• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

疟原虫 PfCRT 介导的药物转运。

PfCRT-mediated drug transport in malarial parasites.

机构信息

Department of Chemistry, Department of Biochemistry and Cellular and Molecular Biology, Georgetown University, Washington, DC 20057, United States.

出版信息

Biochemistry. 2011 Jan 18;50(2):163-71. doi: 10.1021/bi101638n. Epub 2010 Dec 22.

DOI:10.1021/bi101638n
PMID:21142008
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3123679/
Abstract

A wide range of drug transport studies using intact infected red blood cells, isolated malarial parasites, heterologous expression systems, and purified protein, combined with elegant genetic experiments, have suggested that chloroquine transport by the Plasmodium falciparum chloroquine resistance transporter (PfCRT) is a key aspect of the molecular mechanism of quinoline antimalarial drug resistance. However, many questions remain. This short review summarizes data that have led to drug channel versus drug pump hypotheses for PfCRT and suggests ways in which recent contrasting interpretations might be reconciled.

摘要

大量使用完整感染的红细胞、分离的疟原虫、异源表达系统和纯化蛋白的药物转运研究,结合巧妙的遗传实验,表明恶性疟原虫氯喹耐药转运蛋白(PfCRT)对氯喹的转运是奎宁类抗疟药物耐药分子机制的一个关键方面。然而,仍有许多问题尚未解决。本文简要综述了导致 PfCRT 被认为是药物通道或药物泵的相关数据,并提出了最近出现的一些相互矛盾的解释如何得到协调。

相似文献

1
PfCRT-mediated drug transport in malarial parasites.疟原虫 PfCRT 介导的药物转运。
Biochemistry. 2011 Jan 18;50(2):163-71. doi: 10.1021/bi101638n. Epub 2010 Dec 22.
2
Functional Comparison of 45 Naturally Occurring Isoforms of the Plasmodium falciparum Chloroquine Resistance Transporter (PfCRT).恶性疟原虫氯喹抗性转运蛋白(PfCRT)45种天然存在的同工型的功能比较
Biochemistry. 2015 Aug 18;54(32):5083-94. doi: 10.1021/acs.biochem.5b00412. Epub 2015 Aug 6.
3
PfCRT and its role in antimalarial drug resistance.PfCRT 及其在抗疟药物耐药性中的作用。
Trends Parasitol. 2012 Nov;28(11):504-14. doi: 10.1016/j.pt.2012.08.002. Epub 2012 Sep 25.
4
Altered Drug Transport by Chloroquine Resistance Transporter Isoforms Harboring Mutations Associated with Piperaquine Resistance.氯喹耐药转运体同工型突变导致药物转运改变与哌喹耐药相关。
Biochemistry. 2020 Jul 14;59(27):2484-2493. doi: 10.1021/acs.biochem.0c00247. Epub 2020 Jul 1.
5
Chloroquine transport via the malaria parasite's chloroquine resistance transporter.氯喹通过疟原虫的氯喹抗性转运蛋白进行转运。
Science. 2009 Sep 25;325(5948):1680-2. doi: 10.1126/science.1175667.
6
Molecular basis of the functional conflict between chloroquine and peptide transport in the Malaria parasite chloroquine resistance transporter PfCRT.疟原虫氯喹抗性转运蛋白PfCRT中氯喹与肽转运功能冲突的分子基础
Nat Commun. 2025 Mar 27;16(1):2987. doi: 10.1038/s41467-025-58244-0.
7
Combinatorial Genetic Modeling of pfcrt-Mediated Drug Resistance Evolution in Plasmodium falciparum.恶性疟原虫中pfcrt介导的耐药性进化的组合遗传建模
Mol Biol Evol. 2016 Jun;33(6):1554-70. doi: 10.1093/molbev/msw037. Epub 2016 Feb 22.
8
A 2-amino quinoline, 5-(3-(2-(7-chloroquinolin-2-yl)ethenyl)phenyl)-8-dimethylcarbamyl-4,6-dithiaoctanoic acid, interacts with PfMDR1 and inhibits its drug transport in Plasmodium falciparum.一种2-氨基喹啉,5-(3-(2-(7-氯喹啉-2-基)乙烯基)苯基)-8-二甲基氨基甲酰基-4,6-二硫代辛酸,与恶性疟原虫的PfMDR1相互作用并抑制其药物转运。
Mol Biochem Parasitol. 2014 Jun;195(1):34-42. doi: 10.1016/j.molbiopara.2014.05.006. Epub 2014 Jun 8.
9
Functional characteristics of the malaria parasite's "chloroquine resistance transporter": implications for chemotherapy.疟原虫“氯喹耐药转运蛋白”的功能特征:对化疗的影响。
Virulence. 2010 Jul-Aug;1(4):304-8. doi: 10.4161/viru.1.4.12012.
10
Is PfCRT a channel or a carrier? Two competing models explaining chloroquine resistance in Plasmodium falciparum.疟原虫氯喹抗性转运蛋白(PfCRT)是一种通道还是载体?两种相互竞争的模型解释恶性疟原虫对氯喹的抗性。
Trends Parasitol. 2007 Jul;23(7):332-9. doi: 10.1016/j.pt.2007.04.013. Epub 2007 May 10.

