Lye Lon-Fye, Kang Song Ok, Nosanchuk Joshua D, Casadevall Arturo, Beverley Stephen M
Department of Molecular Microbiology, Box 8230, Washington University Medicine School, 600 S. Euclid Ave., St. Louis, MO 63110, USA.
Mol Biochem Parasitol. 2011 Jan;175(1):58-67. doi: 10.1016/j.molbiopara.2010.09.004. Epub 2010 Sep 29.
Aromatic amino acid hydroxylases (AAAH) typically use tetrahydrobiopterin (H(4)B) as the cofactor. The protozoan parasite Leishmania major requires biopterin for growth and expresses strong salvage and regeneration systems to maintain H(4)B levels. Here we explored the consequences of genetic manipulation of the sole L. major phenylalanine hydroxylase (PAH) to explore whether it could account for the Leishmania H(4)B requirement. L. major PAH resembles AAAHs of other organisms, bearing eukaryotic-type domain organization, and conservation of key catalytic residues including those implicated in pteridine binding. A pah(-) null mutant and an episomal complemented overexpressing derivative (pah-/+PAH) were readily obtained, and metabolic labeling studies established that PAH was required to hydroxylate Phe to Tyr. Neither WT nor overexpressing lines were able to hydroxylate radiolabeled tyrosine or tryptophan, nor to synthesize catecholamines. WT but not pah(-) parasites showed reactivity with an antibody to melanin when grown with l-3,4-dihydroxyphenylalanine (L-DOPA), although the reactive product is unlikely to be melanin sensu strictu. WT was auxotrophic for Phe, Trp and Tyr, suggesting that PAH activity was insufficient to meet normal Tyr requirements. However, pah(-) showed an increased sensitivity to Tyr deprivation, while the pah(-)/+PAH overexpressor showed increased survival and could be adapted to grow well without added Tyr. pah(-) showed no alterations in H(4)B-dependent differentiation, as established by in vitro metacyclogenesis, or survival in mouse or macrophage infections. Thus Leishmania PAH may mitigate but not alleviate Tyr auxotrophy, but plays no essential role in the steps of the parasite infectious cycle. These findings suggest PAH is unlikely to explain the Leishmania requirement for biopterin.
芳香族氨基酸羟化酶(AAAH)通常使用四氢生物蝶呤(H(4)B)作为辅因子。原生动物寄生虫利什曼原虫需要生物蝶呤来生长,并表达强大的补救和再生系统以维持H(4)B水平。在此,我们探究了对利什曼原虫唯一的苯丙氨酸羟化酶(PAH)进行基因操作的后果,以探讨它是否能解释利什曼原虫对H(4)B的需求。利什曼原虫PAH类似于其他生物体的AAAH,具有真核生物类型的结构域组织,并且关键催化残基保守,包括那些与蝶呤结合有关的残基。我们很容易获得了pah(-)缺失突变体和一个游离型互补过表达衍生物(pah-/+PAH),代谢标记研究证实PAH是将苯丙氨酸羟化为酪氨酸所必需的。野生型(WT)和过表达系均无法将放射性标记的酪氨酸或色氨酸羟化,也无法合成儿茶酚胺。当与L-3,4-二羟基苯丙氨酸(L-DOPA)一起生长时,野生型寄生虫而非pah(-)寄生虫显示出与黑色素抗体的反应性,尽管反应产物不太可能是严格意义上的黑色素。野生型对苯丙氨酸、色氨酸和酪氨酸是营养缺陷型,这表明PAH活性不足以满足正常的酪氨酸需求。然而,pah(-)对酪氨酸剥夺表现出更高的敏感性,而pah(-)/+PAH过表达体显示出更高的存活率,并且可以在不添加酪氨酸的情况下适应良好生长。通过体外循环前体形成确定,pah(-)在H(4)B依赖性分化方面没有改变,在小鼠或巨噬细胞感染中的存活率也没有改变。因此,利什曼原虫PAH可能减轻但不能缓解酪氨酸营养缺陷,但在寄生虫感染周期的步骤中不发挥重要作用。这些发现表明PAH不太可能解释利什曼原虫对生物蝶呤的需求。