Department of Biochemistry and Molecular Biology, Oregon Health and Science University, Portland, OR 97239, USA.
J Biol Chem. 2013 Mar 29;288(13):8977-90. doi: 10.1074/jbc.M112.431486. Epub 2013 Feb 12.
Leishmania are auxotrophic for purines, and consequently purine acquisition from the host is a requisite nutritional function for the parasite. Both adenylosuccinate synthetase (ADSS) and adenylosuccinate lyase (ASL) have been identified as vital components of purine salvage in Leishmania donovani, and therefore Δadss and Δasl null mutants were constructed to test this hypothesis. Unlike wild type L. donovani, Δadss and Δasl parasites in culture exhibited a profoundly restricted growth phenotype in which the only permissive growth conditions were a 6-aminopurine source in the presence of 2'-deoxycoformycin, an inhibitor of adenine aminohydrolase activity. Although both knock-outs showed a diminished capacity to infect murine peritoneal macrophages, only the Δasl null mutant was profoundly incapacitated in its ability to infect mice. The enormous discrepancy in parasite loads observed in livers and spleens from mice infected with either Δadss or Δasl parasites can be explained by selective accumulation of adenylosuccinate in the Δasl knock-out and consequent starvation for guanylate nucleotides. Genetic complementation of a Δasl lesion in Escherichia coli implied that the L. donovani ASL could also recognize 5-aminoimidazole-(N-succinylocarboxamide) ribotide as a substrate, and purified recombinant ASL displayed an apparent Km of ∼24 μm for adenylosuccinate. Unlike many components of the purine salvage pathway of L. donovani, both ASL and ADSS are cytosolic enzymes. Overall, these data underscore the paramount importance of ASL to purine salvage by both life cycle stages of L. donovani and authenticate ASL as a potential drug target in Leishmania.
利什曼原虫是嘌呤营养缺陷型生物,因此从宿主获取嘌呤是寄生虫必需的营养功能。腺嘌呤核苷琥珀酸合成酶(ADSS)和腺嘌呤核苷琥珀酸裂解酶(ASL)已被鉴定为利什曼原虫嘌呤回收的重要组成部分,因此构建了Δadss 和 Δasl 缺失突变体来验证这一假说。与野生型利什曼原虫不同,Δadss 和 Δasl 寄生虫在培养中表现出明显受限的生长表型,只有在腺嘌呤氨基水解酶活性抑制剂 2'-脱氧咖啡酰嘌呤存在时,腺嘌呤核苷才能作为唯一允许的生长条件。尽管两种敲除体的感染鼠腹腔巨噬细胞的能力都有所下降,但只有 Δasl 缺失突变体在感染小鼠的能力上受到严重削弱。用Δadss 或Δasl 寄生虫感染的小鼠肝脏和脾脏中的寄生虫负荷存在巨大差异,可以用 Δasl 敲除体中腺嘌呤核苷的选择性积累和鸟苷酸核苷酸的饥饿来解释。在大肠杆菌中对 Δasl 病变的基因互补表明,利什曼原虫的 ASL 也可以识别 5-氨基咪唑-(N-琥珀酰基羧酰胺)核苷作为底物,纯化的重组 ASL 对腺嘌呤核苷的表观 Km 值约为 24μm。与利什曼原虫嘌呤回收途径的许多成分不同,ASL 和 ADSS 都是细胞质酶。总的来说,这些数据强调了 ASL 对利什曼原虫两个生命周期阶段嘌呤回收的至关重要性,并证实了 ASL 是利什曼原虫的一个潜在药物靶点。