引用本文的文献

1
Antimicrobial resistance with a focus on antibacterial, antifungal, antimalarial, and antiviral drugs resistance, its threat, global priority pathogens, prevention, and control strategies: a review.以抗菌、抗真菌、抗疟和抗病毒药物耐药性为重点的抗微生物药物耐药性、其威胁、全球重点病原体、预防和控制策略:综述
Ther Adv Infect Dis. 2025 May 23;12:20499361251340144. doi: 10.1177/20499361251340144. eCollection 2025 Jan-Dec.
2
Structures of Chloroquine Resistance Transporter (PfCRT) Isoforms and Their Interactions with Chloroquine.疟原虫氯通道蛋白(PfCRT)异构体的结构及其与氯喹的相互作用。
Biochemistry. 2023 Mar 7;62(5):1093-1110. doi: 10.1021/acs.biochem.2c00669. Epub 2023 Feb 17.
3
A Plasmodium falciparum RING Finger E3 Ubiquitin Ligase Modifies the Roles of PfMDR1 and PfCRT in Parasite Drug Responses.恶性疟原虫 RING 指 E3 泛素连接酶修饰 PfMDR1 和 PfCRT 在寄生虫药物反应中的作用。
Antimicrob Agents Chemother. 2023 Feb 16;67(2):e0082122. doi: 10.1128/aac.00821-22. Epub 2023 Jan 10.
4
Chloroquine and Sulfadoxine-Pyrimethamine Resistance in Sub-Saharan Africa-A Review.撒哈拉以南非洲地区氯喹和磺胺多辛-乙胺嘧啶耐药性综述
Front Genet. 2021 Jun 25;12:668574. doi: 10.3389/fgene.2021.668574. eCollection 2021.
5
Isolation of Mutants With Reduced Susceptibility to Piperaquine From a Mutator of the Rodent Malaria Parasite .从啮齿动物疟原虫的诱变剂中分离对哌喹敏感性降低的突变体。
Front Cell Infect Microbiol. 2021 Jun 16;11:672691. doi: 10.3389/fcimb.2021.672691. eCollection 2021.
6
Elucidating Mechanisms of Drug-Resistant Plasmodium falciparum.阐明耐药性疟原虫的作用机制。
Cell Host Microbe. 2019 Jul 10;26(1):35-47. doi: 10.1016/j.chom.2019.06.001.
7
Leveraging the effects of chloroquine on resistant malaria parasites for combination therapies.利用氯喹对耐药疟原虫的作用进行联合治疗。
BMC Bioinformatics. 2019 Apr 15;20(1):186. doi: 10.1186/s12859-019-2756-y.
8
Imported and autochthonous malaria in West Saudi Arabia: results from a reference hospital.沙特阿拉伯西部的输入性和本地疟疾:一家参考医院的结果。
Malar J. 2018 Aug 7;17(1):286. doi: 10.1186/s12936-018-2438-7.
9
Analysis of Plasmodium vivax Chloroquine Resistance Transporter Mutant Isoforms.间日疟原虫氯喹抗性转运蛋白突变异构体分析
Biochemistry. 2017 Oct 17;56(41):5615-5622. doi: 10.1021/acs.biochem.7b00749. Epub 2017 Sep 26.
10
Evolution of Fitness Cost-Neutral Mutant PfCRT Conferring P. falciparum 4-Aminoquinoline Drug Resistance Is Accompanied by Altered Parasite Metabolism and Digestive Vacuole Physiology.赋予恶性疟原虫4-氨基喹啉耐药性的适应性成本中性突变体PfCRT的进化伴随着寄生虫代谢和消化液泡生理学的改变。
PLoS Pathog. 2016 Nov 10;12(11):e1005976. doi: 10.1371/journal.ppat.1005976. eCollection 2016 Nov.

