Potent and Specific Inhibition of NTCP-Mediated HBV/HDV Infection and Substrate Transporting by a Novel, Oral-Available Cyclosporine A Analogue,Journal of Medicinal Chemistry

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Potent and Specific Inhibition of NTCP-Mediated HBV/HDV Infection and Substrate Transporting by a Novel, Oral-Available Cyclosporine A Analogue
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-12-28 , DOI: 10.1021/acs.jmedchem.0c01484
Yang Liu _{1,

2} , Hanying Ruan ₁ , Ying Li ₁ , Guoliang Sun _{1,

3} , Xiao Liu ₁ , Wenhui He ₁ , Fengfeng Mao ₁ , Miaomiao He _{1,

4} , Liwei Yan ₁ , Guocai Zhong ₁ , Huan Yan ₁ , Wenhui Li ₁ , Zhiyuan Zhang ₁

Affiliation

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.

中文翻译：

NTCP介导的HBV / HDV感染和底物的新型，口服可用环孢菌素A类似物的有效和特异性抑制。

开发了天然产物环孢菌素A（CsA）的类似物，并将其评估为抗乙型肝炎病毒（HBV）及其附属的D型肝炎病毒（HDV）感染的抗病毒药。称为27A的类似物通过特异性阻断病毒与其细胞受体NTCP的结合，从而有效抑制HBV / HDV感染，而它缺乏天然CsA中的免疫抑制活性。腹腔注射或口服27A可以保护HDV易感小鼠模型免受HDV感染。27A是开发新型抗HDV / HBV药物的有希望的先导。

更新日期：2021-01-14

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