Cytotoxic activity of HTI-286 in prostate cancer. Homo sapiens

HTI-286, an analogue of hemiasterlin, interferes with microtubule dynamics and circumvents transport-based resistance to taxanes. In this study we evaluate the inhibitory effects of HTI-286 on human prostate cancer growth in vitro and in different in vivo models. The results show that HTI-286 is a potent inhibitor of proliferation and induced marked increases in apoptotic rates in all cell lines tested. Despite similar transcriptomic changes regarding cell death and cell cycle-regulating genes after exposure to HTI-286 or docetaxel, the gene array revealed distinct molecular signatures for both compounds. Keywords: Drug comparison Overall design: LNCaP cells of the same passage were treated in 14 cm dishes for 72 h with 0.75 nM HTI-286 or 3 nM docetaxel and their corresponding vehicle controls (1.5 or <-1.5 in 3 of 3 experiments were then categorized by function using Ingenuity Pathways Analysis 5.0 (Ingenuity Systems, Redwood City, CA).