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Molecular imaging is a newly merged multidisciplinary subject that requires contributions from biology, medical physics, and chemistry/radiochemistry. Integrin α
v
β
3
, a cell adhesion molecule, plays pivotal roles in regulating tumor angiogenesis and the growth of new blood vessels. In this chapter, we use the cell adhesion molecule integrin α
v
β
3
as an example to demonstrate how one can synthesize appropriate arginine–glycine–aspartic acid (RGD) peptide-containing probes for visualizing and quantifying the receptor expression in vivo by means of microPET, microSPECT, and N
IR
fluorescence.