| Title | Potent and Specific Inhibition of NTCP-Mediated HBV/HDV Infection and Substrate Transporting by a Novel, Oral-Available Cyclosporine A Analogue |
| Authors | Liu, Yang Ruan, Hanying Li, Ying Sun, Guoliang Liu, Xiao He, Wenhui Mao, Fengfeng He, Miaomiao Yan, Liwei Zhong, Guocai Yan, Huan Li, Wenhui Zhang, Zhiyuan |
| Affiliation | Natl Inst Biol Sci, Beijing 102206, Peoples R China Tsinghua Univ, Grad Program, Beijing 100084, Peoples R China Peking Univ, Grad Program, Beijing 100080, Peoples R China Chinese Acad Med Sci & Peking Union Med Coll, Grad Program, Beijing 100005, Peoples R China |
| Keywords | COTRANSPORTING POLYPEPTIDE NTCP BILE-ACID TRANSPORTER B-VIRUS INFECTION HEPATITIS-B MOLECULAR DETERMINANTS ENTRY MECHANISM DRUGS |
| Issue Date | 14-Jan-2021 |
| Publisher | JOURNAL OF MEDICINAL CHEMISTRY |
| Abstract | Analogues of the natural product cyclosporine A (CsA) were developed and assessed as antivirals against infection of hepatitis B virus (HBV) and its satellite hepatitis D virus (HDV). An analogue termed 27A exhibits potent inhibition of HBV/HDV infection by specifically blocking viral engagement to its cellular receptor NTCP, while it lacks immunosuppressive activity found in natural CsA. Intraperitoneal injection or oral intake of 27A protects HDV-susceptible mouse model from HDV infection. 27A serves as a promising lead for the development of novel anti-HDV/HBV agents. |
| URI | http://hdl.handle.net/20.500.11897/604352 |
| ISSN | 0022-2623 |
| DOI | 10.1021/acs.jmedchem.0c01434 |
| Indexed | SCI(E) |
| Appears in Collections: | 待认领 |
