Department of Biological Sciences, Faculty of Science, National University of Singapore, Singapore 117543, Singapore.
Toxicon. 2010 Nov;56(6):855-67. doi: 10.1016/j.toxicon.2010.07.010. Epub 2010 Jul 27.
Snake venoms are complex mixtures of pharmacologically active peptides and proteins. These protein toxins belong to a small number of superfamilies of proteins. Three-finger toxins belong to a superfamily of non-enzymatic proteins found in all families of snakes. They have a common structure of three beta-stranded loops extending from a central core containing all four conserved disulphide bonds. Despite the common scaffold, they bind to different receptors/acceptors and exhibit a wide variety of biological effects. Thus, the structure-function relationships of this group of toxins are complicated and challenging. Studies have shown that the functional sites in these 'sibling' toxins are located on various segments of the molecular surface. Targeting to a wide variety of receptors and ion channels and hence distinct functions in this group of mini proteins is achieved through a combination of accelerated rate of exchange of segments as well as point mutations in exons. In this review, we describe the structural and functional diversity, structure-function relationships and evolution of this group of snake venom toxins.
蛇毒是具有药理活性的肽类和蛋白质的复杂混合物。这些蛋白毒素属于少数几种蛋白质超家族。三指毒素属于在所有蛇科中都存在的非酶蛋白的超家族。它们具有从包含所有四个保守二硫键的中心核心延伸的三个β-折叠环的共同结构。尽管具有共同的支架,但它们结合不同的受体/接受器,并表现出广泛的生物学效应。因此,这群毒素的结构-功能关系复杂且具有挑战性。研究表明,这些“兄弟姐妹”毒素中的功能位点位于分子表面的不同片段上。通过片段交换率的加速以及外显子中的点突变的组合,针对该组小型蛋白质中的各种受体和离子通道,从而实现了不同的功能。在这篇综述中,我们描述了这群蛇毒毒素的结构和功能多样性、结构-功能关系和进化。