VPC-13566 is Binding Function 3 (BF3)-specific inhibitor of the androgen receptor.
VPC-13566 is Binding Function 3 (BF3)-specific inhibitor of the androgen receptor. VPC-13566 potently inhibits AR transcriptional activity by displacement of the BAG1L peptide from the BF3 pocket. VPC-13566 inhibits the growth of various prostate cancer cell lines including an enzalutamide-resistant cell line and inhibits the growth of AR-dependent prostate cancer xenograft in mice.
Molecular cancer therapeutics, 15(12), 2987-2999 (2016-10-22)
Understanding the impact of BRAF signaling inhibition in human melanoma on key disease mechanisms is important for developing biomarkers of therapeutic response and combination strategies to improve long-term disease control. This work investigates the downstream metabolic consequences of BRAF inhibition
The androgen receptor (AR) is a pivotal drug target for the treatment of prostate cancer, including its lethal castration-resistant (CRPC) form. All current non-steroidal AR antagonists, such as hydroxyflutamide, bicalutamide, and enzalutamide, target the androgen binding site of the receptor
Journal of molecular endocrinology, 63(3), 175-185 (2019-08-14)
Oxidative stress (OS) is a major problem during in vitro culture of embryos. Numerous studies have shown that melatonin, which is known to have antioxidant properties, prevents the occurrence of OS in embryos. However, the molecular mechanisms by which melatonin
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