Evidence map›Paper›PMID 33741738›Full record

ArticleProceedings of the National Academy of Sciences of the United States of America2021

Paradoxical androgen receptor regulation by small molecule enantiomers.

Katherin Patsch, Chao Liu, Grzegorz Zapotoczny, Yuanye Sun, Harish Sura, Nolan Ung, Ren X Sun, Bethany Haliday, Chen Yu, Mayada Aljehani and 5 more

Open access · greenAbstract read
In one paragraph

Article in Proceedings of the National Academy of Sciences of the United States of America, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.4field-weighted citation impact, top 36% 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

4 citing papers in PubMed, 3 citations in OpenAlex.

  1. Article
  2. Amino-Acid-Derived Androgen Receptor Modulators.ACS medicinal chemistry letters · 2026
    Article
  3. Review
  4. Paradoxical androgen receptor regulation by small molecule enantiomers.Proceedings of the National Academy of Sciences of the United States of America · 2021
    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.

Katherin PatschLawrence J. Ellison Institute for Transformative Medicine, University of Southern California, Los Angeles, CA 90064.ORCID 0000-0002-8074-9219
Chao LiuDepartment of Chemistry, Dana and David Dornsife College of Letters, Arts, and Sciences, University of Southern California, Los Angeles, CA 90089.ORCID 0000-0002-7411-7821
Grzegorz ZapotocznyLawrence J. Ellison Institute for Transformative Medicine, University of Southern California, Los Angeles, CA 90064.ORCID 0000-0003-2036-2992
Yuanye SunDepartment of Chemistry, Dana and David Dornsife College of Letters, Arts, and Sciences, University of Southern California, Los Angeles, CA 90089.
Harish SuraLawrence J. Ellison Institute for Transformative Medicine, University of Southern California, Los Angeles, CA 90064.
Nolan UngLawrence J. Ellison Institute for Transformative Medicine, University of Southern California, Los Angeles, CA 90064.ORCID 0000-0002-1162-2185
Ren X SunLawrence J. Ellison Institute for Transformative Medicine, University of Southern California, Los Angeles, CA 90064.
Bethany HalidayLawrence J. Ellison Institute for Transformative Medicine, University of Southern California, Los Angeles, CA 90064.ORCID 0000-0001-9907-5966
Chen YuLawrence J. Ellison Institute for Transformative Medicine, University of Southern California, Los Angeles, CA 90064.ORCID 0000-0001-8425-9930
Mayada AljehaniLawrence J. Ellison Institute for Transformative Medicine, University of Southern California, Los Angeles, CA 90064.ORCID 0000-0002-0090-2691
Jerry S H LeeLawrence J. Ellison Institute for Transformative Medicine, University of Southern California, Los Angeles, CA 90064.ORCID 0000-0003-1515-0952
Boris A KashemirovDepartment of Chemistry, Dana and David Dornsife College of Letters, Arts, and Sciences, University of Southern California, Los Angeles, CA 90089.ORCID 0000-0001-7175-9960
David B AgusLawrence J. Ellison Institute for Transformative Medicine, University of Southern California, Los Angeles, CA 90064.ORCID 0000-0002-7499-7822
Charles E McKennaLawrence J. Ellison Institute for Transformative Medicine, University of Southern California, Los Angeles, CA 90064; mckenna@usc.edu druderman@ellison.usc.edu.ORCID 0000-0002-3540-6663
Daniel RudermanLawrence J. Ellison Institute for Transformative Medicine, University of Southern California, Los Angeles, CA 90064; mckenna@usc.edu druderman@ellison.usc.edu.ORCID 0000-0001-5787-5009
University of Southern California · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Small molecules that target the androgen receptor (AR) are the mainstay of therapy for lethal castration-resistant prostate cancer (CRPC), yet existing drugs lose their efficacy during continued treatment. This evolution of resistance is due to heterogenous mechanisms which include AR mutations causing the identical drug to activate instead of inhibit the receptor. Understanding in molecular detail the paradoxical phenomenon wherein an AR antagonist is transformed into an agonist by structural mutations in the target receptor is thus of paramount importance. Herein, we describe a reciprocal paradox: opposing antagonist and agonist AR regulation determined uniquely by enantiomeric forms of the same drug structure. The antiandrogen BMS-641988, which has (

Indexed as

Drug DiscoveryDrug Screening Assays, AntitumorAndrogen Receptor AntagonistsAndrogensCell Line, TumorCells, CulturedDose-Response Relationship, DrugHumansModels, MolecularMolecular StructureProtein BindingReceptors, AndrogenStereoisomerismStructure-Activity RelationshipAndrogen Receptor AntagonistsAndrogensAR protein, humanReceptors, Androgenandrogen receptorcancerchiralitydrug testing

Identifiers

PMID33741738
PMCPMC8000581
OpenAlexW3139108010

What OpenQuestion holds

Textmetadata
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.