Critical Effect of Peptide Cyclization on the Potency of Peptide Inhibitors against Dengue Virus NS2B-NS3 Protease
文献类型：期刊论文
| 作者 | Xu, SQ; Li, H; Shao, XX; Fan, CX; Ericksen, B; Liu, JS; Chi, CW; Wang, CG |
| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2012 |
| 卷号 | 55期号:15页码:6881-6887 |
| 通讯作者 | Chi, CW (reprint author), Tongji Univ, Inst Prot Res, Shanghai 200092, Peoples R China.,zwqi@sibs.ac.cn ; chunguangwang@tongji.edu.cn |
| 英文摘要 | Dengue virus (DENY) infection is a serious public health threat worldwide that demands effective treatment. In the search for potent virus protease inhibitors, several cone snail venoms were screened against serotype 2 DENV NS2B-NS3 protease, and one conotoxin, MrIA, was identified to have inhibitory activity. The inhibitory activity was attributed to a disulfide bond-mediated loop, from which rational optimization was made to improve the potency and stability. An eight-residue cyclic peptide inhibitor was finally obtained with high potency (inhibitory constant 2.2 mu M), stability, and cell permeability. This inhibitor can thus serve as a good lead for DENY drug development. In addition, this work highlights the critical effect of peptide cyclization on the potency of oligopeptide inhibitors against DENY protease, which may advance the design of peptide inhibitors for homologous virus proteases. |
| 学科主题 | Pharmacology & Pharmacy |
| 类目[WOS] | Chemistry, Medicinal |
| 关键词[WOS] | NOREPINEPHRINE TRANSPORTER ; NS3 PROTEASE ; CYSTEINE ; CONFORMATION ; CONOPEPTIDES ; STRATEGIES ; DISCOVERY ; MRIA |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000307264100020 |
| 版本 | 出版稿 |
| 源URL | [http://202.127.25.143/handle/331003/674]  |
| 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 | Xu, SQ,Li, H,Shao, XX,et al. Critical Effect of Peptide Cyclization on the Potency of Peptide Inhibitors against Dengue Virus NS2B-NS3 Protease[J]. JOURNAL OF MEDICINAL CHEMISTRY,2012,55(15):6881-6887. |
| APA | Xu, SQ.,Li, H.,Shao, XX.,Fan, CX.,Ericksen, B.,...&Wang, CG.(2012).Critical Effect of Peptide Cyclization on the Potency of Peptide Inhibitors against Dengue Virus NS2B-NS3 Protease.JOURNAL OF MEDICINAL CHEMISTRY,55(15),6881-6887. |
| MLA | Xu, SQ,et al."Critical Effect of Peptide Cyclization on the Potency of Peptide Inhibitors against Dengue Virus NS2B-NS3 Protease".JOURNAL OF MEDICINAL CHEMISTRY 55.15(2012):6881-6887. |
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