Bhavya Janardhan, Francois Niyonzima N, More Veena S, More Sunil S
School of Basic and Applied Sciences, Dayanand Sagara University, Bangalore-560078, India.
Protein Pept Lett. 2016;23(9):848-59. doi: 10.2174/0929866523666160630184635.
Scorpions are distributed throughout the world and numerous biological molecules are found in their venom most importantly peptide toxins. These toxins modulate the ion channels either by blocking the pore of the channel or by altering the voltage gating. Molecules which block the pores have been useful in deciphering the structure of the ion channels. Many scorpion toxins have already been used for probing the voltage gated sodium channels and studying their activation and inactivation processes. The specialty of scorpion toxins is to discriminate between vertebrate and invertebrate channels which have led them to applications as pharmacological tools. Most of the scorpion toxin polypeptides were isolated, characterized and were shown to possess vital properties useful in the field of medicine. For instance, they show therapeutic properties such as antimicrobial activity, anticancer activity, used to treat autoimmune diseases and cardiovascular effects. Although the scorpion toxins exhibited good therapeutic effects in vitro and in vivo, no one has reached the market with success up to date. In this mini-review, the scorpion polypeptides, their interactions with ion channels and their uses as therapeutic agents are discussed.
蝎子分布于世界各地,其毒液中含有多种生物分子,其中最重要的是肽毒素。这些毒素通过阻断通道孔或改变电压门控来调节离子通道。阻断通道孔的分子有助于解析离子通道的结构。许多蝎子毒素已被用于探测电压门控钠通道,并研究其激活和失活过程。蝎子毒素的独特之处在于能够区分脊椎动物和无脊椎动物的通道,这使其成为药理学工具。大多数蝎子毒素多肽已被分离、表征,并显示出在医学领域有用的重要特性。例如,它们具有抗菌活性、抗癌活性等治疗特性,可用于治疗自身免疫性疾病和心血管疾病。尽管蝎子毒素在体外和体内都显示出良好的治疗效果,但迄今为止还没有一种成功上市。在这篇综述中,我们将讨论蝎子多肽、它们与离子通道的相互作用以及它们作为治疗剂的用途。