2015
DOI: 10.1039/c4md00521j
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Non-nucleoside anti-HBV agents: advances in structural optimization and mechanism of action investigations

Abstract: In this review, we focus on the recent advances in discovery, structural modifications and biological activities studies of several distinct classes of synthetic non-nucleoside small molecular compounds with new mechanisms.

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Cited by 14 publications
(7 citation statements)
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“…In vivo, the HBV capsid assembly process is facilitated by the pgRNA, which acts as a scaffold to bring the capsid subunits together . Surprisingly, in vitro, capsid assembly has also been observed in the absence of pgRNA upon modulation of the experimental conditions. , However, for full-length Cp183 without any artificial truncation at the C-terminus, in vitro capsid assembly can be successfully and efficiently induced by polyanions, including poly­(glutamic acid), dextran sulfate, oligonucleotides, and nonbiological polymers. , In the absence of RNA, antiviral molecules such as heteroaryldihydropyrimidines (HAPs) have been found to accelerate capsid assembly. Binding of HAPs to capsid proteins does not alter the morphology of the protein but does enhance the interdimer contact energy. The first step in capsid assembly is the formation of a nucleus consisting of a trimer of dimers (Figure b) .…”
Section: Introductionmentioning
confidence: 99%
“…In vivo, the HBV capsid assembly process is facilitated by the pgRNA, which acts as a scaffold to bring the capsid subunits together . Surprisingly, in vitro, capsid assembly has also been observed in the absence of pgRNA upon modulation of the experimental conditions. , However, for full-length Cp183 without any artificial truncation at the C-terminus, in vitro capsid assembly can be successfully and efficiently induced by polyanions, including poly­(glutamic acid), dextran sulfate, oligonucleotides, and nonbiological polymers. , In the absence of RNA, antiviral molecules such as heteroaryldihydropyrimidines (HAPs) have been found to accelerate capsid assembly. Binding of HAPs to capsid proteins does not alter the morphology of the protein but does enhance the interdimer contact energy. The first step in capsid assembly is the formation of a nucleus consisting of a trimer of dimers (Figure b) .…”
Section: Introductionmentioning
confidence: 99%
“…In the present study, a pharmacophore model was developed and validated by 34 active inhibitors of HBsAg secretion. The complete information about the inhibitors is reviewed by Liu et al [28]. Nine compounds having 6-chloro-4-(2-chlorophenyl) quinolone residues were clustered into the training set based on their structural relationship and validated by the rest of the compounds as the test set.…”
Section: Discussionmentioning
confidence: 99%
“…Chronic hepatitis B (CHB), which is caused by hepatitis B virus (HBV), is a major health problem affecting approximately 260 million patients globally. CHB is the major cause of chronic liver diseases and hepatocellular carcinoma. , Existing therapies for CHB include interferon alpha and several nucleoside/nucleotide analogs. , However, existing treatment regimens cannot functionally cure HBV, and most patients require further treatment. Because of effective vaccination campaigns, the prevalence of HBV in children has been reduced to 1.3%. However, the initial birth dose vaccination is only 39%, indicating that a large population remains at risk for HBV infection…”
mentioning
confidence: 99%
“…1,2 Existing therapies for CHB include interferon alpha and several nucleoside/nucleotide analogs. 3,4 However, existing treatment regimens cannot functionally cure HBV, and most patients require further treatment. 5−7 Because of effective vaccination campaigns, the prevalence of HBV in children has been reduced to 1.3%.…”
mentioning
confidence: 99%