yk-4-279 and Body-Weight

The aim of the current study was to determine the effects of the ERG small-molecule inhibitor YK-4-279 on ERG. ERG activity was blocked using YK-4-279 in three subcutaneously-implanted ERG. Administration of YK-4-279 decreased TV (p=0.026), proliferation (p=0.0038) and PSA (p=0.022) in Severe Combined Immunodeficiency (SCID) mice bearing LuCaP 23.1 tumors. LuCaP 86.2, LuCaP 35 and LuCaP 96 showed no significant changes in TV, or PSA. Mineralocorticoid receptor (MR) and MR-direct target genes were up-regulated in treatment-resistant LuCaP 86.2 and LuCaP 35 PDX.. YK-4-279 decreased ERG

Topics: Animals; Apoptosis; Body Weight; Cell Proliferation; Gene Expression; Heterografts; Humans; Indoles; Male; Mice; Mice, SCID; Prostate-Specific Antigen; Prostatic Neoplasms; Receptors, Mineralocorticoid; Transcriptional Activation; Transcriptional Regulator ERG; Tumor Burden; Up-Regulation