Ontology highlight
ABSTRACT:
SUBMITTER: Sugawara T
PROVIDER: S-EPMC4868737 | biostudies-literature | 2016 Feb
REPOSITORIES: biostudies-literature
Sugawara Tatsuo T Lejeune Pascale P Köhr Silke S Neuhaus Roland R Faus Hortensia H Gelato Kathy A KA Busemann Matthias M Cleve Arwed A Lücking Ulrich U von Nussbaum Franz F Brands Michael M Mumberg Dominik D Jung Klaus K Stephan Carsten C Haendler Bernard B
Oncotarget 20160201 5
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 evidenced in vivo in the KuCaP-1 prostate cancer model which bears the W741C bicalutamide re ...[more]