We have led a joint laboratory since October 1999 and published over 180 original peer-reviewed research manuscripts as a collaborative scientific effort. Over 110 patents have been filed worldwide, based on intellectual property developed in our laboratory, initially at The University of Texas, M. D. Anderson Cancer Center and currently at The University of New Mexico. Our central working hypothesis is that normal or diseased tissues show differential protein expression in the human vascular endothelium, which offers the potential to develop novel diagnostic, imaging, and therapeutic strategies. Our research program uses combinatorial peptide- and antibody-based library selection to discover, validate, and exploit the biochemical diversity of endothelial cell surface receptors to generate novel vascular-targeted pharmacologies. Translational applications of our work have led to the development of 2 first-in-man clinical trials. The Food and Drug Administration (FDA) granted “safe-to-proceed” status for our first vascular-targeted IND in 2009. This first-in-human study with a cohort of metastatic prostate cancer patients is complete and the results are in press. This trial successfully met drug localization and activity end points based on analyses of patient bone metastasis at multiple dose levels. The filing of a second IND, also sponsored by philanthropy, is now an active Phase I study to evaluate an anti-obesity drug in castrate-resistant prostate patients with no standard treatment options. Three other drugs are in pre-IND stage, and several others are in the pre-clinical laboratory phase. Long-term, the broader vision of our research is to generate a large-scale receptor map of the human vasculature.