Evidence map›Paper›PMID 28094913›Full record

ArticleACS chemical biology2017

Inhibition of Pax2 Transcription Activation with a Small Molecule that Targets the DNA Binding Domain.

Edward Grimley, Chenzhong Liao, Egon J Ranghini, Zaneta Nikolovska-Coleska, Gregory R Dressler

Open access · greenAbstract readValidation Study
In one paragraph

Article in ACS chemical biology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.

0numbers the graph read from it
0cells of the map it votes in
25citing papers in PubMed
1.9field-weighted citation impact, top 14% 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

25 citing papers in PubMed, 42 citations in OpenAlex.

  1. Article
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  3. Review
  4. Article
  5. The Role of the PAX Genes in Renal Cell Carcinoma.International journal of molecular sciences · 2024
    Review
  6. Review
  7. International journal of molecular sciences · 2023
    Review
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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

5 authors at 1 institution in 1 country.

Edward GrimleyDepartment of Pathology, University of Michigan , Ann Arbor, Michigan 48109, United States.ORCID 0000-0003-0438-506X
Chenzhong LiaoDepartment of Pathology, University of Michigan , Ann Arbor, Michigan 48109, United States.
Egon J RanghiniDepartment of Pathology, University of Michigan , Ann Arbor, Michigan 48109, United States.
Zaneta Nikolovska-ColeskaDepartment of Pathology, University of Michigan , Ann Arbor, Michigan 48109, United States.
Gregory R DresslerDepartment of Pathology, University of Michigan , Ann Arbor, Michigan 48109, United States.ORCID 0000-0002-7967-6104
University of Michigan · US

Funding

XenograftP30CA046592 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI Alexey I Nesvizhskii · 1988 to 2026
$178.2M
Research Supplement to Promote Diversity in Health Related ResearchR01DK054740 · NIDDK · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI DRESSLER, GREGORY R · 1999 to 2024
$9.0M
Epigenetic Regulation of Kidney DevelopmentR01DK073722 · NIDDK · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI DRESSLER, GREGORY R · 2006 to 2020
$4.6M
Proteogenomics of Cancer Training ProgramT32CA140044 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI RAO, ARVIND, SARTOR, MAUREEN AGNES · 2010 to 2024
$3.9M
NCI NIH HHS P30 CA046592NCI NIH HHS T32 CA140044NIDDK NIH HHS R01 DK054740NIDDK NIH HHS R01 DK073722
6 · The paper itself

Abstract

The Pax gene family encodes DNA binding transcription factors that control critical steps in embryonic development and differentiation of specific cell lineages. Often, Pax proteins are re-expressed or ectopically expressed in cancer and other diseases of abnormal proliferation, making them attractive targets for tissue specific inhibition by small molecules. In this report, we used a homology model of the Pax2 paired domain and a virtual screen to identify small molecules that can inhibit binding of the paired domain to DNA and Pax2 mediated transcription activation. Candidates from the virtual screen were then confirmed in a cell based Pax2 transactivation assay. Subsequently, we tested analogs of these hits to identify a single compound that effectively blocked Pax2 activity and DNA binding with a K

Indexed as

Small Molecule LibrariesTranscriptional ActivationAnimalsCell Line, TumorComputer SimulationDNAHEK293 CellsHumansKidneyPAX2 Transcription FactorDNAPAX2 Transcription FactorSmall Molecule Libraries

Identifiers

PMID28094913
PMCPMC5761330
OpenAlexW2575094960

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.