Stronger anti-HIV-1 activity of C-peptide derived from HIV-189.6 gp41 C-terminal heptad repeated sequence
Stronger anti-HIV-1 activity of C-peptide derived from HIV-189.6 gp41 C-terminal heptad repeated sequence
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DOI：
10.1016/j.peptides.2005.04.006
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发表时间：
2005-11-01
期刊：
影响因子：
3
通讯作者：
Lee, MK
中科院分区：
文献类型：
--
作者：
Seo, JK;Kim, HK;Lee, MK
含有HIV-I-LA 1 gp 41胞外域的氨基酸118至151的C34-LAI显示出有效的抗HIV-1活性。然而，根据HIV-1毒株，C34肽的N-末端半部分比C-末端半部分变化更大。因此，对来源于各种HIV-1毒株的C34肽的抗HIV-1活性进行了分析。在所测试的C34肽中，C34-89.6表现出最强的抗HIV-1活性。有趣的是，它的N-末端的一半比其他C34肽的酸性更强，而它的C-末端的一半更碱性。由于来源于HIV-1（LAI）株的C肽被广泛使用，因此在HIV-1株89.6和LAI之间比较了这些肽的抗HIV-1活性。当使用嵌合肽时，发现C34-89.6的C-末端碱性区域比其N-末端碱性区域更关键。T20-89.6和C28-89.6的抗HIV-1活性也分别强于T20-LAI和C28-LAI。将C28-89.6的C-末端碱性残基替换为C28-LAI的相应残基后，其抗HIV-1活性减弱。然而，没有发现构象差异之间的C28肽。因此，这些结果意味着，引入HIV-1（89.6）C肽的C末端碱性残基可用于开发有效的抗HIV-1药物。(c)2005年爱思唯尔公司All rights reserved.
C34-LAI containing amino acids 118 to 151 of the HIV-I-LA1 gp41 ectodomain exhibits potent anti-HIV-1 activity. However, the N-terminal halves of C34 peptides vary more according to the HIV-1 strain than the C-terminal halves. Therefore, an analysis was conducted on the anti-HIV-1 activities of the C34 peptides derived from various HIV-1 strains. C34-89.6 exhibited the strongest anti-HIV-1 activity among the C34 peptides tested. Interestingly, its N-terminal half was more acidic than those of the other C34 peptides, whereas its C-terminal half was more basic. Since the C-peptides derived from the HIV-1(LAI) strain are used extensively, the anti-HIV-1 activities of these peptides were compared between the HIV-1 strains 89.6 and LAI. When using chimeric peptides, it was found that the C-terminal basic region of C34-89.6 was more critical than its N-terminal basic region. The anti-HIV-1 activity of T20-89.6 and C28-89.6 was also stronger than that of T20-LAI and C28-LAI, respectively. The anti-HIV-1 activity of C28-89.6 was weakened when the C-terminal basic residues were changed to the corresponding residues of C28-LAI. However, no conformational differences were found among the C28 peptides. Accordingly, these results imply that introducing the C-terminal basic residues of the HIV-1(89.6) C-peptide may be useful for developing potent anti-HIV-1 drugs. (c) 2005 Elsevier Inc. All rights reserved.