Evidence mapPaperPMID 38760437Full record

ArticleScientific reports2024

Identification of DprE1 inhibitors for tuberculosis through integrated in-silico approaches.

Swagatika Dash, Ekta Rathi, Avinash Kumar, Kiran Chawla, Suvarna G Kini

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Article in Scientific reports, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.

0numbers the graph read from it
0cells of the map it votes in
13citing papers in PubMed
field-weighted citation impact
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

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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

13 citing papers in PubMed.

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  5. Design, Synthesis,ACS omega · 2025
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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

5 authors.

Swagatika DashDepartment of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, India, 576104.
Ekta RathiDepartment of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, India, 576104.
Avinash KumarDepartment of Medical Affairs, Curie Sciences Private Limited, Samastipur, Bihar, India, 848125.
Kiran ChawlaDepartment of Microbiology, Kasturba Medical College, Manipal Academy of Higher Education, Manipal, Karnataka, India, 576104.
Suvarna G KiniDepartment of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, India, 576104. suvarna.gk@manipal.edu.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Decaprenylphosphoryl-β-D-ribose-2'-epimerase (DprE1), a crucial enzyme in the process of arabinogalactan and lipoarabinomannan biosynthesis, has become the target of choice for anti-TB drug discovery in the recent past. The current study aims to find the potential DprE1 inhibitors through in-silico approaches. Here, we built the pharmacophore and 3D-QSAR model using the reported 40 azaindole derivatives of DprE1 inhibitors. The best pharmacophore hypothesis (ADRRR_1) was employed for the virtual screening of the chEMBL database. To identify prospective hits, molecules with good phase scores (> 2.000) were further evaluated by molecular docking studies for their ability to bind to the DprE1 enzyme (PDB: 4KW5). Based on their binding affinities (< - 9.0 kcal/mole), the best hits were subjected to the calculation of free-binding energies (Prime/MM-GBSA), pharmacokinetic, and druglikeness evaluations. The top 10 hits retrieved from these results were selected to predict their inhibitory activities via the developed 3D-QSAR model with a regression coefficient (R

Indexed as

Antitubercular AgentsMolecular Docking SimulationQuantitative Structure-Activity RelationshipAlcohol OxidoreductasesBacterial ProteinsComputer SimulationDrug DiscoveryEnzyme InhibitorsMolecular Dynamics SimulationMycobacterium tuberculosisProtein BindingTuberculosisAlcohol OxidoreductasesAntitubercular AgentsBacterial ProteinsDprE1 protein, Mycobacterium tuberculosisEnzyme Inhibitors3D-QSARDprE1Molecular dynamicsMycobacterium tuberculosisPharmacophore

Identifiers

PMID38760437
PMCPMC11101490

What Socratic holds

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Registered trials

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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 Socratic graph.