Evidence map›Paper›PMID 28442704›Full record

ArticleScientific reports2016

Discovery of an enzyme and substrate selective inhibitor of ADAM10 using an exosite-binding glycosylated substrate.

Franck Madoux, Daniela Dreymuller, Jean-Phillipe Pettiloud, Radleigh Santos, Christoph Becker-Pauly, Andreas Ludwig, Gregg B Fields, Thomas Bannister, Timothy P Spicer, Mare Cudic and 2 more

Open access · goldAbstract read
In one paragraph

Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.

0numbers the graph read from it
0cells of the map it votes in
27citing papers in PubMed
12.9field-weighted citation impact, top 1% 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

27 citing papers in PubMed, 176 citations in OpenAlex.

  1. Article
  2. Article
  3. Review
  4. Article
  5. Article
  6. ADAM10-a "multitasker" in sepsis: focus on its posttranslational target.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2023
    Review
  7. Protocol for 3D screening of lung cancer spheroids using natural products.SLAS discovery : advancing life sciences R & D · 2023
    Article
  8. Review
  9. Article
  10. Article
  11. Lead identification using 3D models of pancreatic cancer.SLAS discovery : advancing life sciences R & D · 2022
    Article
  12. Article
  13. Article
  14. Article
  15. Review
  16. Article
  17. Review
  18. Review
  19. Article
  20. Domain integration of ADAM family proteins: Emerging themes from structural studies.Experimental biology and medicine (Maywood, N.J.) · 2019
    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

12 authors at 6 institutions in 2 countries.

Franck MadouxLead Identification Division, Translational Research Institute, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL, 39453, United States.
Daniela DreymullerInstitute of Pharmacology and Toxicology, RWTH Aachen University, Wendlingweg 2, 52074, Aachen, Germany.
Jean-Phillipe PettiloudDepartment of Chemistry and Biochemistry, Florida Atlantic University, 5353 Parkside Drive, Jupiter, FL, 39453, United States.
Radleigh SantosTorrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port Saint Lucie, FL, 34987, United States.
Christoph Becker-PaulyUniversity of Kiel, Institute of Biochemistry, Unit for Degradomics of the Protease Web, Rudolf-Höber-Str. 1, 24118, Kiel, Germany.
Andreas LudwigInstitute of Pharmacology and Toxicology, RWTH Aachen University, Wendlingweg 2, 52074, Aachen, Germany.
Gregg B FieldsDepartment of Chemistry and Biochemistry, Florida Atlantic University, 5353 Parkside Drive, Jupiter, FL, 39453, United States.
Thomas BannisterDepartment of Molecular Therapeutics, Translational Research Institute, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL, 39453, United States.
Timothy P SpicerLead Identification Division, Translational Research Institute, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL, 39453, United States.
Mare CudicDepartment of Chemistry and Biochemistry, Florida Atlantic University, 5353 Parkside Drive, Jupiter, FL, 39453, United States.
Louis D ScampaviaLead Identification Division, Translational Research Institute, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL, 39453, United States.
Dmitriy MinondDepartment of Drug Discovery and Development, Harrison School of Pharmacy, 3211B Walker Building, Auburn University, Auburn, Alabama, 36849, USA. dzm0032@auburn.edu.
Scripps Research Institute · USFlorida Atlantic University · USRWTH Aachen University · DEAuburn University · USKiel University · DETorrey Pines Institute For Molecular Studies · US

Funding

UHTS Implementation(Florida)U54MH084512 · NIMH · SCRIPPS RESEARCH INSTITUTE, THE · PI ROSEN, HUGH · 2008 to 2013
$89.2M
Mechanism &Inhibition of Collagenolytic ActivityR01CA098799 · NCI · UNIVERSITY OF TEXAS HLTH SCIENCE CENTER · PI FIELDS, GREGG B · 2003 to 2017
$4.5M
Novel synthetic tools for mucin glycobiologyR21CA178754 · NCI · FLORIDA ATLANTIC UNIVERSITY · PI CUDIC, MARE · 2014 to 2015
$391k
HTS Assays to Discover Selective Inhibitors of ADAM10 and 17R03DA033985 · NIDA · TORREY PINES INST FOR MOLECULAR STUDIES · PI MINOND, DMITRIY · 2012 to 2013
$90k
NCI NIH HHS R01 CA098799NCI NIH HHS R21 CA178754NIDA NIH HHS R03 DA033985NIMH NIH HHS U54 MH084512
6 · The paper itself

Abstract

ADAM10 and ADAM17 have been shown to contribute to the acquired drug resistance of HER2-positive breast cancer in response to trastuzumab. The majority of ADAM10 and ADAM17 inhibitor development has been focused on the discovery of compounds that bind the active site zinc, however, in recent years, there has been a shift from active site to secondary substrate binding site (exosite) inhibitor discovery in order to identify non-zinc-binding molecules. In the present work a glycosylated, exosite-binding substrate of ADAM10 and ADAM17 was utilized to screen 370,276 compounds from the MLPCN collection. As a result of this uHTS effort, a selective, time-dependent, non-zinc-binding inhibitor of ADAM10 with K

Indexed as

ADAM10 ProteinADAM17 ProteinCell Line, TumorDatabases, ChemicalGlycosylationHigh-Throughput Screening AssaysHumansStructure-Activity RelationshipSubstrate SpecificityADAM10 ProteinADAM17 Protein

Identifiers

PMID28442704
PMCPMC5431342
OpenAlexW2557569289

What OpenQuestion holds

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LicenceCC BY
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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 OpenQuestion graph.