A4B17 is a small molecule that inhibits BAG1L-AR NTD interaction, inhibits the proliferation of AR positive prostate cancer cells.
A4B17 attenuates BAG1L-mediated AR NTD activity, downregulates AR target gene expression.
A4B17 attenuates the expression of AR target genes especially those that regulate oxidative stress and metabolism in a similar manner as a BAG1L knockout.
A4B17 functions more efficaciously than the clinically approved AR antagonist enzalutamide in enhancing the expression of a subset of genes distinct from androgen responsive-genes, a number of which are oxidative stress-induced genes involved in cell death.
A4B17 outperforms enzalutamide in a mouse xenograft model of prostate cancer under castration conditions.
