Evidence map›Paper›PMID 21665483›Full record

ArticleBioorganic & medicinal chemistry2011

Evaluation of NTF1836 as an inhibitor of the mycothiol biosynthetic enzyme MshC in growing and non-replicating Mycobacterium tuberculosis.

Gerald L Newton, Nancy Buchmeier, James J La Clair, Robert C Fahey

Open access · greenAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
1.7field-weighted citation impact, top 17% 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

10 citing papers in PubMed, 29 citations in OpenAlex.

  1. Article
  2. Article
  3. A pro-oxidant property of vitamin C to overcome the burden of latentFrontiers in cellular and infection microbiology · 2023
    Review
  4. Article
  5. Review
  6. Review
  7. Article
  8. Review
  9. Article
  10. Adenylating enzymes in Mycobacterium tuberculosis as drug targets.Current topics in medicinal chemistry · 2012
    Review
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

4 authors at 1 institution in 1 country.

Gerald L NewtonDepartment of Chemistry and Biochemistry, University of California, San Diego, La Jolla, CA 92093-0314, United States.
Nancy Buchmeier
James J La Clair
Robert C Fahey
University of California, San Diego · US

Funding

Whole cell and essential enzyme screening assays for mycothiol biosynthesisR01AI072133 · NIAID · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI FAHEY, ROBERT C · 2007 to 2009
$899k
NIAID NIH HHS AI072133NIAID NIH HHS R01 AI072133
6 · The paper itself

Abstract

The mycothiol biosynthesis enzyme MshC catalyzes the ligation of cysteine with the pseudodisaccharide GlcN-Ins and has been identified as an essential enzyme in Mycobacterium tuberculosis. We now report on the development of NTF1836 as a micromolar inhibitor of MshC. Using commercial libraries, we conducted preliminary structure-activity relationship (SAR) studies on NTF1836. Based on this data, NTF1836 and five structurally related compounds showed similar activity towards clinical strains of M. tuberculosis. A gram scale synthesis was developed to provide ample material for biological studies. Using this material, we determined that inhibition of M. tuberculosis growth by NTF1836 was accompanied by a fall in mycothiol and an increase in GlcN-Ins consistent with the targeting of MshC. We also determined that NTF1836 kills non-replicating M. tuberculosis in the carbon starvation model of latency.

Indexed as

AnimalsBacterial ProteinsChlorocebus aethiopsCysteineDibenzothiazepinesDrug Evaluation, PreclinicalEnzyme InhibitorsGlycopeptidesInositolMycobacterium tuberculosisStructure-Activity RelationshipVero CellsBacterial ProteinsCysteineDibenzothiazepinesEnzyme InhibitorsGlycopeptidesInositolmycothiolNTF 1836

Identifiers

PMID21665483
PMCPMC3123436
OpenAlexW2003988250

What OpenQuestion holds

Textmetadata
LicenceTDM
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.