Molecular imaging is a bioimaging that can detect biochemically and genetically relevant events in molecular level in cells and tissues via quantitative imaging signal. Molecular imaging provides potential advantages to examine early diagnosis of specific diseases, to screen new candidates of a drug, to monitor therapeutic effects in real time, and to communicate with both diagnosis and therapeutics. These diverse advantages of molecular imaging can be allowed by development of nanoplatform technology. The nanoplatform-based probes for molecular imaging is widely investigated to grant multimodal molecular imaging and drug delivery together with medical imagings, which includes the issues of biocompatibility, targeting moiety, proteasespecific peptide substrate, quenching/dequenching system etc. In this paper, nanoplatformbased probes are reviewed in aspects of cancer targeting for diagnosis and therapy and multimodal molecular imaging with inorganic/organic hybrid nanoparticles..