本文引用的文献

1
Spiroindolones, a potent compound class for the treatment of malaria.螺环吲哚酮类,一类用于疟疾治疗的强效化合物。
Science. 2010 Sep 3;329(5996):1175-80. doi: 10.1126/science.1193225.
2
Chloroquine susceptibility and reversibility in a Plasmodium falciparum genetic cross.恶性疟原虫遗传杂交中氯喹的敏感性和可逆转性。
Mol Microbiol. 2010 Nov;78(3):770-87. doi: 10.1111/j.1365-2958.2010.07366.x. Epub 2010 Sep 29.
3
Purified Plasmodium falciparum multi-drug resistance protein (PfMDR 1) binds a high affinity chloroquine analogue.纯化的恶性疟原虫多药耐药蛋白(PfMDR 1)可结合一种高亲和力氯喹类似物。
Mol Biochem Parasitol. 2010 Oct;173(2):158-61. doi: 10.1016/j.molbiopara.2010.05.012. Epub 2010 Jun 1.
4
Purified E255L mutant SERCA1a and purified PfATP6 are sensitive to SERCA-type inhibitors but insensitive to artemisinins.纯化的 E255L 突变 SERCA1a 和纯化的 PfATP6 对 SERCA 型抑制剂敏感,但对青蒿素类药物不敏感。
J Biol Chem. 2010 Aug 20;285(34):26406-16. doi: 10.1074/jbc.M109.090340. Epub 2010 Jun 8.
5
Identification of a mutant PfCRT-mediated chloroquine tolerance phenotype in Plasmodium falciparum.鉴定恶性疟原虫 PfCRT 介导的氯喹耐药表型。
PLoS Pathog. 2010 May 13;6(5):e1000887. doi: 10.1371/journal.ppat.1000887.
6
Solution behavior of hematin under acidic conditions and implications for its interactions with chloroquine.血红素在酸性条件下的溶液行为及其与氯喹相互作用的意义。
J Biol Inorg Chem. 2010 Sep;15(7):1009-22. doi: 10.1007/s00775-010-0661-y. Epub 2010 Apr 29.
7
The structure-activity relationship of the antimalarial ozonide arterolane (OZ277).抗疟臭氧烷(OZ277)的构效关系。
J Med Chem. 2010 Jan 14;53(1):481-91. doi: 10.1021/jm901473s.
8
Reduced digestive vacuolar accumulation of chloroquine is not linked to resistance to chloroquine toxicity.氯喹在消化液泡中的积累减少与对氯喹毒性的抗性无关。
Biochemistry. 2009 Dec 1;48(47):11152-4. doi: 10.1021/bi901765v.
9
Chloroquine transport via the malaria parasite's chloroquine resistance transporter.氯喹通过疟原虫的氯喹抗性转运蛋白进行转运。
Science. 2009 Sep 25;325(5948):1680-2. doi: 10.1126/science.1175667.
10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.介导恶性疟原虫不同化学表型的靶点的遗传图谱分析。
Nat Chem Biol. 2009 Oct;5(10):765-71. doi: 10.1038/nchembio.215. Epub 2009 Sep 6.