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Table 1 Comparing peptidomimetics attributes with native peptides

From: Peptidomimetics in cancer targeting

Characteristics

Peptides

Peptidomimetics

References

Stability

Limited stability toward proteolysis

Higher stability toward proteolysis

Trabocchi (2019), Li Petri et al. (2022), Trabocchi and Guarna (2014)

Interactions/ Specificity

✓ Low selectivity due to high backbone flexibility

✓ Interaction with multiple targets

✓ Higher receptor affinity and selectivity

✓ Pharmacophore-based target selection

Transport system

Rapid excretion, poor cell permeability, lacks specific transport systems due to its relatively high molecular mass

✓ Transports from Peptide transporter 2 (PEPT2) which is a low-capacity/high-affinity proton-coupled cotransporter of diverse di- and tripeptides

✓ The di/tripeptide transporter in the small intestine absorbs some of them

Activity

Limited activity

Higher activity

Kim et al. (2015)

Duration of action

Shorter duration of action

longer duration of action