One of the major problems in classic chemotherapy is the non-specific toxicity of most anticancer agents against normal cells. The specific targeting of tumors has been the main challenge in research on cancer therapy and diagnosis. Presently, innovative tumor-specific therapies address tumor cells via tumor associated antigens, specifically expressed or over expressed on tumor cells, and deliver cytotoxic moieties directly producing tumor cell death. The observation that receptors for different endogenous regulatory peptides are expressed in a number of primary human cancers opened new perspectives on the use of synthetic peptides for tumor-selective targeting. In fact, anticancer drugs or radiotracers have been coupled to analogs of many regulatory peptides. Nonetheless, the use of peptides in vivo has largely been limited by their short half-life.
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