A New Generation of Specific Trypanosoma cruzi trans-Sialidase Inhibitors

摘要

The protozoan parasite Trypanosoma cruzi is the causative agent of human American trypanosomiasis, also known as Chagas' disease, which in its chronic form can lead to severe debilitation and ultimately death. According to World Health Organization (WHO) estimates, 16 to 18 million people were infected in Latin America in 2005. Only two approved drugs (nifurtimox and benznidazole) are currently used for the treatment of the infection, but both display low efficacy and are associated with severe undesired side effects. The whole genome sequence of Trypanosoma cruzi, completed in 2005, contains genes predicted to encode almost 23 000 proteins. The identification of essential proteins specific to the parasite will hopefully provide attractive new drug targets. Among such targets, the Trypanosoma cruzi trans-sialidase (TcTS) has been extensively studied.