Research is currently underway worldwide into the development of receptor-specific radiopharmaceuticals for the imaging and treatment of cancer. The successful clinical development of radiolabeled somatostatin analogs for imaging and treatment of cancers overexpressing somatostatin receptors has catalyzed further preclinical investigation of other radiolabeled peptides for molecular imaging and peptide-receptor radiotherapy, including such well-studied peptide vectors as cholecystokinin, neurotensin, bombesin and RGD peptides. Within this larger context, this article will focus on the current status of two more recent additions to the list of molecular imaging targets - guanylate cyclase C, a specific marker for colorectal cancer, and the urokinase plasminogen activator receptor, a cell-surface receptor overexpressed in diverse cancer types.