Evidence map›Paper›PMID 33472061›Full record

ArticleCell reports2021

Impact of WIN site inhibitor on the WDR5 interactome.

Alissa D Guarnaccia, Kristie L Rose, Jing Wang, Bin Zhao, Tessa M Popay, Christina E Wang, Kiana Guerrazzi, Salisha Hill, Chase M Woodley, Tyler J Hansen and 8 more

Open access · goldAbstract read
In one paragraph

Article in Cell reports, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 47 papers.

0numbers the graph read from it
0cells of the map it votes in
47citing papers in PubMed
4.8field-weighted citation impact, top 4% 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

47 citing papers in PubMed, 72 citations in OpenAlex.

  1. Review
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  7. Probing the Cancer Mutational Landscape of KMT2 Regulatory Subunits.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2026
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  17. Deciphering Facioscapulohumeral Dystrophy in the clinical trials era: where are we now?Acta myologica : myopathies and cardiomyopathies : official journal of the Mediterranean Society of Myology · 2025
    Review
  18. Article
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  20. Article
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

18 authors at 2 institutions in 1 country.

Alissa D GuarnacciaDepartment of Cell and Developmental Biology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Kristie L RoseDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN 37232, USA; Mass Spectrometry Research Center, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Jing WangDepartment of Biostatistics, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Center for Quantitative Sciences, Vanderbilt University Medical Center, Nashville, TN, 37232, USA.
Bin ZhaoDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Tessa M PopayDepartment of Cell and Developmental Biology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Christina E WangDepartment of Cell and Developmental Biology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Kiana GuerrazziDepartment of Cell and Developmental Biology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Salisha HillMass Spectrometry Research Center, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Chase M WoodleyDepartment of Cell and Developmental Biology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Tyler J HansenDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Shelly L LoreyDepartment of Cell and Developmental Biology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
J Grace ShawDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
William G PayneDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
April M WeissmillerDepartment of Cell and Developmental Biology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Edward T OlejniczakDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Stephen W FesikDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN 37232, USA; Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA; Department of Chemistry, Vanderbilt University, Nashville, TN 37232, USA.
Qi LiuDepartment of Biostatistics, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Center for Quantitative Sciences, Vanderbilt University Medical Center, Nashville, TN, 37232, USA.
William P TanseyDepartment of Cell and Developmental Biology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA; Department of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN 37232, USA. Electronic address: william.p.tansey@vanderbilt.edu.
Vanderbilt University · USVanderbilt University Medical Center · US

Funding

Tumor Immunology and Microenvironment Research ProgramP30CA068485 · NCI · VANDERBILT UNIVERSITY MEDICAL CENTER · PI MATTHEW J TYSKA · 1995 to 2026
$172.8M
VANDERBILT UNIVERSITY CTSA FOR PEDIATRIC RESEARCHUL1RR024975 · NCRR · VANDERBILT UNIVERSITY · PI BERNARD, GORDON RAPHAEL · 2007 to 2011
$45.7M
Translational Analysis CoreP30DK058404 · NIDDK · VANDERBILT UNIVERSITY MEDICAL CENTER · PI RICHARD M. PEEK · 2002 to 2026
$29.9M
Vanderbilt Diabetes Research CenterP30DK020593 · NIDDK · VANDERBILT UNIVERSITY MEDICAL CENTER · PI OWEN P MCGUINNESS · 2012 to 2026
$29.3M
Shop Module CoreP30EY008126 · NEI · VANDERBILT UNIVERSITY MEDICAL CENTER · PI Kevin L Schey · 1989 to 2026
$19.6M
Vanderbilt Mouse Metabolic Physiology CenterU24DK059637 · NIDDK · VANDERBILT UNIVERSITY · PI WASSERMAN, DAVID H · 2001 to 2015
$14.9M
BIOCHEMICAL &CHEMICAL TRAINING FOR CANCER RESEARCHT32CA009582 · NCI · VANDERBILT UNIVERSITY · PI David K Cortez · 1987 to 2026
$8.8M
VANTAGE:Consolidation to create the Vanderbilt Technologies for Advanced GenomicsG20RR030956 · NCRR · VANDERBILT UNIVERSITY · PI PIETENPOL, JENNIFER A · 2010 to 2010
$8.7M
Integrated Biological Systems Training in OncologyT32CA119925 · NCI · VANDERBILT UNIVERSITY · PI Vivian Gama, William Patrick Tansey · 2008 to 2026
$7.6M
Facilitated recruitment of MYC to chromatin by interaction with WDR5R01CA200709 · NCI · VANDERBILT UNIVERSITY · PI TANSEY, WILLIAM PATRICK · 2016 to 2025
$3.9M
Investigating MYC and WDR5 chromatin interactions in cancerF31CA225065 · NCI · VANDERBILT UNIVERSITY · PI GUARNACCIA, ALISSA DUPUY · 2018 to 2020
$88k
CCR NIH HHS HHSN261200800001CNCI NIH HHS F31 CA225065NCI NIH HHS HHSN261200800001ENCI NIH HHS P30 CA068485NCI NIH HHS R01 CA200709NCI NIH HHS T32 CA009582NCI NIH HHS T32 CA119925NCRR NIH HHS G20 RR030956NCRR NIH HHS UL1 RR024975NEI NIH HHS P30 EY008126NIDDK NIH HHS P30 DK020593NIDDK NIH HHS P30 DK058404NIDDK NIH HHS U24 DK059637
6 · The paper itself

Abstract

The chromatin-associated protein WDR5 is a promising pharmacological target in cancer, with most drug discovery efforts directed against an arginine-binding cavity in WDR5 called the WIN site. Despite a clear expectation that WIN site inhibitors will alter the repertoire of WDR5 interaction partners, their impact on the WDR5 interactome remains unknown. Here, we use quantitative proteomics to delineate how the WDR5 interactome is changed by WIN site inhibition. We show that the WIN site inhibitor alters the interaction of WDR5 with dozens of proteins, including those linked to phosphatidylinositol 3-kinase (PI3K) signaling. As proof of concept, we demonstrate that the master kinase PDPK1 is a bona fide high-affinity WIN site binding protein that engages WDR5 to modulate transcription of genes expressed in the G2 phase of the cell cycle. This dataset expands our understanding of WDR5 and serves as a resource for deciphering the action of WIN site inhibitors.

Indexed as

3-Phosphoinositide-Dependent Protein KinasesAmino Acid SequenceBinding SitesDrug DiscoveryG2 PhaseGene Expression RegulationHEK293 CellsHumansImmunoprecipitationIntracellular Signaling Peptides and ProteinsModels, MolecularMolecular Targeted TherapyProtein Binding3-Phosphoinositide-Dependent Protein KinasesIntracellular Signaling Peptides and ProteinsPDPK1 protein, humanWDR5 protein, humancancer therapychromatinPDPK1WDR5

Identifiers

PMID33472061
PMCPMC7871196
OpenAlexW3124478018

What OpenQuestion holds

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LicenceCC BY-NC-ND
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.