The integration of advances in molecular biology, synthetic chemistry and visualization techniques has catapulted imaging into a molecular-functional realm, so that imaging is finding basic-research, preclinical and translational applications in cancer. Currently, molecular-imaging capabilities include the ability to image gene expression, receptors, signaling pathways, apoptosis, multidrug resistance and the extracellular matrix (ECM). Functional-imaging capabilities include the ability to assess angiogenesis, hypoxia and metabolism. Traditionally, imaging has played an important role in cancer diagnosing and determining response to treatment. However, it is the realization of the goal of noninvasively visualizing molecules and molecular pathways and relating these to function that makes multi-modality imaging such an exciting and powerful means for studying a multifaceted disease such as cancer.