The potent inhibitory activity of histone H1.2 C-terminal fragments on furin
文献类型：期刊论文
| 作者 | Han, JB; Zhang, L; Shao, XX; Shi, JH; Chi, CW |
| 刊名 | FEBS JOURNAL
 |
| 出版日期 | 2006 |
| 卷号 | 273期号:19页码:4459-4469 |
| 关键词 | furin gene expression histone H1 inhibitory activity limited proteolysis peptide synthesis |
| 通讯作者 | Chi, CW (reprint author), Chinese Acad Sci, Shanghai Inst Biochem & Cell Biol, Grad Sch, 320 Yue Yang Rd, Shanghai 200031, Peoples R China.,chi@sunm.shcnc.ac.cn |
| 英文摘要 | Many physiologically important proproteins, pathogenic bacterial exotoxins and viral envelope glycoproteins are activated by the proprotein convertase furin, which makes furin inhibitor a hot target for basic research and drug design. Although synthetic and bioengineered inhibitors of furin have been well characterized, its endogenous inhibitor has not been directly purified from mammalian tissues to date. In this study, three inhibitors were purified from the porcine liver by using a combination of chromatographic techniques, and identified to be the C-terminal truncated fragments with different sizes of histone H1.2. The gene of porcine histone H1.2 was cloned and sequenced, further confirming the determined sequences. These three C-terminal fragments inhibited furin with K-i values around 2 x 10(-7) M while the full-length histone H1.2 inhibited it with a lesser activity, suggesting that the inhibitory activity relies on the C-terminal lysine-rich domain. Though the inhibition was temporary, these inhibitors were specific, and the reactive site of one C-terminal fragment was identified. A 36 amino acid peptide around the reactive site was synthesized, which could still inhibit furin with a K-i of 5.2 x 10(-7) M. |
| 学科主题 | Biochemistry & Molecular Biology |
| 类目[WOS] | Biochemistry & Molecular Biology |
| 关键词[WOS] | NEUROENDOCRINE POLYPEPTIDE 7B2 ; PROHORMONE CONVERTASE PC2 ; PROPROTEIN CONVERTASE ; CELL-SURFACE ; D-ARGININE ; PROTEINS ; ACTIVATION ; IDENTIFICATION ; PEPTIDES ; CLEAVAGE |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000240558500010 |
| 版本 | 出版稿 |
| 源URL | [http://202.127.25.143/handle/331003/1793]  |
| 专题 | 上海生化细胞研究所_上海生科院生化细胞研究所 |
| 推荐引用方式 GB/T 7714 | Han, JB,Zhang, L,Shao, XX,et al. The potent inhibitory activity of histone H1.2 C-terminal fragments on furin[J]. FEBS JOURNAL,2006,273(19):4459-4469. |
| APA | Han, JB,Zhang, L,Shao, XX,Shi, JH,&Chi, CW.(2006).The potent inhibitory activity of histone H1.2 C-terminal fragments on furin.FEBS JOURNAL,273(19),4459-4469. |
| MLA | Han, JB,et al."The potent inhibitory activity of histone H1.2 C-terminal fragments on furin".FEBS JOURNAL 273.19(2006):4459-4469. |
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