Ortiz Diana, Sanchez Marco A, Quecke Paula, Landfear Scott M
Department of Molecular Microbiology and Immunology, Oregon Health & Science University, Portland, OR 97239, USA.
Mol Biochem Parasitol. 2009 Feb;163(2):67-76. doi: 10.1016/j.molbiopara.2008.09.011. Epub 2008 Oct 17.
African trypanosomes are unable to synthesize purines de novo and must salvage preformed purine nucleosides and nucleobases from their hosts. The Trypanosoma brucei genome project has identified 12 members of the equilibrative nucleoside transporter family, most of which have been characterized previously as nucleoside and/or nucleobase transporters. Here the 11th member of this family, TbNT11.1, has been functionally expressed in null mutants of Leishmania that are deficient in purine nucleoside or nucleobase uptake and identified as a high-affinity purine nucleobase transporter. Expression of TbNT11.1 in Xenopus oocytes revealed that it is also a transporter for the diamidine drug pentamidine that is the principal drug employed to treat early stage human African trypanosomiasis and may thus contribute to the uptake of this therapeutically important compound. In addition, characterization of the 12th member of the family, TbNT12.1, reveals that it is an adenine/pentamidine transporter.
非洲锥虫无法从头合成嘌呤,必须从宿主那里获取现成的嘌呤核苷和碱基。布氏锥虫基因组计划已鉴定出12个平衡核苷转运体家族成员,其中大多数此前已被表征为核苷和/或碱基转运体。在此,该家族的第11个成员TbNT11.1在嘌呤核苷或碱基摄取缺陷的利什曼原虫无功能突变体中实现了功能表达,并被鉴定为一种高亲和力的嘌呤碱基转运体。TbNT11.1在非洲爪蟾卵母细胞中的表达表明,它也是双脒类药物喷他脒的转运体,喷他脒是治疗早期人类非洲锥虫病的主要药物,因此可能有助于摄取这种具有重要治疗意义的化合物。此外,对该家族第12个成员TbNT12.1的表征表明,它是一种腺嘌呤/喷他脒转运体。