A prodrug of the capsid assembly modulator improved druggability and lowing HBsAg and HBeAg for the treatment of chronic hepatitis B
文献类型：期刊论文
| 作者 | Chen, Wuhong2; Gong, Ying3,4; Long, Guozhang2,4; Wang, Xinran1,3; Yang, Yurong1,2; Liu, Jia2,5 ; Li, Heng3,4; Tong, Xiankun3; Zhao, Qiliang2,4; Yang, Li3
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 2023-09-05 |
| 卷号 | 257页码:8 |
| 关键词 | HBV Capsid assembly modulators Prodrug Hepatitis B surface antigen |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2023.115485 |
| 通讯作者 | Yang, Li(yangli@simm.ac.cn) ; Zuo, Jianping(jpzuo@simm.ac.cn) ; Hu, Youhong(yhhu@simm.ac.cn) |
| 英文摘要 | CAMs were disclosed to alter cccDNA levels with sustained hepatitis B surface antigen (HBsAg) loss or sero-conversion in preclinical investigation. Here, we report the discovery of a prodrug Yhhu6669 as CAMs based on the intestinal peptide transporter. This compound exhibited the promising anti-HBV activity with sustained suppression of HBV DNA, as well as HBsAg and HBeAg in the AAV HBV mouse model by oral treatment for 7 weeks and maintained for a further 8 weeks following drug withdraw. Our results show an alternative possibility for a functional cure by specific CAMs and provide the basis for the further mechanism study. |
| WOS关键词 | VIRUS INFECTION ; RO7049389 ; DRUG |
| 资助项目 | National Natural Science Foundation of China[81872725] ; National Natural Science Foundation of China[82104240] ; Shanghai Sci- ence and Technology Innovation Project[20S11906200] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001007121800001 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/306209]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Yang, Li; Zuo, Jianping; Hu, Youhong |
| 作者单位 | 1.Nanjing Univ Chinese Med, Coll Pharm, Sch Chinese Mat Med, 138 Xianlin Rd, Nanjing 210023, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zu ChongZhi Rd, Shanghai 201203, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Lab Immunopharmacol, 555 Zu ChongZhi Rd, Shanghai 201203, Peoples R China 4.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China 5.Univ Chinese Acad Sci, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, 1st Xiangshan Branch Alley, Hangzhou 310024, Peoples R China |
| 推荐引用方式 GB/T 7714 | Chen, Wuhong,Gong, Ying,Long, Guozhang,et al. A prodrug of the capsid assembly modulator improved druggability and lowing HBsAg and HBeAg for the treatment of chronic hepatitis B[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2023,257:8. |
| APA | Chen, Wuhong.,Gong, Ying.,Long, Guozhang.,Wang, Xinran.,Yang, Yurong.,...&Hu, Youhong.(2023).A prodrug of the capsid assembly modulator improved druggability and lowing HBsAg and HBeAg for the treatment of chronic hepatitis B.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,257,8. |
| MLA | Chen, Wuhong,et al."A prodrug of the capsid assembly modulator improved druggability and lowing HBsAg and HBeAg for the treatment of chronic hepatitis B".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 257(2023):8. |
入库方式： OAI收割
来源：上海药物研究所
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