Evidence map›Paper›PMID 24900769›Full record

ArticleACS medicinal chemistry letters2014

Identification of ML251, a Potent Inhibitor of T. brucei and T. cruzi Phosphofructokinase.

Kyle R Brimacombe, Martin J Walsh, Li Liu, Montserrat G Vásquez-Valdivieso, Hugh P Morgan, Iain McNae, Linda A Fothergill-Gilmore, Paul A M Michels, Douglas S Auld, Anton Simeonov and 3 more

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.

0numbers the graph read from it
0cells of the map it votes in
17citing papers in PubMed
1.6field-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

17 citing papers in PubMed, 33 citations in OpenAlex.

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  5. PEX1 is essential for glycosome biogenesis and trypanosomatid parasite survival.Frontiers in cellular and infection microbiology · 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

13 authors at 3 institutions in 2 countries.

Kyle R BrimacombeNational Center for Advancing Translational Sciences, National Institutes of Health , 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Martin J WalshNational Center for Advancing Translational Sciences, National Institutes of Health , 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Li LiuNational Center for Advancing Translational Sciences, National Institutes of Health , 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Montserrat G Vásquez-ValdiviesoCentre for Translational and Chemical Biology, School of Biological Sciences, University of Edinburgh , Michael Swann Building, The King's Buildings, Mayfield Road, Edinburgh EH9 3JR, U.K.
Hugh P MorganCentre for Translational and Chemical Biology, School of Biological Sciences, University of Edinburgh , Michael Swann Building, The King's Buildings, Mayfield Road, Edinburgh EH9 3JR, U.K.
Iain McNaeCentre for Translational and Chemical Biology, School of Biological Sciences, University of Edinburgh , Michael Swann Building, The King's Buildings, Mayfield Road, Edinburgh EH9 3JR, U.K.
Linda A Fothergill-GilmoreCentre for Translational and Chemical Biology, School of Biological Sciences, University of Edinburgh , Michael Swann Building, The King's Buildings, Mayfield Road, Edinburgh EH9 3JR, U.K.
Paul A M MichelsResearch Unit for Tropical Diseases, de Duve Institute and Laboratory of Biochemistry, Université catholique de Louvain , Avenue Hippocrate 74, B-1200 Brussels, Belgium.
Douglas S AuldNational Center for Advancing Translational Sciences, National Institutes of Health , 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Anton SimeonovNational Center for Advancing Translational Sciences, National Institutes of Health , 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Malcolm D WalkinshawCentre for Translational and Chemical Biology, School of Biological Sciences, University of Edinburgh , Michael Swann Building, The King's Buildings, Mayfield Road, Edinburgh EH9 3JR, U.K.
Min ShenNational Center for Advancing Translational Sciences, National Institutes of Health , 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Matthew B BoxerNational Center for Advancing Translational Sciences, National Institutes of Health , 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
National Center for Advancing Translational Sciences · USNational Institutes of Health · USde Duve Institute · BE

Funding

NIH Chemical Genomics CenterZIBTR000004 · NCATS · NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES · PI MCKEW, JOHN · 2012 to 2014
$52.3M
Wellcome Trust 092076
6 · The paper itself

Abstract

Human African Trypanosomiasis (HAT) is a severe, often fatal disease caused by the parasitic protist Trypanosoma brucei. The glycolytic pathway has been identified as the sole mechanism for ATP generation in the infective stage of these organisms, and several glycolytic enzymes, phosphofructokinase (PFK) in particular, have shown promise as potential drug targets. Herein, we describe the discovery of ML251, a novel nanomolar inhibitor of T. brucei PFK, and the structure-activity relationships within the series.

Indexed as

glycolysishigh-throughput screeninginhibitorsphosphofructokinaseTrypanosoma bruceiTrypanosoma cruzi

Identifiers

PMID24900769
PMCPMC4027769
OpenAlexW2029589290

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.