATP的化物选择性道. 这些通道是由细胞体积调节的,这表明P-葡萄糖蛋白在药物排放之外具有新的生理作用.
科学领域:
- 生物化学 生物化学
- 细胞生物学 细胞生物学
- 分子生物学分子生物学
背景情况:
- 已知由MDR1基因编码的P-糖蛋白通过积极地将疏水性药物从细胞中运输出来,从而赋予多种药物耐药性.
- P-葡萄糖蛋白属于ATP结合盒 (ABC) 超级家族,其中包括像囊性纤维化转膜调节器 (CFTR) 这样的载体.
- CFTR是一种循环AMP调节的化通道,存在于分泌表皮质中,其他表皮质化通道由细胞体积和细胞内调节.
研究的目的:
- 研究P-糖蛋白在离子通道功能中的潜在作用.
- 探索P-糖蛋白是否与表皮细胞中已知的化物通道有关.
- 为了确定P-糖蛋白表达是否产生新的离子通道活性.
主要方法:
- 在细胞系统中表达P-糖蛋白的表达.
- 电生理学记录以表征离子通道活动.
- 分析道特性,包括离子选择性,ATP依赖性和调节机制.
主要成果:
- P-糖蛋白的表达导致了功能性离子通道的产生.
- 这些通道被发现是选择性化物和依赖ATP的.
- 这些通道表现出体积调节的活性,类似于之前描述的上皮质化物通道.
结论:
- P-葡萄糖蛋白表达可以产生体积调节的,依赖ATP的,选择性化物道.
- 这些发现表明,P-甘氨蛋白在表皮细胞运输中的潜在生理作用超出了多药性耐药性.
- 这项研究强调了P-糖蛋白和其他参与道功能的ABC载体之间的结构和功能相似之处.
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