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将胆固醇分子通过1个半胱氨酸侧链硫醚键和1个β-丙氨酸连接臂引入到所设计的非天然HR序列抗HIV融合活性多肽的C端和N端,合成了与天然C肽序列同源性很低的非天然序列的类肽抗HIV融合分子,以考察胆固醇修饰对非天然HR序列活性的影响,探讨克服耐药性的新思路.生物活性评价结果表明,胆固醇与HR肽C端结合物抑制HIV融合活性显著提高,而连接到N端的序列则完全失去了抗病毒活性,表明所设计的非天然序列确实具有与天然序列类似的作用机制.
The cholesterol molecule was introduced into the C-terminal and N-terminal of the designed non-natural HR sequence anti-HIV fusion active polypeptide through one cysteine side chain thioether bond and one β-alanine linker to synthesize the natural C peptide sequence homology of non-natural peptide-like anti-HIV fusion molecules in order to investigate the impact of cholesterol modification on non-natural HR sequence activity to explore new ideas to overcome drug resistance biological activity evaluation results show that cholesterol and The HR peptide C-terminal conjugate inhibited HIV fusion activity significantly, while the sequence linked to the N terminus completely lost its antiviral activity, suggesting that the designed non-native sequence does have a similar mechanism of action to the native sequence.