Division of Biochemistry, Central Drug Research Institute, Council of Scientific and Industrial Research, Chattar Manzil Palace, Lucknow, India.
Antimicrob Agents Chemother. 2012 Jan;56(1):518-25. doi: 10.1128/AAC.00736-11. Epub 2011 Nov 7.
Emergence of resistance to pentavalent antimonials has become a severe obstacle in the treatment of visceral leishmaniasis (VL) on the Indian subcontinent. The mechanisms operating in laboratory-generated strains are somewhat known, but the determinants of clinical antimony resistance are not well understood. By utilizing a DNA microarray expression profiling approach, we identified a gene encoding mitogen-activated protein kinase 1 (MAPK1) for the kinetoplast protozoan Leishmania donovani (LdMAPK1) that was consistently downregulated in antimony-resistant field isolates. The expression level of the gene was validated by real-time PCR. Furthermore, decreased expression of LdMAPK1 was also confirmed at the protein level in resistant isolates. Primary structure analysis of LdMAPK1 revealed the presence of all of the characteristic features of MAPK1. When expressed in Escherichia coli, the recombinant enzyme showed kinase activity with myelin basic protein as the substrate and was inhibited by staurosporine. Interestingly, overexpression of this gene in a drug-sensitive laboratory strain and a resistant field isolate resulted in increased the sensitivity of the transfectants to potassium antimony tartrate, suggesting that it has a role in antimony resistance. Our results demonstrate that downregulation of LdMAPK1 may be in part correlated with antimony drug resistance in Indian VL isolates.
在印度次大陆,针对五价锑的抗药性的出现已成为治疗内脏利什曼病(VL)的严重障碍。虽然对实验室产生的菌株中起作用的机制有一定了解,但对抗锑药物的耐药性的决定因素还不太清楚。通过利用 DNA 微阵列表达谱分析方法,我们鉴定了一种编码丝裂原活化蛋白激酶 1(MAPK1)的基因,该基因存在于原生动物利什曼原虫(LdMAPK1)中,在抗锑的野外分离株中其表达水平持续下调。通过实时 PCR 验证了该基因的表达水平。此外,在耐药分离株中也证实了 LdMAPK1 的蛋白水平表达下调。LdMAPK1 的一级结构分析表明其具有 MAPK1 的所有特征。当在大肠杆菌中表达时,重组酶以髓鞘碱性蛋白为底物显示激酶活性,并被 staurosporine 抑制。有趣的是,该基因在药物敏感的实验室菌株和耐药的野外分离株中的过表达导致转染子对酒石酸锑钾的敏感性增加,这表明它在抗锑耐药性中起作用。我们的研究结果表明,LdMAPK1 的下调可能与印度 VL 分离株对抗锑药物的耐药性部分相关。
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