Development of androgen receptor antagonists with promising activity in castration-resistant prostate cancer

Howard C Shen; Steven P Balk

doi:10.1016/j.ccr.2009.05.005

Development of androgen receptor antagonists with promising activity in castration-resistant prostate cancer

Cancer Cell. 2009 Jun 2;15(6):461-3. doi: 10.1016/j.ccr.2009.05.005.

Authors

Howard C Shen¹, Steven P Balk

Affiliation

¹ Department of Medicine, Hematology-Oncology Division, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA 02115, USA.

PMID: 19477425
DOI: 10.1016/j.ccr.2009.05.005

Abstract

Androgen receptor (AR) continues to play a central role in prostate cancers that relapse after androgen deprivation therapy, but these tumors are refractory to available AR antagonists. In a recent issue of Science, Tran et al. describe an antagonist that prevents AR recruitment to chromatin and shows efficacy in relapsed prostate cancer.

MeSH terms

Androgen Receptor Antagonists
Androgens
Antineoplastic Agents / pharmacology
Antineoplastic Agents / therapeutic use*
Benzamides
Chromatin / metabolism
Humans
Male
Neoplasm Recurrence, Local
Nitriles
Orchiectomy
Phenylthiohydantoin / analogs & derivatives*
Phenylthiohydantoin / pharmacology
Phenylthiohydantoin / therapeutic use
Prostatic Neoplasms / drug therapy*
Prostatic Neoplasms / pathology
Receptors, Androgen / physiology*
Signal Transduction
Transcriptional Activation / drug effects

Substances

Androgen Receptor Antagonists
Androgens
Antineoplastic Agents
Benzamides
Chromatin
Nitriles
Receptors, Androgen
Phenylthiohydantoin
enzalutamide