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Drug resistance in African trypanosomiasis: the melarsoprol and pentamidine story.非洲锥虫病的耐药性：美拉胂醇和喷他脒的故事。
Trends Parasitol. 2013 Mar;29(3):110-8. doi: 10.1016/j.pt.2012.12.005. Epub 2013 Jan 30.
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Melarsoprol Resistance in African Trypanosomiasis.梅拉硫磷耐药性与非洲锥虫病。
Trends Parasitol. 2018 Jun;34(6):481-492. doi: 10.1016/j.pt.2018.04.002. Epub 2018 Apr 25.
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Positively selected modifications in the pore of TbAQP2 allow pentamidine to enter .TbAQP2 孔中的正选择修饰允许戊烷脒进入。
Elife. 2020 Aug 11;9:e56416. doi: 10.7554/eLife.56416.
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Arsenicals (melarsoprol), pentamidine and suramin in the treatment of human African trypanosomiasis.砷剂（美拉胂醇）、喷他脒和苏拉明用于治疗人类非洲锥虫病。
Parasitol Res. 2003 May;90(1):71-9. doi: 10.1007/s00436-002-0799-9. Epub 2003 Jan 31.
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Melarsoprol sensitivity profile of Trypanosoma brucei gambiense isolates from cured and relapsed sleeping sickness patients from the Democratic Republic of the Congo.来自刚果民主共和国已治愈和复发昏睡病患者的布氏冈比亚锥虫分离株的美拉胂醇敏感性概况。
PLoS Negl Trop Dis. 2014 Oct 2;8(10):e3212. doi: 10.1371/journal.pntd.0003212. eCollection 2014 Oct.
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Aquaglyceroporin 2 controls susceptibility to melarsoprol and pentamidine in African trypanosomes.水甘油通道蛋白 2 控制非洲锥虫对米替福新和喷他脒的敏感性。
Proc Natl Acad Sci U S A. 2012 Jul 3;109(27):10996-1001. doi: 10.1073/pnas.1202885109. Epub 2012 Jun 18.
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Anti-sleeping sickness drugs and cancer chemotherapy.抗昏睡病药物与癌症化疗。
Parasitol Today. 2000 Jan;16(1):7-9. doi: 10.1016/s0169-4758(99)01560-4.
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Trypanosoma brucei aquaglyceroporin 2 is a high-affinity transporter for pentamidine and melaminophenyl arsenic drugs and the main genetic determinant of resistance to these drugs.布氏锥虫水甘油通道蛋白2是喷他脒和美拉明苯基砷药物的高亲和力转运体，也是对这些药物耐药性的主要遗传决定因素。
J Antimicrob Chemother. 2014 Mar;69(3):651-63. doi: 10.1093/jac/dkt442. Epub 2013 Nov 13.
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Chimerization at the AQP2-AQP3 locus is the genetic basis of melarsoprol-pentamidine cross-resistance in clinical Trypanosoma brucei gambiense isolates.在临床布氏冈比亚锥虫分离株中，水通道蛋白2-水通道蛋白3基因座的嵌合化是美拉胂醇-喷他脒交叉耐药性的遗传基础。
Int J Parasitol Drugs Drug Resist. 2015 May 7;5(2):65-8. doi: 10.1016/j.ijpddr.2015.04.002. eCollection 2015 Aug.
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The biochemical basis of arsenical-diamidine crossresistance in African trypanosomes.非洲锥虫中砷剂-双脒交叉耐药性的生化基础。
Parasitol Today. 1999 Apr;15(4):136-40. doi: 10.1016/s0169-4758(99)01414-3.
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Human African Trypanosomiasis (HAT): Epidemiology, Biological Diagnosis and Treatment: A Review.人类非洲锥虫病（昏睡病）：流行病学、生物学诊断与治疗：综述
Acta Parasitol. 2025 Sep 9;70(5):193. doi: 10.1007/s11686-025-01128-6.
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Controlling rate of release of tsetse fly repellent blend by encapsulating in β-cyclodextrin nanoparticles.通过包封于β-环糊精纳米颗粒中来控制采采蝇驱避剂混合物的释放速率。
J Nanotechnol. 2025;2025(1). doi: 10.1155/jnt/6677970. Epub 2025 Mar 24.
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Antiproliferative and Trypanocidal Activity of Ivermectin Bioconjugates.伊维菌素生物共轭物的抗增殖和杀锥虫活性
ACS Omega. 2025 Jun 18;10(25):27380-27392. doi: 10.1021/acsomega.5c02998. eCollection 2025 Jul 1.
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Discovery of Novel CRK12 Inhibitors for the Treatment of Human African Trypanosomiasis: An Integrated Computational and Experimental Approach.发现用于治疗人类非洲锥虫病的新型CRK12抑制剂：一种综合计算和实验的方法。
Pharmaceuticals (Basel). 2025 May 23;18(6):778. doi: 10.3390/ph18060778.
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Chalcogen Derivatives for the Treatment of African Trypanosomiasis: Biological Evaluation of Thio- and Seleno-Semicarbazones and Their Azole Derivatives.用于治疗非洲锥虫病的硫属元素衍生物：硫代和硒代氨基脲及其唑类衍生物的生物学评价
ACS Omega. 2025 Jun 5;10(23):24872-24886. doi: 10.1021/acsomega.5c02014. eCollection 2025 Jun 17.
