Article
Pharmacology & Pharmacy
Hsing Huang, Hsiu-Chen Huang, Wei-Chung Chiou, Lie-Chwen Lin, Jui-Chieh Chen, Hui-Kang Liu, Yu-Heng Lai, Cheng Huang
Summary: Hepatitis B virus (HBV) infection causes severe liver diseases, but current therapies are unable to eradicate the virus completely. The newly identified inhibitor EP targets the entry step of HBV infection and shows potential for fighting against HBV infection by interfering with the NTCP-LHBsAg interaction.
ANTIVIRAL RESEARCH
(2021)
Article
Chemistry, Medicinal
Sheng Han, Heng Li, Weixiong Chen, Li Yang, Xiankun Tong, Jianping Zuo, Youhong Hu
Summary: In this study, a series of potent Ebola entry inhibitors were discovered, with compound 28 displaying the highest potency and remarkable selectivity. Structure-activity relationship and molecular docking analysis of the new chemical scaffold provided guidance for the design of further potent inhibitors.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Plant Sciences
Xi Xie, Shengsheng Lu, Xiaoyan Pan, Min Zou, Fangfang Li, Haixing Lin, Jianan Hu, Sheng Fan, Jian He
Summary: A new bafilomycin derivative and known bafilomycins isolated from Streptomyces sp. HTL16 showed potent antiviral activities against influenza A and SARS-CoV-2 viruses by inhibiting endosomal ATP-driven proton pumps, with IC50 values in the nanomolar range.
JOURNAL OF NATURAL PRODUCTS
(2021)
Article
Immunology
Jisu Hong, Youngjin Choi, Yoonjoo Choi, Jiwoo Lee, Hyo Jeong Hong
Summary: By conducting experiments and structural analysis, it was found that 1A8 can effectively block HBV infection of different genotypes, making it a promising candidate for the prevention and treatment of HBV infection.
Article
Biochemistry & Molecular Biology
Quanjian Li, Hongbin Yan
Summary: This work catalogued the oligonucleotide sequences and their composition based on their overall yield. It was found that sequences containing more 2'-deoxyadenosine residues and specific dinucleotide steps tend to have lower yields.
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
(2023)
Article
Biochemistry & Molecular Biology
Dongjae Lee, Jung-Ah Kang, Chanseok Lim, Sunjae Bae, Jieun Choi, Minji Park, Yong-Chul Kim, Yuri Cho, Sung-Gyoo Park, Jiwon Seo
Summary: Hepatitis B virus (HBV) infection is a serious global health issue that leads to liver cirrhosis and hepatocellular carcinoma. Developing new therapies and combining them with approved drugs is considered an effective strategy for curing HBV. In this study, a library of cyclosporin O derivatives was generated and evaluated for its inhibitory activity against HBV entry. The lead compound showed the highest potency with minimal cytotoxicity. This research provides a platform for screening other targets requiring macrocyclic chemical entities.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Liang Shao, Fan Yang, Yangqing Su, Weijia Li, Jihong Zhang, Huan Xu, Boxuan Huang, Mengsi Sun, Yu Mu, Yuan Zhang, Fei Yu
Summary: The designed and synthesized oleanolic acid (OA) trimers exhibited potent antiviral activities against influenza virus, potentially by interrupting the interaction between the virus and host cells to block viral entry. These findings suggest the utility of multivalent OA conjugates in enhancing ligand-target interactions for anti-influenza virus drug design.
ACS MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Biochemistry & Molecular Biology
Keiji Ueda, Yadarat Suwanmanee
Summary: The precise mechanism of HBV entry into cells is still largely unknown. However, researchers have identified ATP5B as an essential factor for HBV entry, which is believed to bind with myristoylated preS1 2-47. Knockdown of ATP5B in NTCP-expressing HepG2 cells reduced HBV infectivity, indicating that ATP5B is involved in the HBV entry process.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Xinlei Li, Zhaohui Xu, Bidisha Mitra, Minghang Wang, Haitao Guo, Zongdi Feng
Summary: Our study showed that culturing NTCP-reconstituted HepG2 cells in a commercial human iPSC-derived hepatocyte maintenance medium (HMM) significantly increased susceptibility to HBV infection, likely through activation of the NTCP promoter by HMM. However, even with enhanced NTCP expression by HMM, no apparent HBV spread was observed in vitro.
