Effects of small molecules targeting the androgen receptor DNA-binding domain on prostate cancer cell transcriptome

Prostate cancer is a leading cause of cancer related death among men. Current Androgen Receptor (AR) antagonists often target the ligand binding domain (LBD). However, occurrence of resistance to drugs targeting the LBD is common due to emergence of mutations in the LBD or constitutively active variants that lack the LBD itself. Two novel small molecules, VPC-17005 and VPC-14449 targeting the DNA-binding domain have been developed and published previously. In this study, LNCaP cells were treated with one of these drugs or the well-established AR antagonist Enzalutamide, and the transcriptomic changes have been determined using RNA-seq analysis. Overall design: Polyadenylated RNA profiles of LNCaP cells treated with treated with dihydrotestosterone (DHT) plus either DMSO (Control), Enzalutamide, VPC-17005, or VPC-14449, in three biological replicates, obtained using BGISeq500 platform.