Evidence map›Paper›PMID 36720643›Full record

ArticleMolecular pharmacology2023

The Small Molecule Antagonist KCI807 Disrupts Association of the Amino-Terminal Domain of the Androgen Receptor with ELK1 by Modulating the Adjacent DNA Binding Domain.

Claire Soave, Charles Ducker, Naeyma Islam, Seongho Kim, Sally Yurgelevic, Nathan I Nicely, Luke Pardy, Yanfang Huang, Peter E Shaw, Gregory Auner and 2 more

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Molecular pharmacology, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
0.5field-weighted citation impact, top 32% 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

2 citing papers in PubMed, 2 citations in OpenAlex.

  1. Review
  2. The alkylglycerone phosphate synthase sustains the resistance of gastric cancer cells to ferroptosis induced by Apatinib.Gastric cancer : official journal of the International Gastric Cancer Association and the Japanese Gastric Cancer Association · 2025
    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

12 authors at 1 institution in 2 countries.

Claire SoaveDepartment of Oncology (C.S., S.K., Y.H., L.P., M.R.) and Smart Sensors and Integrated Microsystems (SSIM) Program (S.Y., G.A.), Wayne State University School of Medicine and Barbara Ann Karmanos Cancer Institute, Detroit, Michigan; Department of Biochemistry and Molecular Biology, College of Natural Science, Michigan State University, East Lansing, Michigan (N.I. and A.D.); School of Life Sciences, University of Nottingham, Queens Medical Centre, Nottingham, United Kingdom (C.D. and P.E.S.); and Department of Pharmacology, UNC-Chapel Hill School of Medicine, Chapel Hill, North Carolina (N.N.).ORCID 0000-0003-0546-4368
Charles DuckerDepartment of Oncology (C.S., S.K., Y.H., L.P., M.R.) and Smart Sensors and Integrated Microsystems (SSIM) Program (S.Y., G.A.), Wayne State University School of Medicine and Barbara Ann Karmanos Cancer Institute, Detroit, Michigan; Department of Biochemistry and Molecular Biology, College of Natural Science, Michigan State University, East Lansing, Michigan (N.I. and A.D.); School of Life Sciences, University of Nottingham, Queens Medical Centre, Nottingham, United Kingdom (C.D. and P.E.S.); and Department of Pharmacology, UNC-Chapel Hill School of Medicine, Chapel Hill, North Carolina (N.N.).
Naeyma IslamDepartment of Oncology (C.S., S.K., Y.H., L.P., M.R.) and Smart Sensors and Integrated Microsystems (SSIM) Program (S.Y., G.A.), Wayne State University School of Medicine and Barbara Ann Karmanos Cancer Institute, Detroit, Michigan; Department of Biochemistry and Molecular Biology, College of Natural Science, Michigan State University, East Lansing, Michigan (N.I. and A.D.); School of Life Sciences, University of Nottingham, Queens Medical Centre, Nottingham, United Kingdom (C.D. and P.E.S.); and Department of Pharmacology, UNC-Chapel Hill School of Medicine, Chapel Hill, North Carolina (N.N.).
Seongho KimDepartment of Oncology (C.S., S.K., Y.H., L.P., M.R.) and Smart Sensors and Integrated Microsystems (SSIM) Program (S.Y., G.A.), Wayne State University School of Medicine and Barbara Ann Karmanos Cancer Institute, Detroit, Michigan; Department of Biochemistry and Molecular Biology, College of Natural Science, Michigan State University, East Lansing, Michigan (N.I. and A.D.); School of Life Sciences, University of Nottingham, Queens Medical Centre, Nottingham, United Kingdom (C.D. and P.E.S.); and Department of Pharmacology, UNC-Chapel Hill School of Medicine, Chapel Hill, North Carolina (N.N.).
Sally YurgelevicDepartment of Oncology (C.S., S.K., Y.H., L.P., M.R.) and Smart Sensors and Integrated Microsystems (SSIM) Program (S.Y., G.A.), Wayne State University School of Medicine and Barbara Ann Karmanos Cancer Institute, Detroit, Michigan; Department of Biochemistry and Molecular Biology, College of Natural Science, Michigan State University, East Lansing, Michigan (N.I. and A.D.); School of Life Sciences, University of Nottingham, Queens Medical Centre, Nottingham, United Kingdom (C.D. and P.E.S.); and Department of Pharmacology, UNC-Chapel Hill School of Medicine, Chapel Hill, North Carolina (N.N.).
Nathan I NicelyDepartment of Oncology (C.S., S.K., Y.H., L.P., M.R.) and Smart Sensors and Integrated Microsystems (SSIM) Program (S.Y., G.A.), Wayne State University School of Medicine and Barbara Ann Karmanos Cancer Institute, Detroit, Michigan; Department of Biochemistry and Molecular Biology, College of Natural Science, Michigan State University, East Lansing, Michigan (N.I. and A.D.); School of Life Sciences, University of Nottingham, Queens Medical Centre, Nottingham, United Kingdom (C.D. and P.E.S.); and Department of Pharmacology, UNC-Chapel Hill School of Medicine, Chapel Hill, North Carolina (N.N.).
Luke PardyDepartment of Oncology (C.S., S.K., Y.H., L.P., M.R.) and Smart Sensors and Integrated Microsystems (SSIM) Program (S.Y., G.A.), Wayne State University School of Medicine and Barbara Ann Karmanos Cancer Institute, Detroit, Michigan; Department of Biochemistry and Molecular Biology, College of Natural Science, Michigan State University, East Lansing, Michigan (N.I. and A.D.); School of Life Sciences, University of Nottingham, Queens Medical Centre, Nottingham, United Kingdom (C.D. and P.E.S.); and Department of Pharmacology, UNC-Chapel Hill School of Medicine, Chapel Hill, North Carolina (N.N.).
Yanfang HuangDepartment of Oncology (C.S., S.K., Y.H., L.P., M.R.) and Smart Sensors and Integrated Microsystems (SSIM) Program (S.Y., G.A.), Wayne State University School of Medicine and Barbara Ann Karmanos Cancer Institute, Detroit, Michigan; Department of Biochemistry and Molecular Biology, College of Natural Science, Michigan State University, East Lansing, Michigan (N.I. and A.D.); School of Life Sciences, University of Nottingham, Queens Medical Centre, Nottingham, United Kingdom (C.D. and P.E.S.); and Department of Pharmacology, UNC-Chapel Hill School of Medicine, Chapel Hill, North Carolina (N.N.).
Peter E ShawDepartment of Oncology (C.S., S.K., Y.H., L.P., M.R.) and Smart Sensors and Integrated Microsystems (SSIM) Program (S.Y., G.A.), Wayne State University School of Medicine and Barbara Ann Karmanos Cancer Institute, Detroit, Michigan; Department of Biochemistry and Molecular Biology, College of Natural Science, Michigan State University, East Lansing, Michigan (N.I. and A.D.); School of Life Sciences, University of Nottingham, Queens Medical Centre, Nottingham, United Kingdom (C.D. and P.E.S.); and Department of Pharmacology, UNC-Chapel Hill School of Medicine, Chapel Hill, North Carolina (N.N.).
Gregory AunerDepartment of Oncology (C.S., S.K., Y.H., L.P., M.R.) and Smart Sensors and Integrated Microsystems (SSIM) Program (S.Y., G.A.), Wayne State University School of Medicine and Barbara Ann Karmanos Cancer Institute, Detroit, Michigan; Department of Biochemistry and Molecular Biology, College of Natural Science, Michigan State University, East Lansing, Michigan (N.I. and A.D.); School of Life Sciences, University of Nottingham, Queens Medical Centre, Nottingham, United Kingdom (C.D. and P.E.S.); and Department of Pharmacology, UNC-Chapel Hill School of Medicine, Chapel Hill, North Carolina (N.N.).
Alex DicksonDepartment of Oncology (C.S., S.K., Y.H., L.P., M.R.) and Smart Sensors and Integrated Microsystems (SSIM) Program (S.Y., G.A.), Wayne State University School of Medicine and Barbara Ann Karmanos Cancer Institute, Detroit, Michigan; Department of Biochemistry and Molecular Biology, College of Natural Science, Michigan State University, East Lansing, Michigan (N.I. and A.D.); School of Life Sciences, University of Nottingham, Queens Medical Centre, Nottingham, United Kingdom (C.D. and P.E.S.); and Department of Pharmacology, UNC-Chapel Hill School of Medicine, Chapel Hill, North Carolina (N.N.).
Manohar RatnamDepartment of Oncology (C.S., S.K., Y.H., L.P., M.R.) and Smart Sensors and Integrated Microsystems (SSIM) Program (S.Y., G.A.), Wayne State University School of Medicine and Barbara Ann Karmanos Cancer Institute, Detroit, Michigan; Department of Biochemistry and Molecular Biology, College of Natural Science, Michigan State University, East Lansing, Michigan (N.I. and A.D.); School of Life Sciences, University of Nottingham, Queens Medical Centre, Nottingham, United Kingdom (C.D. and P.E.S.); and Department of Pharmacology, UNC-Chapel Hill School of Medicine, Chapel Hill, North Carolina (N.N.) ratnamm@karmanos.org.
University of North Carolina at Chapel Hill · US

