Novel N-Peptides HIV-1 Fusion Inhibitors with Hydrophobic and Salt-Bridges Mutations

来源 :第十三届中国国际多肽大会 | 被引量 : 0次 | 上传用户：xxcdejingcai

【摘要】

：

　　Peptides derived from HIV-1 gp41 N-terminal heptad repeat(NHR)region(N-peptide)are weak fusion inhibitors due to their tendency to aggregate instead of form

【作者】

：

Baohua Zheng Huihui Chong Deqiang Cao Xifeng Jiang Xiaoyu Xu Guiying Zhang Yuxian He Maosheng Cheng Keliang Liu Lifeng Cai

【机构】

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DepartmentofMedicinalChemistry,BeijingInstituteofPharmacology&Toxicology,Beijing,100850,China;KeyLab

【出处】

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第十三届中国国际多肽大会

【发表日期】

：

2014年6期

【关键词】

：

HIV-1 gp41 fusion inhibitor N-peptide NHR coiled-coil

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　　Peptides derived from HIV-1 gp41 N-terminal heptad repeat(NHR)region(N-peptide)are weak fusion inhibitors due to their tendency to aggregate instead of forming active trimer.We introduced hydrophobic mutations and salt-bridge to stabilize the trimerized N-peptide coiled-coil structure and improve the solubility of the N-peptide.The salt-bridge modified N-peptide LKC142 showed significantly improved inhibitory potency against virus-cell membrane fusion and target binding ability with CHR.Its IC50 was 30 folders lower than the native N-peptide N38MC against T20 sensitive or T20-resistant strains.

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Novel N-Peptides HIV-1 Fusion Inhibitors with Hydrophobic and Salt-Bridges Mutations

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