Sulfamoylbenzamide-based Capsid Assembly Modulators for Selective Inhibition of Hepatitis B Viral Replication
| Autor: | Yoon-Sun Yi, Hye-Jin Kim, Hyo Jin Kang, Meehyein Kim, Jun Yeon Hwang, Ga Hyeon Kim, So Yeong Park, Sang J. Chung, Joo-Youn Lee, Ali Imran, Avinash G Vishakantegowda, Hyeon-Min Cha, Soo Bong Han, Yeon Hee Lee, Sangmi Jun |
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| Rok vydání: | 2021 |
| Předmět: |
Hepatitis B virus
Cure rate 010405 organic chemistry Organic Chemistry virus diseases Core protein Biology Selective inhibition medicine.disease_cause 01 natural sciences Biochemistry Virology digestive system diseases 0104 chemical sciences Viral Assembly 010404 medicinal & biomolecular chemistry Capsid Targeted drug delivery Drug Discovery medicine Hepatitis b viral |
| Zdroj: | ACS Med Chem Lett |
| ISSN: | 1948-5875 |
| Popis: | [Image: see text] As the spread of infections caused by hepatitis B virus (HBV) threatens public health worldwide, investigations from multiple perspectives and of various mechanisms of action are urgently required to increase the HBV cure rate. Targeting the encapsidation of the nuclear capsid protein (core protein, HBc) has emerged as an attractive strategy for inhibiting the viral assembly process; however, a drug targeting this mechanism has not yet been approved. We synthesized novel sulfamoylbenzamides (SBAs) as capsid assembly modulators of HBV and found that the effects and safety profiles of compounds 3 and 8 have potential therapeutic applicability against HBV. The formation of tubular particles was time-dependent in the presence of 3, indicating a new mode of protein assembly by SBA compounds. Our findings provide a new entity for developing safe and efficient treatments for HBV infection. |
| Databáze: | OpenAIRE |
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