Evidence map›Paper›PMID 26152429›Full record

ArticleBioorganic & medicinal chemistry letters2015

Structure-activity relationship studies of QS11, a small molecule Wnt synergistic agonist.

Manish K Singh, Huanyao Gao, Wei Sun, Zhiquan Song, Robert Schmalzigaug, Richard T Premont, Qisheng Zhang

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
0.3field-weighted citation impact, top 39% 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

9 citing papers in PubMed, 15 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Article
  5. Article
  6. Targeting the Small GTPase Superfamily through Their Regulatory Proteins.Angewandte Chemie (International ed. in English) · 2020
    Review
  7. Article
  8. Article
  9. Arf GAPs as Regulators of the Actin Cytoskeleton-An Update.International journal of molecular sciences · 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

7 authors at 2 institutions in 1 country.

Manish K SinghDivision of Chemical Biology and Medicinal Chemistry, The University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
Huanyao GaoDivision of Chemical Biology and Medicinal Chemistry, The University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
Wei SunDivision of Chemical Biology and Medicinal Chemistry, The University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
Zhiquan SongDivision of Chemical Biology and Medicinal Chemistry, The University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
Robert SchmalzigaugDivision of Gastroenterology, School of Medicine, Duke University, Durham, NC 27710, USA.
Richard T PremontDivision of Gastroenterology, School of Medicine, Duke University, Durham, NC 27710, USA.
Qisheng ZhangDivision of Chemical Biology and Medicinal Chemistry, The University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA. Electronic address: qszhang@unc.edu.
University of North Carolina at Chapel Hill · USDuke University · US

Funding

Developing Small Molecule ARFGAP Regulators to Dissect Cell SignalingR01GM086558 · NIGMS · UNIV OF NORTH CAROLINA CHAPEL HILL · PI ZHANG, QISHENG · 2011 to 2015
$1.4M
NIGMS NIH HHS GM086558NIGMS NIH HHS R01 GM086558
6 · The paper itself

Abstract

Both the Wnt/β-catenin signaling pathway and small GTPases of the ADP-ribosylation factors (ARF) family play important roles in regulating cell development, homeostasis and fate. The previous report of QS11, a small molecule Wnt synergist that binds to ARF GTPase-activating protein 1 (ARFGAP1), suggests a role for ARFGAP1 in the Wnt/β-catenin pathway. However, direct inhibition of enzymatic activity of ARFGAP1 by QS11 has not been established. Whether ARFGAP1 is the only target that contributes to QS11's Wnt synergy is also not clear. Here we present structure-activity relationship (SAR) studies of QS11 analogs in two assays: direct inhibition of enzymatic activity of purified ARFGAP1 protein and cellular activation of the Wnt/β-catenin pathway. The results confirm the direct inhibition of ARFGAP1 by QS11, and also suggest the presence of other potential cellular targets of QS11.

Indexed as

beta CateninDose-Response Relationship, DrugGTPase-Activating ProteinsHumansMolecular StructurePurinesStructure-Activity RelationshipWnt ProteinsWnt Signaling PathwayARFGAP1 protein, humanbeta CateninGTPase-Activating ProteinsPurinesQS11 compoundWnt ProteinsADP-ribosylation factorsGTPase-activating proteinsQS11Structure–activity relationship (SAR)Wnt/β-catenin signaling

Identifiers

PMID26152429
PMCPMC4607626
OpenAlexW814776857

What OpenQuestion holds

Textmetadata
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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.