Early diagnoses and targeted therapies are the crux of successful patient care for almost every cancer. Within this work, we explore various facets of this by studying tumorigenesis and therapeutic development in a variety of cancer models.First, we explored the potential cytotoxicity of compounds previously used for their anti-microbial purposes in order to repurpose them in cancer. We successfully tested two candidate compounds in in vivo xenograft models, which resulted in successful tumor inhibition and characterization of some adverse events associated with treatment. Second, we sought to understand the development and progression of cancer, particularly ovarian cancer, through autotaxin-induced miRNA changes. Using an autotaxin transgenic mouse model, we were able to mimic the progression of a healthy patient to one that had elevated autotaxin that later developed tumors. Changes in serum miRNA expression in these mice were crucial in understanding the functional role of miR-489-3p as not only an indicator of autotaxin elevation and tumorigenesis, but also as an inhibitor of the prominent oncogene MEK1 in malignant cells in vivo and in vitro. Finally, we developed a novel bioengineered particle named antibody-labeled exosomes (Abi-exosomes) that are capable of being fully customized with a surface antibody and loaded miRNA of choice to specifically target cancer cells. Abi-exosomes are capable of achieving significantly higher miRNA delivery efficiency compared to miRNA transfection and exosomes without the antibody-label on the surface. This invention is currently under patent consideration and being explored in the lab as a possible carrier for therapeutics beyond miRNA such as small molecules, proteins, and currently approved therapeutics to further improve target reachability upon delivery.Overall, we have investigated the repurposing of anti-microbial compounds for cancer, sought to understand the underlying biology of miRNA expression driven by autotaxin, and developed a novel therapeutic delivery system in Abi-exosomes to benefit future drug delivery. This will help us better understand the complexity of cancer, and combat it with powerful tools that can improve patient survival in the clinic.