Human immunodeficiency virus (HIV) causes acquired immune deficiency syndrome (AIDS) where the immune system progressively deteriorates and consequently threatens life. The peptide Kn2-7, a modified version of scorpion venom non-disulphide peptide, possesses the highest anti-HIV activity inhibiting antiviral potencies of 13 HIV-1 strains. In the present study, we achieved a new synthesis of Kn2-7 through a commercially viable, scalable, and impurity-free approach using Tagging Technique. We used (2,4-bis(octadecyloxy)phenyl)methanol as the Tag support for the synthesis and couplings were achieved by COMU with Fmoc-protected amino acids. The method is highly advantageous over conventional SPPS or LPPS methods in terms of economy, time, and most importantly purification. The peptide Kn2-7 and the intermediates were isolated as pure solids, the structures of which were unequivocally confirmed by H NMR, C NMR, and Mass spectroscopy.

中文翻译：

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合成抗 HIV 肽 Kn2-7 的便捷途径：TAG 方法


人类免疫缺陷病毒（HIV）会导致获得性免疫缺陷综合症（艾滋病），使免疫系统逐渐恶化，从而威胁生命。肽Kn2-7是蝎毒非二硫肽的改良版本，在13种HIV-1毒株中具有最高的抗HIV活性和抑制抗病毒效力。在本研究中，我们使用标记技术通过商业上可行的、可扩展的且无杂质的方法实现了 Kn2-7 的新合成。我们使用（2,4-双（十八烷氧基）苯基）甲醇作为合成的标签支持物，并通过 COMU 与 Fmoc 保护的氨基酸实现偶联。该方法在经济、时间和最重要的纯化方面比传统的 SPPS 或 LPPS 方法具有很大的优势。肽Kn2-7和中间体被分离为纯固体，其结构通过1H NMR、13C NMR和质谱明确证实。