评估新霉素类似物对 HIV-1 RRE RNA 的识别能力，发现了增强活性的简化新霉素类似物。
Evaluation of neomycin analogues for HIV-1 RRE RNA recognition identifies enhanced activity simplified neamine analogues.
机构信息
Manchester Institute of Biotechnology and School of Chemistry, The University of Manchester, Manchester M1 7DN, UK.
Division of Biochemistry, Glaxo Wellcome, Research Triangle Park, North Carolina, 27709, USA.
出版信息
Bioorg Med Chem Lett. 2019 Jan 15;29(2):339-341. doi: 10.1016/j.bmcl.2018.11.004. Epub 2018 Nov 9.
Synthetic neamine mimetics have been evaluated for binding to the HIV-1 Rev response element. Modified neamine derivatives, obtained from reductive amination of neamine, led to identification of new 6-amino modified neamine-type ligands with HIV-1 RRE binding affinity up to 20× that of neamine and up to 6× that of the more complex neomycin itself. This provides a noteworthy structure-activity increase and a useful lead to simplified, chemically accessible mimetics.
人工合成的新霉胺类似物已被评估用于与 HIV-1 Rev 反应元件结合。通过对新霉胺进行还原胺化得到的新霉胺衍生物，鉴定出了新的 6-氨基修饰的新霉胺型配体，其对 HIV-1 RRE 的结合亲和力比新霉胺高 20 倍，比更复杂的新霉素高 6 倍。这提供了显著的结构活性增加，为简化、化学可及的类似物提供了有用的先导。
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