TitlePotent and Specific Inhibition of NTCP-Mediated HBV/HDV Infection and Substrate Transporting by a Novel, Oral-Available Cyclosporine A Analogue
AuthorsLiu, 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
AffiliationNatl 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
KeywordsCOTRANSPORTING POLYPEPTIDE NTCP
BILE-ACID TRANSPORTER
B-VIRUS INFECTION
HEPATITIS-B
MOLECULAR DETERMINANTS
ENTRY
MECHANISM
DRUGS
Issue Date14-Jan-2021
PublisherJOURNAL OF MEDICINAL CHEMISTRY
AbstractAnalogues 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.
URIhttp://hdl.handle.net/20.500.11897/604352
ISSN0022-2623
DOI10.1021/acs.jmedchem.0c01434
IndexedSCI(E)
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