Evidence map›Paper›PMID 34473519›Full record

ArticleJournal of medicinal chemistry2021

Discovery of ARD-2585 as an Exceptionally Potent and Orally Active PROTAC Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer.

Weiguo Xiang, Lijie Zhao, Xin Han, Chong Qin, Bukeyan Miao, Donna McEachern, Yu Wang, Hoda Metwally, Paul D Kirchhoff, Lu Wang and 5 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 50 papers.

0numbers the graph read from it
0cells of the map it votes in
50citing papers in PubMed
8.7field-weighted citation impact, top 1% 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

50 citing papers in PubMed, 135 citations in OpenAlex.

  1. Evolving CRBN ligands enhance the drug-like properties of protein degraders.Journal of enzyme inhibition and medicinal chemistry · 2026
    Review
  2. Article
  3. Article
  4. Review
  5. Review
  6. Article
  7. Review
  8. PROTACs therapeutically target the polyglutamine androgen receptor in spinal and bulbar muscular atrophy models.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2025
    Article
  9. Targeting the mutant androgen receptor with PROTACs in spinal and bulbar muscular atrophy.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2025
    Article
  10. Article
  11. Review
  12. Click-constructed modular signal aptamer chimeras enable receptor-independent degradation of membrane proteins.Proceedings of the National Academy of Sciences of the United States of America · 2025
    Article
  13. Review
  14. Article
  15. Property-based optimisation of PROTACs.RSC medicinal chemistry · 2025
    Article
  16. Article
  17. Article
  18. Article
  19. Review
  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

15 authors at 1 institution in 1 country.

Weiguo XiangThe Rogel Cancer Center, University of Michigan, Ann Arbor, Michigan 48109, United States.
Lijie ZhaoThe Rogel Cancer Center, University of Michigan, Ann Arbor, Michigan 48109, United States.
Xin HanThe Rogel Cancer Center, University of Michigan, Ann Arbor, Michigan 48109, United States.ORCID 0000-0003-0904-220X
Chong QinThe Rogel Cancer Center, University of Michigan, Ann Arbor, Michigan 48109, United States.
Bukeyan MiaoThe Rogel Cancer Center, University of Michigan, Ann Arbor, Michigan 48109, United States.
Donna McEachernThe Rogel Cancer Center, University of Michigan, Ann Arbor, Michigan 48109, United States.
Yu WangThe Rogel Cancer Center, University of Michigan, Ann Arbor, Michigan 48109, United States.
Hoda MetwallyThe Rogel Cancer Center, University of Michigan, Ann Arbor, Michigan 48109, United States.
Paul D KirchhoffThe Rogel Cancer Center, University of Michigan, Ann Arbor, Michigan 48109, United States.
Lu WangDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, Ann Arbor, Michigan 48109, United States.
Aleksas MatvekasDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, Ann Arbor, Michigan 48109, United States.
Miao HeDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, Ann Arbor, Michigan 48109, United States.
Bo WenDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, Ann Arbor, Michigan 48109, United States.
Duxin SunDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, Ann Arbor, Michigan 48109, United States.ORCID 0000-0002-6406-2126
Shaomeng WangThe Rogel Cancer Center, University of Michigan, Ann Arbor, Michigan 48109, United States.ORCID 0000-0002-8782-6950
University of Michigan · US

Funding

XenograftP30CA046592 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI Alexey I Nesvizhskii · 1988 to 2026
$178.2M
Tissue/InformaticsP50CA186786 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI Ganesh S Palapattu · 2014 to 2026
$27.6M
NCI NIH HHS P30 CA046592NCI NIH HHS P50 CA186786
6 · The paper itself

Abstract

We report herein the discovery of exceptionally potent and orally bioavailable PROTAC AR degraders with ARD-2585 being the most promising compound. ARD-2585 achieves DC

Indexed as

Adaptor Proteins, Signal TransducingAndrogen Receptor AntagonistsAnimalsAntineoplastic AgentsCell Line, TumorDrug DesignHumansMaleMiceMice, SCIDMolecular StructurePhthalimidesPiperidonesProstatic Neoplasms, Castration-ResistantProteolysisReceptors, AndrogenAdaptor Proteins, Signal TransducingAndrogen Receptor AntagonistsAntineoplastic AgentsAR protein, humanCrbn protein, mousePhthalimidesPiperidonesReceptors, Androgen

Identifiers

PMID34473519
PMCPMC8855934
OpenAlexW3197508711

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.