Cell-Penetrating, Dimeric α-Helical Peptides: Nanomolar Inhibitors of HIV-1 Transcription
Cell-Penetrating, Dimeric α-Helical Peptides: Nanomolar Inhibitors of HIV-1 Transcription
复制标题
DOI：
10.1002/anie.201404684
复制
发表时间：
2014-09-15
影响因子：
16.6
通讯作者：
Yu, Jaehoon
中科院分区：
文献类型：
--
作者：
Jang, Sangmok;Hyun, Soonsil;Yu, Jaehoon
我们构建了基于亮氨酸（L）和赖氨酸（K）残基的二聚体α-螺旋肽束，用于有效的细胞穿透和抑制Tat-TAR相互作用。LK二聚体可以几乎定量地渗透到真核细胞中，并在低纳摩尔浓度下有效地抑制TAR转录物的延伸。对HIV-1复制的有效抑制强烈表明LK二聚体具有作为抗HIV-1药物的强大潜力。
We constructed dimeric alpha-helical peptide bundles based on leucine (L) and lysine (K) residues for both efficient cell penetration and inhibition of the Tat-TAR interaction. The LK dimers can penetrate nearly quantitatively into eukaryotic cells and effectively inhibit the elongation of the TAR transcript at low nanomolar concentrations. The effective inhibition of HIV-1 replication strongly suggests that the LK dimer has strong potential as an anti-HIV-1 drug.