Evidence map›Paper›PMID 31241178›Full record

ArticleJournal of medical virology2019

Study on the structure optimization and anti-hepatitis B virus activity of novel human La protein inhibitor HBSC11.

Shuangmei Tong, Jiaqian Pan, Jing Tang

Open access · hybridAbstract read
In one paragraph

Article in Journal of medical virology, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
0.6field-weighted citation impact, top 29% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

3 citing papers in PubMed, 8 citations in OpenAlex.

  1. Bioactive compounds fromIn silico pharmacology · 2024
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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

3 authors at 1 institution in 1 country.

Shuangmei TongDepartment of Pharmacy, The Obstetrics & Gynecology Hospital of Fudan University, Shanghai, China.
Jiaqian PanDepartment of Pharmacy, The Obstetrics & Gynecology Hospital of Fudan University, Shanghai, China.
Jing TangDepartment of Pharmacy, The Obstetrics & Gynecology Hospital of Fudan University, Shanghai, China.ORCID 0000-0003-3100-1842
Obstetrics and Gynecology Hospital of Fudan University · CN

Funding

Biomedical innovation fund project of Chinese Pharmaceutical association & Yi Ling LTD. GL-B03-20180298Natural Science Foundation of China 81470852Shanghai Key Specialty Project of Clinical Pharmacy AB83110002017005
6 · The paper itself

Abstract

In our previous study, Methyl pyrazolo[1,5-a] pyridine-2-carboxylate (HBSC11) was shown to combine with La protein, which conferred anti-hepatitis B virus (HBV) effects. The purpose of this study was to optimize, synthesize, and evaluate the anti-HBV activity of HBSC11. The methyl group of HBSC11 was substituted with hydrophobic, hydrophilic, and tricyclic groups to generate novel HBV inhibitors with desirable potency. On in vitro evaluation, several derivatives exhibited good anti-HBV activity compared with control. In particular, compound 5a reduced the level of HBV antigen by approximately 50%, which was similar to the activity of entecavir. In a mouse model, 5a showed 98.9% inhibition rate for HBV DNA, 57.4% for HBsAg, and 46.4% for HBeAg; the corresponding rates in the control group were 90.8, 3.8, and 9.8%, respectively. In addition, prediction of binding modes and physicochemical properties showed that 5a formed hydrogen bonds with La protein and conformed well to the Lipinski's rule of five. Our results suggest that 5a is a potential new anti-HBV drug.

Indexed as

Antiviral AgentsCell LineGene Expression RegulationHepatocytesHumansModels, MolecularMolecular StructurePhosphoproteinsProtein ConformationPyrazolesPyridinesStructure-Activity RelationshipAntiviral AgentsHBSC11La protein, humanPhosphoproteinsPyrazolesPyridinesantiviral agentsdrug-like optimizationhepatitis B virus

Identifiers

PMID31241178
PMCPMC6771476
OpenAlexW2954715063

What OpenQuestion holds

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LicenceCC BY
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.