Current status of androgen receptor-splice variant 7 inhibitor niclosamide in castrate-resistant prostate-cancer
- 7 August 2018
- journal article
- review article
- Published by Springer Nature in Investigational New Drugs
- Vol. 36 (6) , 1133-1137
Abstract
Castrate-Resistant Prostate-Cancer (CRPC) is one of the most common malignancies occurring in men. Unfortunately, even if several recently approved agents clinically improved the outcome of CRPC patients, none of these is curative especially for a splice version of the Androgen Receptor (AR) AR-V7, which is a variant of the receptor constitutively activated and does not require the presence of androgens for the activation AR down-stream pathways. Since high AR-V7 expression is one of the most common features of CRPC, targeting this receptor variant is considered as one of the most promising strategies for treating this disease. Therefore anti-AR-V7 molecules could lead to a potential shift in paradigm in the treatment of CRPC. Niclosamide, an already FDA-approved anti-helminthic drug, was identified as a potent AR-V7 inhibitor in prostate cancer cells. Due to the recent positive preclinical results, niclosamide may be an interesting and novel type of targeted treatments for CRPC. This mini-review outlines the most recent pre- and clinical- data on the current status of niclosamide in the treatment of ARV7-positive CRPC patients.Keywords
This publication has 47 references indexed in Scilit:
- Posttranslational Modification of the Androgen Receptor in Prostate CancerInternational Journal of Molecular Sciences, 2013
- The hinge region in androgen receptor controlMolecular and Cellular Endocrinology, 2012
- Alternatively spliced androgen receptor variantsEndocrine-Related Cancer, 2011
- Androgen receptor signaling and mutations in prostate cancerAsian Journal of Andrology, 2010
- Sipuleucel-T Immunotherapy for Castration-Resistant Prostate CancerNew England Journal of Medicine, 2010
- Ligand-Independent Androgen Receptor Variants Derived from Splicing of Cryptic Exons Signify Hormone-Refractory Prostate CancerCancer Research, 2008
- Splicing of a Novel Androgen Receptor Exon Generates a Constitutively Active Androgen Receptor that Mediates Prostate Cancer Therapy ResistanceCancer Research, 2008
- Drug Insight: testosterone preparationsNature Reviews Endocrinology, 2006
- Interplay between Two Hormone-Independent Activation Domains in the Androgen ReceptorCancer Research, 2006
- Sex hormone-binding globulin: Anatomy and physiology of a new regulatory systemThe Journal of Steroid Biochemistry and Molecular Biology, 1991