摘要
背景:蛋白质法呢基转移酶(PFT)抑制剂已经成为恶性疟原虫(Pf)寄生虫引起的疟疾治疗的有力靶标。 目的:探讨对Pf-PFT靶标有活性的各种支架。 结果:迄今为止,已经开发了基于乙二胺,拟肽,二苯甲酮,苯甲酰胺,四氢喹啉,萘啶和氧四氢喹啉的七种抑制剂支架。 结论:得出结论:萘啶类药物是最有前景的药物。 此外,将疏水性分子如异戊二烯基引入蛋白质或化学化合物促进蛋白质 - 蛋白质和蛋白质 - 膜相互作用,从而使其成为新的治疗剂的良好候选物。 未来的研究应该集中在疾病而不是感染和传播的动力学上; 这将为疾病带来新的视野。
关键词: 恶性疟原虫,抗疟疾,蛋白质,法呢基转移酶,抑制剂
图形摘要
Current Drug Targets
Title:A Review on Plasmodium falciparum-Protein Farnesyltransferase Inhibitors as Antimalarial Drug Targets
Volume: 18 Issue: 14
关键词: 恶性疟原虫,抗疟疾,蛋白质,法呢基转移酶,抑制剂
摘要: Background: Protein farnesyltransferase (PFT) inhibitors have emerged as a potent target for the malaria treatment caused by the Plasmodium falciparum (Pf) parasite.
Objective: To explore the various scaffolds which are active against Pf-PFT target.
Result: Seven inhibitor scaffolds based on ethylenediamine, peptidomimetic, benzophenone, benzamide, tetrahydroquinoline, naphthyridine and oxy-tetrahydroquinoline, have been developed till date.
Conclusion: It is concluded that naphthyridine based drugs are the most promising one. Furthermore, introducing the hydrophobic molecules like isoprenyl groups to a protein or a chemical compound facilitate protein-protein and protein-membrane interactions thereby makes them good candidates as new therapeutics. The future research should focus on the disease rather than the infection and the dynamics of its transmission; this will bring a new vision about the disease.
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A Review on Plasmodium falciparum-Protein Farnesyltransferase Inhibitors as Antimalarial Drug Targets, Current Drug Targets 2017; 18 (14) . https://dx.doi.org/10.2174/1389450117666160823165004
DOI https://dx.doi.org/10.2174/1389450117666160823165004 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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