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Uncovering the Unusual Inhibition Mechanism of a Trypanosome Alternative Oxidase Inhibitor Displaying Broad-Spectrum Activity against African Animal Trypanosomes.揭示一种对非洲动物锥虫具有广谱活性的锥虫交替氧化酶抑制剂的异常抑制机制。
J Med Chem. 2025 Aug 28;68(16):17155-17174. doi: 10.1021/acs.jmedchem.5c00631. Epub 2025 Jun 4.
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Carmaphycin B-Based Proteasome Inhibitors to Treat Human African Trypanosomiasis: Structure-Activity Relationship and Efficacy.基于卡马霉素B的蛋白酶体抑制剂治疗人类非洲锥虫病：构效关系与疗效
ACS Infect Dis. 2024 Dec 13;10(12):4182-4193. doi: 10.1021/acsinfecdis.4c00441. Epub 2024 Nov 26.
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New Lipophilic Hydroxamates as Promising Trypanocidal Agents: Design, Synthesis, SAR, and Conformational Behavior Studies.新型亲脂性异羟肟酸酯作为有前景的杀锥虫剂：设计、合成、构效关系及构象行为研究
ACS Med Chem Lett. 2024 Jun 6;15(7):1041-1048. doi: 10.1021/acsmedchemlett.4c00111. eCollection 2024 Jul 11.
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An in-depth exploration of the multifaceted roles of EVs in the context of pathogenic single-cell microorganisms.深入探讨 EV 在致病单细胞微生物背景下的多方面作用。
Microbiol Mol Biol Rev. 2024 Sep 26;88(3):e0003724. doi: 10.1128/mmbr.00037-24. Epub 2024 Jun 13.
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Structural insights into drug transport by an aquaglyceroporin.水通道蛋白介导药物转运的结构基础研究
Nat Commun. 2024 May 11;15(1):3985. doi: 10.1038/s41467-024-48445-4.
本文引用的文献
1
Safety and efficacy of the 10-day melarsoprol schedule for the treatment of second stage Rhodesiense sleeping sickness.10 天美拉胂醇方案治疗第二期罗得西亚锥虫病的安全性和疗效。
PLoS Negl Trop Dis. 2012 Aug;6(8):e1695. doi: 10.1371/journal.pntd.0001695. Epub 2012 Aug 28.
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Pharmacology of DB844, an orally active aza analogue of pafuramidine, in a monkey model of second stage human African trypanosomiasis.DB844 的药理学研究，一种口服有效的 pafuramidine 的氮杂类似物，在第二阶段人体非洲锥虫病的猴模型中。
PLoS Negl Trop Dis. 2012;6(7):e1734. doi: 10.1371/journal.pntd.0001734. Epub 2012 Jul 24.
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Modulation of Leishmania major aquaglyceroporin activity by a mitogen-activated protein kinase.丝裂原活化蛋白激酶对利什曼原虫水通道蛋白活性的调节。
Mol Microbiol. 2012 Sep;85(6):1204-18. doi: 10.1111/j.1365-2958.2012.08169.x. Epub 2012 Jul 26.
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Aquaglyceroporin 2 controls susceptibility to melarsoprol and pentamidine in African trypanosomes.水甘油通道蛋白 2 控制非洲锥虫对米替福新和喷他脒的敏感性。
Proc Natl Acad Sci U S A. 2012 Jul 3;109(27):10996-1001. doi: 10.1073/pnas.1202885109. Epub 2012 Jun 18.
5
Update on field use of the available drugs for the chemotherapy of human African trypanosomiasis.更新现有的抗人体非洲锥虫病化疗药物的现场使用情况。
Parasitology. 2012 Jun;139(7):842-6. doi: 10.1017/S0031182012000169. Epub 2012 Feb 6.
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High-throughput decoding of antitrypanosomal drug efficacy and resistance.高通量解码抗锥虫药物疗效和耐药性。
Nature. 2012 Jan 25;482(7384):232-6. doi: 10.1038/nature10771.
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MIPModDB: a central resource for the superfamily of major intrinsic proteins.MIPModDB：主要内在蛋白超家族的中央资源。
Nucleic Acids Res. 2012 Jan;40(Database issue):D362-9. doi: 10.1093/nar/gkr914. Epub 2011 Nov 12.
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New prodrugs of the antiprotozoal drug pentamidine.新型抗寄生虫药物喷他脒前药。
ChemMedChem. 2011 Dec 9;6(12):2233-42. doi: 10.1002/cmdc.201100422. Epub 2011 Oct 7.
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Drug resistance in human African trypanosomiasis.人体非洲锥虫病的耐药性。
Future Microbiol. 2011 Sep;6(9):1037-47. doi: 10.2217/fmb.11.88.
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Melarsoprol cyclodextrin inclusion complexes as promising oral candidates for the treatment of human African trypanosomiasis.环糊精包合物作为有前途的口服药物用于治疗非洲人类锥虫病。
PLoS Negl Trop Dis. 2011 Sep;5(9):e1308. doi: 10.1371/journal.pntd.0001308. Epub 2011 Sep 6.
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