单个S1034C突变赋予对PfMDR1 ATP酶活性改变的药物敏感性，这是7G8亚型的特征。
A single S1034C mutation confers altered drug sensitivity to PfMDR1 ATPase activity that is characteristic of the 7G8 isoform.
作者信息
Lekostaj Jacqueline K, Amoah Linda E, Roepe Paul D
机构信息
Department of Chemistry, Department of Biochemistry, Cellular & Molecular Biology, Lombardi Cancer Center, Georgetown University, 37th and O Streets, Washington, DC 20057, USA.
出版信息
Mol Biochem Parasitol. 2008 Jan;157(1):107-11. doi: 10.1016/j.molbiopara.2007.09.008. Epub 2007 Oct 5.
Abstract
The mechanism behind how PfMDR1 may contribute to antimalarial drug resistance is unclear. Transfection studies suggest that PfMDR1 mutations may make small contributions to drug sensitivity in a strain-dependent fashion, whereas field data link over expression (not necessarily mutation) of the gene with clinical drug treatment failure. This study dissects the contribution of individual mutations of PfMDR1 that contribute to the unique behavior of the 7G8 PfMDR1 isoform. A single mutation in putative TM 11 (S1034C) is found to abolish drug stimulation of PfMDR1 ATPase activity.
摘要
疟原虫多药耐药蛋白1（PfMDR1）导致抗疟药耐药性的背后机制尚不清楚。转染研究表明，PfMDR1突变可能以菌株依赖的方式对药物敏感性产生微小影响，而现场数据将该基因的过表达（不一定是突变）与临床药物治疗失败联系起来。本研究剖析了PfMDR1单个突变对7G8 PfMDR1亚型独特行为的影响。研究发现，假定跨膜区11（TM 11）中的单个突变（S1034C）可消除对PfMDR1 ATP酶活性的药物刺激。
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