Funding

TRAINING PROGRAM IN THE BIOLOGY OF CANCERT32CA009531 · NCI · WAYNE STATE UNIVERSITY · PI Larry H Matherly · 1985 to 2026
$5.3M
NCI NIH HHS T32 CA009531
6 · The paper itself

Abstract

The androgen receptor (AR) is a crucial coactivator of ELK1 for prostate cancer (PCa) growth, associating with ELK1 through two peptide segments (358-457 and 514-557) within the amino-terminal domain (NTD) of AR. The small-molecule antagonist 5-hydroxy-2-(3-hydroxyphenyl)chromen-4-one (KCI807) binds to AR, blocking ELK1 binding and inhibiting PCa growth. We investigated the mode of interaction of KCI807 with AR using systematic mutagenesis coupled with ELK1 coactivation assays, testing polypeptide binding and Raman spectroscopy. In full-length AR, deletion of neither ELK1 binding segment affected sensitivity of residual ELK1 coactivation to KCI807. Although the NTD is sufficient for association of AR with ELK1, interaction of the isolated NTD with ELK1 was insensitive to KCI807. In contrast, coactivation of ELK1 by the AR-V7 splice variant, comprising the NTD and the DNA binding domain (DBD), was sensitive to KCI807. Deletions and point mutations within DBD segment 558-595, adjacent to the NTD, interfered with coactivation of ELK1, and residual ELK1 coactivation by the mutants was insensitive to KCI807. In a

Indexed as

Prostatic NeoplasmsReceptors, AndrogenDNAets-Domain Protein Elk-1HumansMalePeptidesProtein DomainsDNAELK1 protein, humanets-Domain Protein Elk-1PeptidesReceptors, Androgen

Identifiers

PMID36720643
PMCPMC11033959
OpenAlexW4318689626

What OpenQuestion holds

Textmetadata
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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.