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With the discovery of a number of therapeutically important and promising native peptides and protein fragments, the clinical development of peptide and peptidomimetics drug leads has become a priority of academia as well as the pharmaceutical industry. This expanding family of drug leads still has important restraints towards clinical use due to the physicochemical properties of most bioactive peptides. The increased size and faster degradation compared to traditional non-peptidic drugs only partially explain why many peptide-based drugs have not reached the clinical trial stage.

A common obstacle to routine therapeutic use of peptides is that these molecules cannot cross certain biological barriers. Most importantly, peptides rarely can be administered by the oral route, since they are not absorbed, or undergo digestion and inactivation in the gastrointestinal tract.

The phos ...