4862F, a New Inhibitor of HIV-1 Protease, from the Culture of Streptomyces I03A-04862
We have isolated an extraordinary pentapeptide, called 4862F, from the culture broth of Streptomyces albosporus I03A-04862 by Diaion HP-20 macroporous adsorbent resin column, ODS-A and Sephadex LH-20 chromatography, followed by preparative HPLC. This peptide shows inhibitory activity against HIV-1 p...
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| Format: | Article |
| Language: | English |
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MDPI AG
2012-12-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/18/1/236 |
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doaj-bd5ba573c34b4a15961effe2fedb762c2020-11-25T01:51:44ZengMDPI AGMolecules1420-30492012-12-0118123624310.3390/molecules180102364862F, a New Inhibitor of HIV-1 Protease, from the Culture of Streptomyces I03A-04862Peizhen TaoWei JiangLiyan YuMinghua ChenShuoke BaiYexiang WuXiuyong FanYuqin ZhangYongzhen LiTian ZhangBiao DongMaoluo GanXiao LiuShuyi SiWe have isolated an extraordinary pentapeptide, called 4862F, from the culture broth of Streptomyces albosporus I03A-04862 by Diaion HP-20 macroporous adsorbent resin column, ODS-A and Sephadex LH-20 chromatography, followed by preparative HPLC. This peptide shows inhibitory activity against HIV-1 protease. The structure was elucidated by spectroscopic approaches, including ESI-MS and various NMR methods. Absolute configuration of the amino acid residues in 4862F was defined using Marfey’s method, and the structure was identified as N,N,N-(trimethylated)-Tyr-L-Leu-L-Val-L-Leu-(dehydrated)-His. The peptide 4862F displays inhibitory activity against HIV-1 protease, with IC50 values of 15.26 nM, using a fluorescence-based assay.http://www.mdpi.com/1420-3049/18/1/236Streptomyces albosporusstructure elucidationHIV-1 protease inhibitor |
| collection |
DOAJ |
| language |
English |
| format |
Article |
| sources |
DOAJ |
| author |
Peizhen Tao Wei Jiang Liyan Yu Minghua Chen Shuoke Bai Yexiang Wu Xiuyong Fan Yuqin Zhang Yongzhen Li Tian Zhang Biao Dong Maoluo Gan Xiao Liu Shuyi Si |
| spellingShingle |
Peizhen Tao Wei Jiang Liyan Yu Minghua Chen Shuoke Bai Yexiang Wu Xiuyong Fan Yuqin Zhang Yongzhen Li Tian Zhang Biao Dong Maoluo Gan Xiao Liu Shuyi Si 4862F, a New Inhibitor of HIV-1 Protease, from the Culture of Streptomyces I03A-04862 Molecules Streptomyces albosporus structure elucidation HIV-1 protease inhibitor |
| author_facet |
Peizhen Tao Wei Jiang Liyan Yu Minghua Chen Shuoke Bai Yexiang Wu Xiuyong Fan Yuqin Zhang Yongzhen Li Tian Zhang Biao Dong Maoluo Gan Xiao Liu Shuyi Si |
| author_sort |
Peizhen Tao |
| title |
4862F, a New Inhibitor of HIV-1 Protease, from the Culture of Streptomyces I03A-04862 |
| title_short |
4862F, a New Inhibitor of HIV-1 Protease, from the Culture of Streptomyces I03A-04862 |
| title_full |
4862F, a New Inhibitor of HIV-1 Protease, from the Culture of Streptomyces I03A-04862 |
| title_fullStr |
4862F, a New Inhibitor of HIV-1 Protease, from the Culture of Streptomyces I03A-04862 |
| title_full_unstemmed |
4862F, a New Inhibitor of HIV-1 Protease, from the Culture of Streptomyces I03A-04862 |
| title_sort |
4862f, a new inhibitor of hiv-1 protease, from the culture of streptomyces i03a-04862 |
| publisher |
MDPI AG |
| series |
Molecules |
| issn |
1420-3049 |
| publishDate |
2012-12-01 |
| description |
We have isolated an extraordinary pentapeptide, called 4862F, from the culture broth of Streptomyces albosporus I03A-04862 by Diaion HP-20 macroporous adsorbent resin column, ODS-A and Sephadex LH-20 chromatography, followed by preparative HPLC. This peptide shows inhibitory activity against HIV-1 protease. The structure was elucidated by spectroscopic approaches, including ESI-MS and various NMR methods. Absolute configuration of the amino acid residues in 4862F was defined using Marfey’s method, and the structure was identified as N,N,N-(trimethylated)-Tyr-L-Leu-L-Val-L-Leu-(dehydrated)-His. The peptide 4862F displays inhibitory activity against HIV-1 protease, with IC50 values of 15.26 nM, using a fluorescence-based assay. |
| topic |
Streptomyces albosporus structure elucidation HIV-1 protease inhibitor |
| url |
http://www.mdpi.com/1420-3049/18/1/236 |
| work_keys_str_mv |
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