Department of Medicinal Chemistry, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, 2-3-10 Kandasurugadai, Chiyoda-ku, Tokyo 101-0062, Japan.
J Med Chem. 2010 Jul 22;53(14):5356-60. doi: 10.1021/jm1003528.
Anti-HIV peptides with inhibitory activity against HIV-1 integrase (IN) have been found in overlapping peptide libraries derived from HIV-1 gene products. In a strand transfer assay using IN, inhibitory active peptides with certain sequential motifs related to Vpr- and Env-derived peptides were found. The addition of an octa-arginyl group to the inhibitory peptides caused a remarkable inhibition of the strand transfer and 3'-end-processing reactions catalyzed by IN and significant inhibition against HIV replication.
已在源自 HIV-1 基因产物的重叠肽文库中发现具有抗 HIV-1 整合酶 (IN) 抑制活性的抗 HIV 肽。在使用 IN 的链转移测定中,发现了具有与 Vpr 和 Env 衍生肽相关的特定序列基序的抑制活性肽。将八精氨酸基团添加到抑制性肽中,导致 IN 催化的链转移和 3'-末端加工反应显著抑制,并且对 HIV 复制具有显著抑制作用。