Gilbert Ian H
Welsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, UK.
Biochim Biophys Acta. 2002 Jul 18;1587(2-3):249-57. doi: 10.1016/s0925-4439(02)00088-1.
The protozoan diseases leishmaniasis, Chagas' disease and African trypanosomiasis are major health problems in many countries, particularly developing countries, and there are few drugs available to treat these diseases. Dihydrofolate reductase (DHFR) inhibitors have been used successfully in the treatment of a number of other diseases such as cancer, malaria and bacterial infections; however they have not been used for the treatment of these diseases. This article summarises studies on leishmanial and trypanosomal DHFR inhibitor development and evaluation. Possible mechanisms of resistance to DHFR inhibitors are also discussed.
原生动物疾病利什曼病、恰加斯病和非洲锥虫病是许多国家,尤其是发展中国家的主要健康问题,而治疗这些疾病的药物很少。二氢叶酸还原酶(DHFR)抑制剂已成功用于治疗许多其他疾病,如癌症、疟疾和细菌感染;然而,它们尚未用于治疗这些疾病。本文总结了关于利什曼原虫和锥虫DHFR抑制剂开发与评估的研究。还讨论了对DHFR抑制剂产生耐药性的可能机制。