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The delivery of radioisotopes to tumor cells in vivo involves a complex interplay of tumor target biology and radiopharmaceutical pharmacology and pharmacokinetics. A radiopharmaceutical agent is typically composed of a tumor-specific targeting moiety (the “binder”), linked to a chelator cage housing the radioactive ion, in the case of transition metal or rare earth metal isotopes. In this chapter, we focus on the binder moiety chemical matter and approaches to identifying de novo novel binders using high throughput peptidomimetic libraries of macrocycles.

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