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State of the Art in the Studies on Crotamine a Cell Penetrating Peptide from South American Rattlesnake

机译:研究来自南美洲响尾蛇的一种可穿透细胞的肽巴豆胺的最新技术

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摘要

Animal venoms comprise a naturally selected cocktail of bioactive peptides/proteins and other molecules, each of which playing a defined role thanks to the highly specific interactions with diverse molecular targets found in the prey. Research focused on isolation, structural, and functional characterizations of novel natural biologics (bioactive peptides/proteins from natural sources) has a long way to go through from the basic science to clinical applications. Herein, we overview the structural and functional characteristics of the myoneurotoxin crotamine, firstly isolated from the South American rattlesnake venom. Crotamine is the first venom peptide classified as a natural cell penetrating and antimicrobial peptide (CPP and AMP) with a more pronounced antifungal activity. In contrast to other known natural CPPs and AMPs, crotamine demonstrates a wide spectrum of biological activities with potential biotechnological and therapeutic values. More recent studies have demonstrated the selective in vitro anticancer activity of crotamine. In vivo, using a murine melanoma model, it was shown that crotamine delays tumor implantation, inhibits tumor cells proliferation, and also increases the survival of mice engrafted with subcutaneous melanoma. The structural and functional properties and also the possible biotechnological applications of minimized molecules derived from crotamine are also discussed.
机译:动物毒液包含天然选择的生物活性肽/蛋白质和其他分子的混合物,由于与猎物中发现的多种分子靶标具有高度特异性的相互作用,每种毒剂均起着确定的作用。专注于新型天然生物制剂(天然来源的生物活性肽/蛋白质)的分离,结构和功能表征的研究,从基础科学到临床应用,还有很长的路要走。在这里,我们概述了首先从南美响尾蛇毒液中分离出来的神经毒素巴豆胺的结构和功能特性。巴豆胺是第一种被分类为天然细胞穿透和抗菌肽(CPP和AMP)的毒液肽,具有更明显的抗真菌活性。与其他已知的天然CPP和AMP相比,巴豆胺具有广泛的生物活性,具有潜在的生物技术和治疗价值。最近的研究表明,巴豆胺具有选择性的体外抗癌活性。在体内,使用鼠类黑色素瘤模型显示,巴豆胺延迟了肿瘤的植入,抑制了肿瘤细胞的增殖,并且还增加了植入皮下黑色素瘤的小鼠的存活率。还讨论了由巴豆胺衍生的最小化分子的结构和功能特性以及可能的生物技术应用。

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