摘要
背景: 近几十年来,致病酵母白色念珠菌结构中的多组分主要活性ATP结合盒转运体Cdr1p是抗真菌药物抗性的祸首之一。到目前为止,已经对这种蛋白质的各种潜在的新型抑制剂/调节剂进行了纯化,合成和生物学测试,结果表明它们有效地逆转CaCdr1p介导的耐药现象的能力。这些化合物具有不同的来源,具有不相同的结构特征,并采取不同的作用机制。 方法:采用原始研究出版物和综述文章对CaCdr1p研究调节剂的化学特征和机制进行结构化检索。分析与泵的结构和活性有关的可能的泵抑制机制的性质。总结了列出的化合物对2种其他外源白念珠菌外源泵(即Cdr2p和Mdr1p)的调节光谱的过程,其间揭示了Cdr1p的选择性抑制剂。 结果:在本文中,描述了分子可以显示其对外排泵的活性的6种可能的机制,并且提供了文献中发现的近50种CaCdr1p调节剂及其各自机制(如果已经鉴定)的列表总结了迄今为止在寻找能增强常用抗真菌剂效力的药物挤出转运蛋白的新抑制剂方面所获得的结果。还给出了所列化合物对Cdr1p,Cdr2p和Mdr1p的抑制谱图,最后显示了几种Cdr1p的选择性调节剂。 结论:本综述的结果通过总结迄今为止在新出现的健康科学问题上获得的结果,有助于今后对CaCdr1p及其调节剂的研究。需要进一步研究能够抑制Cdr1p的新型化合物,希望完成本文提供的列表。
关键词: 白色念珠菌,Cdr1p,外排泵,调节剂,抑制剂,机制,结合,相互作用。
Current Medicinal Chemistry
Title:Modulators of the Efflux Pump Cdr1p of Candida albicans: Mechanisms of Action and Chemical Features
Volume: 24 Issue: 30
关键词: 白色念珠菌,Cdr1p,外排泵,调节剂,抑制剂,机制,结合,相互作用。
摘要: Background: The multicomponent primary active ATP-binding cassette transporter Cdr1p in the structure of the pathogenic yeast Candida albicans is among the culprits of antifungal agent resistance reported in recent decades. So far, various potential novel inhibitors/ modulators of this protein have been purified, synthesized, and biologically tested, with results showing their ability to effectively reverse CaCdr1p-mediated drug resistance phenomenon. These compounds are of diverse origins, possess non-identical structural features and adopt different mechanisms of action.
Method: A structured search of chemical features and mechanisms of studied modulators of CaCdr1p was carried out using both original research publications and review articles. The nature of possible inhibitory mechanisms against the pump was analyzed in relation to the structure and the activity of the transporter. A process of summarizing modulatory spectra of the listed compounds against 2 other efflux pumps of Candida albicans namely Cdr2p and Mdr1p was also conducted, during which selective inhibitors of Cdr1p were revealed.
Results: In this article, 6 possible mechanisms with which a molecule can manifest their activity against the efflux pump are described, and a list of nearly 50 CaCdr1p modulators found in literatures along with their respective mechanism(s) (if already identified) is provided, summarizing the results obtained so far in the search of new inhibitors of the drug extrusion transporter that can enhance the potency of commonly used antifungal agents. A table of inhibitory spectra of the listed compounds against Cdr1p, Cdr2p and Mdr1p is also given, with several selective modulators of Cdr1p finally indicated.
Conclusion: The findings of this review contribute to future studies regarding CaCdr1p and its modulators by summarizing the results obtained so far on this emerging issue of health sciences. Further research concerning novel compounds capable of inhibiting Cdr1p needs to be carried out in hopes of completing the lists provided in this article.
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Cite this article as:
Modulators of the Efflux Pump Cdr1p of Candida albicans: Mechanisms of Action and Chemical Features, Current Medicinal Chemistry 2017; 24 (30) . https://dx.doi.org/10.2174/0929867324666170523102244
DOI https://dx.doi.org/10.2174/0929867324666170523102244 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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