Ramnarine Emabelle J, Devico Anthony L, Vigil-Cruz Sandra C
Department of Pharmaceutical Sciences, University of Connecticut, 69 North Eagleville Road, Storrs, CT 06269, USA.
Bioorg Med Chem Lett. 2006 Jan 1;16(1):93-5. doi: 10.1016/j.bmcl.2005.09.044. Epub 2005 Oct 19.
A series of synthetic peptide fragments derived from RANTES were designed, synthesized, and evaluated to determine the effect of N-terminal truncation on the ability of the lead compound Ac[Ala(10,11)]RANTES-(1-14)NH(2) to inhibit HIV-1 infectivity. Both the lead compound and the truncated analogue Ac[Ala(10,11)]RANTES-(3-14)NH(2) were able to significantly inhibit HIV-1 infectivity. These results suggest that a small synthetic peptide may be able to mimic RANTES and have the ability to prevent transmission of HIV-1.
设计、合成并评估了一系列源自RANTES的合成肽片段,以确定N端截短对先导化合物Ac[Ala(10,11)]RANTES-(1-14)NH₂抑制HIV-1感染性能力的影响。先导化合物和截短类似物Ac[Ala(10,11)]RANTES-(3-14)NH₂均能够显著抑制HIV-1感染性。这些结果表明,一种小的合成肽可能能够模拟RANTES并具有预防HIV-1传播的能力。