Evidence map›Paper›PMID 30565725›Full record

ReviewMedicinal research reviews2019

Molecules targeting the androgen receptor (AR) signaling axis beyond the AR-Ligand binding domain.

N G R Dayan Elshan, Matthew B Rettig, Michael E Jung

Abstract readReview
In one paragraph

Review in Medicinal research reviews, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.

0numbers the graph read from it
0cells of the map it votes in
31citing papers in PubMed
–field-weighted citation impact
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

31 citing papers in PubMed.

  1. Article
  2. Review
  3. Article
  4. Review
  5. Rapid Dereplication of Trunk Bark Constituents ofInternational journal of molecular sciences · 2025
    Article
  6. Review
  7. Article
  8. Article
  9. Review
  10. Article
  11. Article
  12. Core Structure-Activity Relationship Studies of 5,7,20-Pharmaceuticals (Basel, Switzerland) · 2023
    Article
  13. Article
  14. Article
  15. Article
  16. Synthesis and biological evaluation of niclosamide PROTACs.Bioorganic & medicinal chemistry letters · 2022
    Article
  17. 3-Molecules (Basel, Switzerland) · 2021
    Article
  18. Article
  19. Article
  20. 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

3 authors.

N G R Dayan ElshanDepartment of Chemistry and Biochemistry, UCLA, Los Angeles, California.ORCID 0000-0001-7830-1477
Matthew B RettigDivision of Hematology/Oncology, VA Greater Los Angeles Healthcare System West LA, Los Angeles, California.ORCID 0000-0002-7394-3056
Michael E JungDepartment of Chemistry and Biochemistry, UCLA, Los Angeles, California.ORCID 0000-0003-1290-8588

Funding

UCLA SPORE IN PROSTATE CANCERP50CA092131 · NCI · UNIVERSITY OF CALIFORNIA LOS ANGELES · PI REITER, ROBERT E · 2002 to 2023
$42.6M
Identification of Inhibitors of the N-Terminal Region of the Androgen ReceptorR01CA164331 · NCI · UNIVERSITY OF CALIFORNIA LOS ANGELES · PI RETTIG, MATTHEW B · 2012 to 2016
$1.3M
NCI NIH HHS P50 CA092131NCI NIH HHS R01 CA164331
6 · The paper itself

Abstract

Prostate cancer (PCa) is the second most common cause of cancer-related mortality in men in the United States. The androgen receptor (AR) and the physiological pathways it regulates are central to the initiation and progression of PCa. As a member of the nuclear steroid receptor family, it is a transcription factor with three distinct functional domains (ligand-binding domain [LBD], DNA-binding domain [DBD], and transactivation domain [TAD]) in its structure. All clinically approved drugs for PCa ultimately target the AR-LBD. Clinically active drugs that target the DBD and TAD have not yet been developed due to multiple factors. Despite these limitations, the last several years have seen a rise in the discovery of molecules that could successfully target these domains. This review aims to present and comprehensively discuss such molecules that affect AR signaling through direct or indirect interactions with the AR-TAD or the DBD. The compounds discussed here include hairpin polyamides, niclosamide, marine sponge-derived small molecules (eg, EPI compounds), mahanine, VPC compounds, JN compounds, and bromodomain and extraterminal domain inhibitors. We highlight the significant in vitro and in vivo data found for each compound and the apparent limitations and/or potential for further development of these agents as PCa therapies.

Indexed as

Signal TransductionAnimalsClinical Trials as TopicDisease ProgressionHumansLigandsProtein DomainsReceptors, AndrogenLigandsReceptors, Androgenandrogen receptorandrogen receptor degradationandrogen receptor DNA-binding domainandrogen receptor signaling axisandrogen receptor transactivation domaincastration-resistant prostate cancerprostate cancer

Identifiers

PMID30565725
PMCPMC6608750

What OpenQuestion holds

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Registered trials

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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.