RLA-5331 is an Iron Activator Containing Anti-androgen
Prostate cancer (PCa) is one of the most prevalent malignancies in the world. Depending on the grade of cancer, a variable percentage of these patients experience progression to castration-resistant prostate cancer (CRPC) within 10 years. However, CRPC can develop into metastatic castration-resistant prostate cancer (MCRPC). Research has shown that...
EPI-7170 is a Potent AR N-terminal Structural Domain Antagonist
EPI-7170, a Ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist. It blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 (0-12 μM, 24 or 48 h) inhibits cell proliferation in VCaP-ENZR and C4-2B-ENZR cells. Additionally, it also enhances the effect of Enzalutamide which has...
EPI-001 is a Selective Inhibitor of Androgen Receptor with Anti-tumor Activity
The androgen receptor (AR) is a type of nuclear receptor and a modular steroid hormone receptor transcription factor. Specifically, the androgen receptor is activated by binding any of the androgenic hormones then translocating into the nucleus. Besides, the main function of the androgen receptor is to regulate gene expression...
IPI-9119 is an Orally Active, Selective and Irreversible FASN Inhibitor
Fatty acid synthase (FASN) is a multi-enzyme protein that catalyzes the synthesis of fatty acids. Its main function is to catalyze the synthesis of palmitate (C16:0) from acetyl CoA and malonyl COA in the presence of NADPH. Specifically, FASN is a key enzyme responsible for the synthesis of fatty...
Y06137 is a Selective BET Inhibitor for Treatment of CRPC
Prostate cancer arises as an androgen driven disease. Therefore the mainstay of systemic therapy for patients with advanced disease is androgen deprivation therapy. Despite of significant responses, nearly all patients ultimately progress and castration resistance ensues. Castration resistant prostate cancer therefore represents a stage in the continuum of the...