Evidence map›Paper›PMID 33863813›Full record

ArticleMolecular cancer research : MCR2021

NF-κB Blockade with Oral Administration of Dimethylaminoparthenolide (DMAPT), Delays Prostate Cancer Resistance to Androgen Receptor (AR) Inhibition and Inhibits AR Variants.

Katherine L Morel, Anis A Hamid, John G Clohessy, Nicole Pandell, Leigh Ellis, Christopher J Sweeney

Open access · bronzeAbstract read
In one paragraph

Article in Molecular cancer research : MCR, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
15citing papers in PubMed, 1 pooled it
1.1field-weighted citation impact, top 26% 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

15 citing papers in PubMed, 1 synthesis or guideline pooled it, 21 citations in OpenAlex.

  1. Pooled it
  2. Exosomes as Emerging Nanocarriers for Targeted Cancer Therapy.International journal of nanomedicine · 2026
    Review
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  4. Article
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  6. Article
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  8. Article
  9. Article
  10. Versatile function of NF-ĸB in inflammation and cancer.Experimental hematology & oncology · 2024
    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

6 authors at 4 institutions in 2 countries.

Katherine L MorelDepartment of Oncologic Pathology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, Massachusetts.ORCID 0000-0002-7968-4032
Anis A HamidDepartment of Medical Oncology, Lank Center for Genitourinary Oncology, Dana-Farber Cancer Institute, Boston, Massachusetts.ORCID 0000-0002-7193-9723
John G ClohessyDepartment of Medicine, Preclinical Murine Pharmacogenetics Facility, Cancer Research Institute, Beth Israel Deaconess Cancer Center, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Massachusetts.ORCID 0000-0001-5186-9775
Nicole PandellDepartment of Medicine, Preclinical Murine Pharmacogenetics Facility, Cancer Research Institute, Beth Israel Deaconess Cancer Center, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Massachusetts.
Leigh EllisDepartment of Oncologic Pathology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, Massachusetts.ORCID 0000-0003-4739-5049
Christopher J SweeneyDepartment of Medical Oncology, Lank Center for Genitourinary Oncology, Dana-Farber Cancer Institute, Boston, Massachusetts. Christopher_Sweeney@DFCI.harvard.edu.ORCID 0000-0002-0398-6018
Beth Israel Deaconess Medical Center · USBroad Institute · USDana-Farber Cancer Institute · USThe University of Melbourne · AU

Funding

Tumor and Circulating Markers as Links Between Obesity and Lethal Prostate CanceP50CA090381 · NCI · DANA-FARBER CANCER INSTITUTE · PI KANTOFF, PHILIP W · 2002 to 2017
$36.2M
NCI NIH HHS P50 CA090381
6 · The paper itself

Abstract

NF-κB activation has been linked to prostate cancer progression and is commonly observed in castrate-resistant disease. It has been suggested that NF-κB-driven resistance to androgen-deprivation therapy (ADT) in prostate cancer cells may be mediated by aberrant androgen receptor (AR) activation and AR splice variant production. Preventing resistance to ADT may therefore be achieved by using NF-κB inhibitors. However, low oral bioavailability and high toxicity of NF-κB inhibitors is a major challenge for clinical translation. Dimethylaminoparthenolide (DMAPT) is an oral NF-κB inhibitor in clinical development and has already shown favorable pharmacokinetic and pharmacodyanamic data in patients with heme malignancies, including decrease of NF-κB in circulating leuchemic blasts. Here, we report that activation of NF-κB/p65 by castration in mouse and human prostate cancer models resulted in a significant increase in AR variant-7 (AR-V7) expression and modest upregulation of AR.

Indexed as

Administration, OralAndrogen Receptor AntagonistsAnimalsCell Line, TumorDrug Resistance, NeoplasmGene Expression ProfilingGene Expression Regulation, NeoplasticHumansKaplan-Meier EstimateMaleMiceMice, Inbred ICRMice, SCIDNF-kappa BProstatic Neoplasms, Castration-ResistantProtein IsoformsAndrogen Receptor AntagonistsLC-1 compoundNF-kappa BProtein IsoformsReceptors, AndrogenSesquiterpenes

Identifiers

PMID33863813
PMCPMC8254800
OpenAlexW3155592702

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.