Sivagurunathan Senthilkumar, Heaslip Aoife, Liu Jun, Hu Ke
Department of Biology, Indiana University, Bloomington, IN 47405, USA.
Mol Biochem Parasitol. 2013 May;189(1-2):43-53. doi: 10.1016/j.molbiopara.2013.05.004. Epub 2013 May 17.
The intracellular parasite Toxoplasma gondii is a leading cause of congenital neurological defects. To cause disease, it must reiterate its lytic cycle through host cell invasion, replication, and parasite egress. This requires the parasite to sense changes in its environment and switch between the non-motile (for replication) and motile (for invasion and egress) states appropriately. Recently, we discovered a previously unknown mechanism of motility regulation in T. gondii, mediated by a lysine methyltransferase, AKMT (for Apical complex lysine (K) methyltransferase). When AKMT is absent, activation of motility is inhibited, which compromises parasite invasion and egress, and thus severely impairs the lytic cycle. Although the methyltransferase activity of AKMT has been established, the phylogenetic relationship of AKMT with other better studied lysine methyltransferases (KMTs) was not known. Also unknown was the functional relationships between different domains of AKMT. In this work we carried out phylogenetic analyses, which show that AKMT orthologs form a new subfamily of KMTs. We systematically generated truncation mutants of AKMT, and discovered that the predicted enzymatic domain alone is a very poor enzyme and cannot complement the function of AKMT in vivo. Interestingly, the N- and C-terminal domains of the AKMT have drastically different impacts on its enzyme activity, localization as well as in vivo function. Our results thus reveal that AKMT is an unusual, parasite-specific enzyme and identified regions and interactions within this novel lysine methyltransferase that can be used as drug targets.
细胞内寄生虫刚地弓形虫是先天性神经缺陷的主要病因。为引发疾病,它必须通过宿主细胞入侵、复制和寄生虫逸出反复进行其裂解周期。这要求寄生虫感知其环境变化并在非运动状态(用于复制)和运动状态(用于入侵和逸出)之间适当地切换。最近,我们发现了刚地弓形虫中一种以前未知的运动调节机制,由一种赖氨酸甲基转移酶AKMT(顶复合赖氨酸(K)甲基转移酶)介导。当缺乏AKMT时,运动的激活受到抑制,这会损害寄生虫的入侵和逸出,从而严重损害裂解周期。尽管AKMT的甲基转移酶活性已经确定,但AKMT与其他研究更深入的赖氨酸甲基转移酶(KMTs)的系统发育关系尚不清楚。AKMT不同结构域之间的功能关系也不清楚。在这项工作中,我们进行了系统发育分析,结果表明AKMT直系同源物形成了一个新的KMT亚家族。我们系统地构建了AKMT的截短突变体,发现仅预测的酶结构域是一种非常低效的酶,无法在体内补充AKMT的功能。有趣的是,AKMT的N端和C端结构域对其酶活性、定位以及体内功能有截然不同的影响。因此,我们的结果表明AKMT是一种不同寻常的、寄生虫特异性的酶,并确定了这种新型赖氨酸甲基转移酶内可作为药物靶点的区域和相互作用。