Synthesis and HIV-1 integrase inhibitory activity of dimeric and tetrameric analogs of indolicidin
文献类型：期刊论文
| 作者 | Krajewski, K; Marchand, C; Long, YQ; Pommier, Y; Roller, PP |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2004-11-15 |
| 卷号 | 14期号:22页码:5595-5598 |
| 关键词 | indolicidin integrase inhibitors multimeric peptides |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2004.08.061 |
| 文献子类 | Article |
| 英文摘要 | We found that indolicidin, a natural antimicrobial peptide, has HIV-1 integrase inhibitory activity. Subsequently, we also discovered analogs of indolicidin with substantially higher inhibitory potency. The dimers and tetramers of the most active sequence (ILPWKWPWWPWPP) were prepared by connection of the monomers' C-terminal ends, using lysine as a linker. The inhibitory potency of the dimeric peptide is higher than the monomeric peptide. The tetrameric peptide, prepared by connection of two dimers at C-ends using again lysine as the linker, is the most potent integrase inhibitor with IC50 value of 0.6 muM for both 3'-end processing and strand transfer. (C) 2004 Elsevier Ltd. All rights reserved. |
| WOS关键词 | PEPTIDE ; PROTEIN ; CELLS |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000224715300028 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273992]  |
| 专题 | 新药研究国家重点实验室 中科院受体结构与功能重点实验室 |
| 通讯作者 | Roller, PP |
| 作者单位 | 1.NCI, CCR, Med Chem Lab, NIH, Ft Detrick, MD 21702 USA 2.NCI, Mol Pharmacol Lab, CCR, NIH, Bethesda, MD 20892 USA 3.Chinese Acad Sci, SIMM, SIBS, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Krajewski, K,Marchand, C,Long, YQ,et al. Synthesis and HIV-1 integrase inhibitory activity of dimeric and tetrameric analogs of indolicidin[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2004,14(22):5595-5598. |
| APA | Krajewski, K,Marchand, C,Long, YQ,Pommier, Y,&Roller, PP.(2004).Synthesis and HIV-1 integrase inhibitory activity of dimeric and tetrameric analogs of indolicidin.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,14(22),5595-5598. |
| MLA | Krajewski, K,et al."Synthesis and HIV-1 integrase inhibitory activity of dimeric and tetrameric analogs of indolicidin".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 14.22(2004):5595-5598. |
入库方式： OAI收割
来源：上海药物研究所
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