Trypanosomatid protein kinases as potential drug targets.
Trypanosomatid protein kinases as potential drug targets.
复制标题
锥虫蛋白激酶作为潜在的药物靶点。
DOI：
--
复制
发表时间：
2009
期刊：
影响因子：
--
通讯作者：
K. Grant
中科院分区：
文献类型：
--
作者：
M. Wiese;A. Morris;K. Grant
锥虫原虫包括医学上重要的寄生虫布氏锥虫、克氏锥虫和利什曼原虫。它们造成了危害世界发展中国家的一系列疾病。目前治疗这些疾病的化疗还很不理想，人们正在采取许多不同的方法来确定新的药物靶点。一类潜在的药物靶点是原生动物蛋白激酶。蛋白激酶广泛存在于真核生物中，参与多种不同的细胞内信号转导途径，影响细胞的分化、增殖、运动和细胞凋亡等。在寄生原生动物中，几种蛋白激酶起着至关重要的作用，破坏它们的活性对寄生虫是严重有害的。此外，尽管与哺乳动物的蛋白激酶有同源性，但原生动物蛋白激酶在开发寄生虫选择性抑制剂的方式上存在显著差异。在这篇文章中，我们将概述目前重要的寄生虫蛋白激酶的知识，并讨论它们作为新的药物靶点的适用性。
The trypanosomatid protozoa include the medically important parasites Trypanosoma brucei, Trypanosoma cruzi and Leishmania. They are responsible for a wide range of diseases which blight the developing nations of the world. Current chemotherapy to treat these diseases is far from ideal and many different approaches are being taken to identify new drug targets. One family of potential drug targets are the protozoan protein kinases. Protein kinases are ubiquitous in eukaryotes and act in many different intracellular signalling pathways affecting for example: differentiation, proliferation, motility, and apoptosis. Within parasitic protozoa, several protein kinases play essential roles and disruption of their activity is seriously deleterious to the parasite. Moreover, despite homology to their mammalian counterparts, protozoan protein kinases are significantly different in ways which open up the possibility of developing parasite-selective inhibitors. In this article, we will outline the current knowledge of important parasite protein kinases and discuss their suitability as novel drug targets.