Histone deacetylase inhibitors (HDACIs) can disrupt the viability of prostate cancer (PCa) cells through modulation of the cytosolic androgen receptor (AR) chaperone protein heat shock protein 90 (HSP90). However, toxicities associated with their pleiotropic effects could contribute to the ineffectiveness of HDACIs in PCa treatment. We designed hybrid molecules containing partial chemical scaff...

Various novel androgen receptor (AR) targeting drugs have been developed recently and have shown beneficial effects on survival in patients with metastatic castration-resistant prostate cancer (mCRPC). However, no consensus has been reached regarding which of these agents provides the most favorable oncological outcomes. Here, we aimed to compare the efficacy of novel AR-targeted agents by perf...

BACKGROUND The treatment of metastatic castration-resistant prostate cancer has changed with the introduction of radium-223, cabazitaxel, abiraterone and enzalutamide. To assess value for money, their cost effectiveness in patients with metastatic castration-resistant prostate cancer previously treated with docetaxel from the Dutch societal perspective was investigated. METHODS A cost-effecti...

Triple-negative breast cancer (TNBC) has the lowest 5-year survival rate of invasive breast carcinomas, and currently there are no approved targeted therapies for this aggressive form of the disease. The androgen receptor (AR) is expressed in up to one third of TNBC and we find that all AR(+) TNBC primary tumors tested display nuclear localization of AR, indicative of transcriptionally active r...

To the Editor: In the randomized trial reported by Scher et al. (Sept. 27 issue),1 the administration of enzalutamide, an androgen-receptor–signaling inhibitor, was associated with an increased incidence of headache, as compared with placebo, in patients with castration-resistant prostate cancer. Androgens are implicated in the pathogenesis of migraine; thus, it is important to understand wheth...

Castration-resistant prostate cancer (CRPC) remains dependent on androgen receptor (AR) signaling. Alternative splicing of the AR to generate constitutively active, ligand-independent variants is one of the principal mechanisms that promote the development of resistance to next-generation antiandrogens such as enzalutamide. Here, we demonstrate that the splicing factor heterogeneous nuclear RNA...

Triple-negative breast cancer (TNBC) has the lowest 5-year survival rate of invasive breast carcinomas, and currently there are no approved targeted therapies for this aggressive form of the disease. The androgen receptor (AR) is expressed inup toone third of TNBC and we find that all ARþ TNBC primary tumors tested display nuclear localization of AR, indicative of transcriptionally active recep...

You have accessJournal of UrologyProstate Cancer: Basic Research & Pathophysiology I (MP33)1 Sep 2021MP33-16 INCREASED GLYCOLYSIS AS A POTENTIAL MECHANISM FOR ENZALUTAMIDE-RESISTANCE IN PROSTATE CANCER Sayani Bhattacharjee, Jonathan Doan, Rebecca Wynn, and Nagalakshmi Nadiminty BhattacharjeeSayani Bhattacharjee More articles by this author , DoanJonathan Doan WynnRebecca Wynn NadimintyNagalaksh...

UNLABELLED Next-generation antiandrogen therapies, such as enzalutamide and abiraterone, have had a profound impact on the management of metastatic castration-resistant prostate cancer (mCRPC). However, mCRPC patients invariably develop resistance to these agents. Here, a series of clonal cell lines were developed from enzalutamide-resistant prostate tumor xenografts to study the molecular mech...

INTRODUCTION This study aims to make an indirect comparison between enzalutamide and abiraterone acetate for mCRPC post-docetaxel. METHODS A search for published phase 3 trials was performed with PubMed. Indirect comparisons of enzalutamide (AFFIRM) to abiraterone acetate (COU-AA-301) on outcomes overall survival (OS), time to prostate-specific-antigen (PSA) progression, radiographic progress...