CELL AND BIOSCIENCE
(2021)
Article
Virology
Kamilla Toon, Mphatso D. Kalemera, Machaela Palor, Nicola J. Rose, Yasuhiro Takeuchi, Joe Grove, Giada Mattiuzzo
Summary: Due to increased and broadened screening efforts, the number of viral species in the Hepacivirus genus has rapidly expanded. Genetic features of hepaciviruses suggest they have adapted and evolved to hijack host proteins for efficient liver propagation. A study on GB virus B (GBV-B) found that claudin-1 is an essential entry factor, shared with hepatitis C virus (HCV), but with distinct mechanisms of entry. Understanding the molecular mechanisms of hepacivirus entry can inform the design of new vaccines and treatments targeting the first stage of HCV infection.
JOURNAL OF VIROLOGY
(2023)
Review
Microbiology
Jean-Francois Bruxelle, Nino Trattnig, Marianne W. Mureithi, Elise Landais, Ralph Pantophlet
Summary: This review discusses the challenges in developing effective strategies to prevent HIV-1 infection based on insights from the current model of mucosal transmission and cell entry. It examines key viral and host factors, preventive strategies using antibody-mediated protection against T/F viruses and mucosal immunity, and treatment strategies targeting viral entry with a focus on clinically advanced entry inhibitors.
Review
Immunology
Hadrien Peyret, John F. C. Steele, Jae-Wan Jung, Eva C. Thuenemann, Yulia Meshcheriakova, George P. Lomonossoff
Summary: Plant molecular farming has grown in the past 30 years as a method for producing recombinant proteins, especially in the production of vaccine candidates. Despite challenges in expressing and purifying membrane-bound proteins for enveloped viruses, there have been significant successes with promising clinical trials for plant-produced vaccine candidates against such viruses.
Article
Medicine, General & Internal
Heiner Wedemeyer, Soo Aleman, Maurizia Rossana Brunetto, Antje Blank, Pietro Andreone, Pavel Bogomolov, Vladimir Chulanov, Nina Mamonova, Natalia Geyvandova, Viacheslav Morozov, Olga Sagalova, Tatyana Stepanova, Annemarie Berger, Dmitry Manuilov, Vithika Suri, Qi An, Ben Da, John Flaherty, Anu Osinusi, Yang Liu, Uta Merle, Julian Schulze zur Wiesch, Stefan Zeuzem, Sandra Ciesek, Markus Cornberg, Pietro Lampertico
Summary: Bulevirtide treatment reduces HDV RNA and ALT levels in patients with chronic hepatitis D, with a dose-dependent effect.
NEW ENGLAND JOURNAL OF MEDICINE
(2023)
Article
Medicine, General & Internal
Heiner Wedemeyer, Soo Aleman, Maurizia Rossana Brunetto, Antje Blank, Pietro Andreone, Pavel Bogomolov, Vladimir Chulanov, Nina Mamonova, Natalia Geyvandova, Viacheslav Morozov, Olga Sagalova, Tatyana Stepanova, Annemarie Berger, Dmitry Manuilov, Vithika Suri, Qi An, Ben Da, John Flaherty, Anu Osinusi, Yang Liu, Uta Merle, Julian Schulzezur Wiesch, Stefan Zeuzem, Sandra Ciesek, Markus Cornberg, Pietro Lampertico
Summary: In this study, it was found that bulevirtide is effective in inhibiting the entry of hepatitis D virus and reducing the progression of liver disease in patients with chronic hepatitis B. The recommended dosage of bulevirtide is 2 mg or 10 mg per day.
NEW ENGLAND JOURNAL OF MEDICINE
(2023)
Article
Chemistry, Medicinal
WooChan Kim, Jung-Ah Kang, Minji Park, Pyeong-Hwa Jeong, Yoon Jun Kim, Yuri Cho, Sung-Gyoo Park, Yong-Chul Kim
Summary: Novel potent pyrimidine derivatives have been synthesized as core assembly modulators for the treatment of chronic hepatitis B virus (HBV) infection. These derivatives showed potent inhibitory effects in in vitro assays and significantly decreased serum HBV DNA levels in a human liver-chimeric uPA/SCID mouse model, particularly when combined with tenofovir.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)