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IsCT-based analogs intending better biological activity.
Journal of Peptide Science ( IF 1.8 ) Pub Date : 2019-10-22 , DOI: 10.1002/psc.3219
Isabel Cristina Chica Acevedo 1 , Pedro Ismael Silva 2 , Fernanda Dias Silva 1 , Iris Araújo 1 , Flávio Lopes Alves 1, 3 , Cyntia Silva Oliveira 3 , Vani Xavier Oliveira 1, 3
Affiliation  

IsCT1‐NH2 is a cationic antimicrobial peptide isolated from the venom of the scorpion Opisthacanthus madagascariensis that has a tendency to form an α‐helical structure and shows potent antimicrobial activity and also inopportunely shows hemolytic effects. In this study, five IsCT1 (ILGKIWEGIKSLF)‐based analogs with amino acid modifications at positions 1, 3, 5, or 8 and one analog with three simultaneous substitutions at the 1, 5, and 8 positions were designed. The net charge of each analog was between +2 and +3. The peptides obtained were characterized by mass spectrometry and analyzed by circular dichroism for their structure in different media. Studies of antimicrobial activity, hemolytic activity, and stability against proteases were also carried out.

中文翻译:

基于IsCT的类似物具有更好的生物活性。

IsCT1-NH 2是一种阳离子抗微生物肽,是从马达加斯加蝎(Opishacanthus madagascariensis)的毒液中分离出来的,具有形成α-螺旋结构的趋势,并显示出强效的抗菌活性,并且不适当地显示出溶血作用。在这项研究中,设计了5种基于IsCT1(ILGKIWEGIKSLF)的类似物,这些类似物在1、3、5或8位具有氨基酸修饰,并且设计了一种在1、5和8位具有3个同时取代的类似物。每个类似物的净电荷在+2到+3之间。通过质谱法对获得的肽进行表征,并通过圆二色性分析其在不同介质中的结构。还进行了抗菌活性,溶血活性和对蛋白酶的稳定性研究。
更新日期:2019-10-22
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