Design of peptide inhibitors for furin based on the C-terminal fragment of histone H1.2
文献类型：期刊论文
| 作者 | Wang, SM; Han, JB; Wang, YF; Lu, WY; Chi, CW |
| 刊名 | ACTA BIOCHIMICA ET BIOPHYSICA SINICA
 |
| 出版日期 | 2008 |
| 卷号 | 40期号:10页码:848-854 |
| 关键词 | furin inhibitor histone H1.2 peptide synthesis |
| 通讯作者 | Chi, CW (reprint author), Tongji Univ, Inst Prot Res, Coll Life Sci & Technol, Shanghai 200092, Peoples R China.,zwqi@sibs.ac.cn |
| 英文摘要 | The mammalian proprotein convertase furin has been found to play an important role in diverse physiological and pathological events, such as the activation of viral glycoproteins and bacterial exotoxins. Small, non-toxic and highly active, furin inhibitors are considered to be attractive drug candidates for diseases caused by virus and bacteria. In this study, a series of peptide inhibitors were designed and synthesized based on the C-terminal fragment of histone H1.2, which has an inhibitory effect on furin. Replacing the reactive site of inhibitors with the consensus substrate recognition sequence of furin has been found to increase inhibitory activity greatly. The most potent inhibitor, I-4, with 14 amino acid residues has a K-i value of 17 nM for furin. Although most of the synthesized peptides were temporary inhibitors, the inhibitor I-5, with nine amino acids, retained its full potency, even after a 3 h incubation period with furin at 37 degrees C. These inhibitors may potentially lead to the development of anti-viral and antibacterial drug compounds. |
| 学科主题 | Biochemistry & Molecular Biology; Biophysics |
| 类目[WOS] | Biochemistry & Molecular Biology ; Biophysics |
| 关键词[WOS] | BEAN TRYPSIN-INHIBITOR ; PROPROTEIN CONVERTASES ; PROHORMONE CONVERTASES ; D-ARGININE ; IN-SITU ; EGLIN-C ; POTENT ; ACTIVATION ; PROTEASE ; IDENTIFICATION |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000260131100002 |
| 版本 | 出版稿 |
| 源URL | [http://202.127.25.143/handle/331003/1440]  |
| 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 | Wang, SM,Han, JB,Wang, YF,et al. Design of peptide inhibitors for furin based on the C-terminal fragment of histone H1.2[J]. ACTA BIOCHIMICA ET BIOPHYSICA SINICA,2008,40(10):848-854. |
| APA | Wang, SM,Han, JB,Wang, YF,Lu, WY,&Chi, CW.(2008).Design of peptide inhibitors for furin based on the C-terminal fragment of histone H1.2.ACTA BIOCHIMICA ET BIOPHYSICA SINICA,40(10),848-854. |
| MLA | Wang, SM,et al."Design of peptide inhibitors for furin based on the C-terminal fragment of histone H1.2".ACTA BIOCHIMICA ET BIOPHYSICA SINICA 40.10(2008):848-854. |
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