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恶性疟原虫:多药耐药性。

Plasmodium falciparum: Multidrug resistance.

机构信息

School of Biotechnology, KIIT University, Bhubaneswar, Odisha, India.

出版信息

Chem Biol Drug Des. 2019 May;93(5):737-759. doi: 10.1111/cbdd.13484. Epub 2019 Feb 12.

Abstract

Malaria is the most lethal and debilitating disease caused by the protozoan parasite Plasmodium worldwide. The most severe forms of disease and the incidence rates of mortality are associated with P. falciparum infections. With the identification of disease source and symptoms, many chemical entities were developed naturally and synthetically for administration as a potential antimalarial drug. The major classes of approved antimalarial drugs that are governed as first-line treatment in tropical and subtropical areas include quinolines, naphthoquinones, antifolates, 8-aminoquinolines, and endoperoxides. However, the efficacy of antimalarial drugs has decreased due to ongoing multidrug resistance problem to current drugs. With increasing resistance to the current antimalarial artemisinin and its combination therapies, malaria prophylaxis has declined gradually. New-generation antimalarial and novel drug target are required to check the incidence of malaria resistance. This review summarizes the emergence of multidrug resistance to known antimalarial and the development of new antimalarial to resolve drug resistance condition. Few essential proteins are also discussed that can be considered as novel drug target against malaria in future.

摘要

疟疾是由疟原虫引起的最致命和致残的疾病,在全球范围内。最严重的疾病形式和死亡率的发生率与恶性疟原虫感染有关。随着对疾病来源和症状的认识,许多天然和合成的化学实体被开发出来,作为一种潜在的抗疟药物进行管理。在热带和亚热带地区,被批准的主要抗疟药物类别包括喹啉类、萘醌类、抗叶酸类、8-氨基喹啉类和内过氧化物类。然而,由于目前药物持续存在的多药耐药问题,抗疟药物的疗效已经下降。随着对当前抗疟药青蒿素及其联合疗法的耐药性不断增加,疟疾预防逐渐下降。需要新一代的抗疟药和新的药物靶点来控制疟疾耐药性的发生。这篇综述总结了已知抗疟药的多药耐药性的出现以及新抗疟药的开发,以解决耐药性问题。还讨论了一些基本的蛋白质,这些蛋白质可以被认为是未来对抗疟疾的新药物靶点。

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