Biomolecular Science, The North Haugh, The University, St. Andrews, Fife Scotland KY16 9ST, UK.
Mol Microbiol. 2010 Jun;76(6):1461-82. doi: 10.1111/j.1365-2958.2010.07151.x. Epub 2010 Apr 1.
Sphingomyelin is the main sphingolipid in Trypanosoma brucei, the causative agent of African sleeping sickness. In vitro and in vivo characterization of the T. brucei neutral sphingomyelinase demonstrates that it is directly involved in sphingomyelin catabolism. Gene knockout studies in the bloodstream form of the parasite indicate that the neutral sphingomyelinase is essential for growth and survival, thus highlighting that the de novo biosynthesis of ceramide is unable to compensate for the loss of sphingomyelin catabolism. The phenotype of the conditional knockout has given new insights into the highly active endocytic and exocytic pathways in the bloodstream form of T. brucei. Hence, the formation of ceramide in the endoplasmic reticulum affects post-Golgi sorting and rate of deposition of newly synthesized GPI-anchored variant surface glycoprotein on the cell surface. This directly influences the corresponding rate of endocytosis, via the recycling endosomes, of pre-existing cell surface variant surface glycoprotein. The trypanosomes use this coupled endocytic and exocytic mechanism to maintain the cell density of its crucial variant surface glycoprotein protective coat. TbnSMase is therefore genetically validated as a drug target against African trypanosomes, and suggests that interfering with the endocytic transport of variant surface glycoprotein is a highly desirable strategy for drug development against African trypanosomasis.
鞘磷脂是布氏锥虫(引起非洲昏睡病的病原体)中的主要神经鞘脂。对布氏锥虫中性神经鞘磷脂酶的体外和体内特性的研究表明,它直接参与神经鞘磷脂的分解代谢。寄生虫血腔形式的基因敲除研究表明,中性神经鞘磷脂酶对生长和存活是必需的,因此强调从头合成神经酰胺不能弥补神经鞘磷脂分解代谢的损失。条件性敲除的表型为布氏锥虫血腔形式中高度活跃的内吞作用和外排途径提供了新的见解。因此,内质网中神经酰胺的形成影响高尔基体后分拣和新合成的 GPI-锚定变异表面糖蛋白在细胞表面沉积的速度。这直接影响通过再循环内体的先前存在的细胞表面变异表面糖蛋白的相应内吞作用速率。锥虫利用这种偶联的内吞作用和外排机制来维持其关键变异表面糖蛋白保护性涂层的细胞密度。因此,TbnSMase 在遗传上被验证为针对非洲锥虫的药物靶点,并表明干扰变异表面糖蛋白的内吞作用运输是针对非洲锥虫病开发药物的一种非常理想的策略。