Evidence map›Paper›PMID 34822095›Full record

ArticleMolecular diversity2022

Detection of a target protein (GroEl2) in Mycobacterium tuberculosis using a derivative of 1,2,4-triazolethiols.

Sampa Sarkar, Sagar Swami, Sarvesh Kumar Soni, Jessica K Holien, Arshad Khan, Arvind M Korwar, Anjali P Likhite, Ramesh A Joshi, Rohini R Joshi, Dhiman Sarkar

Abstract read
PubMed Publisher
In one paragraph

Article in Molecular diversity, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing 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

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

2 citing papers in PubMed.

  1. Article
  2. Structural chemistry · 2022
    Article
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

10 authors.

Sampa Sarkar *School of Science, STEM College, Engineering and Health, RMIT University, GPO Box 2476, Melbourne, VIC, 3001, Australia.ORCID http://orcid.org/0000-0003-3265-4546
Sagar Swami *Combi-Chem Bio-Resource Centre, Organic Chemistry Division, CSIR-National Chemical Laboratory, Pune, Maharashtra, 411 008, India.ORCID http://orcid.org/0000-0001-9540-7660
Sarvesh Kumar SoniSchool of Science, STEM College, Engineering and Health, RMIT University, GPO Box 2476, Melbourne, VIC, 3001, Australia.
Jessica K HolienSchool of Science, STEM College, Engineering and Health, RMIT University, GPO Box 2476, Melbourne, VIC, 3001, Australia.
Arshad KhanCombi-Chem Bio-Resource Centre, Organic Chemistry Division, CSIR-National Chemical Laboratory, Pune, Maharashtra, 411 008, India.
Arvind M KorwarBiochemical Sciences Division, CSIR-National Chemical Laboratory, Pune, Maharashtra, 411 008, India.
Anjali P LikhiteOrganic Chemistry Division, CSIR-National Chemical Laboratory, Pune, Maharashtra, 411 008, India.
Ramesh A JoshiOrganic Chemistry Division, CSIR-National Chemical Laboratory, Pune, Maharashtra, 411 008, India.
Rohini R JoshiOrganic Chemistry Division, CSIR-National Chemical Laboratory, Pune, Maharashtra, 411 008, India.
Dhiman SarkarCombi-Chem Bio-Resource Centre, Organic Chemistry Division, CSIR-National Chemical Laboratory, Pune, Maharashtra, 411 008, India. d.sarkar@ncl.res.in.ORCID http://orcid.org/0000-0002-3912-1104

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Herein, we identified a potent lead compound RRA2, within a series of 54 derivatives of 1,2,4-triazolethiols (exhibit good potency as an anti-mycobacterial agents) against intracellular Mycobacterium tuberculosis (Mtb). Compound RRA2 showed significant mycobactericidal activity against active stage Mycobacterium bovis BCG and Mtb with minimum inhibitory concentration (MIC) values of 2.3 and 2.0 µg/mL, respectively. At MIC value, RRA2 compound yielded 0.82 log reduction of colony-forming unit (cfu) against non-replicating Mtb. Furthermore, RRA2 compound was selected for further target identification due to the presence of alkyne group, showing higher selectivity index (> 66.66 ± 0.22, in non-replicating stage). Using "click" chemistry, we synthesized the biotin linker-RRA2 conjugate, purified with HPLC method and confirmed the conjugation of biotin linker-RRA2 complex by HR-MS analysis. Furthermore, we successfully pulled down and identified a specific target protein GroEl2, from Mtb whole-cell extract. Furthermore, computational molecular modeling indicated RRA2 could interact with GroEl2, which explains the structure-activity relationship observed in this study. GroEL-2 identified a potent and specific target protein for RRA 2 compound in whole cell extract of Mtb H37Ra.

Indexed as

Mycobacterium tuberculosisAlkynesAnti-Bacterial AgentsAntitubercular AgentsBacterial ProteinsBCG VaccineBiotinCell ExtractsMicrobial Sensitivity TestsProteinsSulfhydryl CompoundsTriazoles1,2,4-triazoleAlkynesAnti-Bacterial AgentsAntitubercular AgentsBacterial ProteinsBCG VaccineBiotinCell ExtractsProteinsSulfhydryl CompoundsTriazoles1,2,4-triazolethiolsGroEl2Mycobactericidal activityMycobacterium bovis BCGMycobacterium tuberculosis

Identifiers

What OpenQuestion holds

Textmetadata
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.