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Article

BAY 1024767 blocks androgen receptor mutants found in castration-resistant prostate cancer patients.

Oncotarget - 2 Feb 2016

Sugawara Tatsuo, Lejeune Pascale, Köhr Silke, Neuhaus Roland, Faus Hortensia, Gelato Kathy A, Busemann Matthias, Cleve Arwed, Lücking Ulrich, von Nussbaum Franz, Brands Michael, Mumberg Dominik, Jung Klaus, Stephan Carsten, Haendler Bernard

Abstract excerpt

Androgen receptor (AR) mutations arise in patients developing resistance to hormone deprivation therapies. Here we describe BAY 1024767, a thiohydantoin derivative with strong antagonistic activity against nine AR variants with mutations located in the AR ligand-binding domain (LBD), and against wild-type AR. Antagonism was maintained, though reduced, at increased androgen levels. Anti-tumor efficacy was...

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Methodology Data sources Editorial policy Privacy Delete account & data About Contact Helena Bioinformatics

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Source

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Identifiers

PMID: 26760770
DOI: 10.18632/oncotarget.6864
PMCID: PMC4868737

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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