Table 1.
HB-19 and related Nucant pseudopeptides.
| HB-19 |
| Presents pentavalently the pseudo-tripeptide Lysψ(CH2N)-Pro-Arg coupled to the template: H2NLys-Lys-Lys-Gly-Pro-Lys-Glu-Lys-AhxCONH2. |
| Nucant 7: N7 |
| Presents hexavalently the pseudo-tripeptide Lysψ(CH2N)-Pro-Arg coupled to a similar template as in HB-19: Ac-Lys-Ala-Lys-Pro-Gly-Lys-Ala-Lys-Pro-Gly-Lys-Ala-Lys-Pro-Gly-CONH2. |
| Nucant 3: N3 |
| Presents pentavalently the pseudo-tripeptide Lysψ(CH2N)-Pro-Arg coupled to the polypeptide template containing Aib (2-aminoisobutyric acid): Ac-Lys-Aib-Gly-Lys-Aib-Gly-Lys-Aib-Gly-Lys-Aib-Gly-Lys-Aib-Gly-CONH2. |
| Nucant 6: N6 |
| Presents hexavalently the pseudo-tripeptide Lysψ(CH2N)-Pro-Arg (a mixture in L and D configuration) coupled to the polypeptide template containing Aib: Ac-Lys-Aib-Gly-Lys-Aib-Gly-Lys-Aib-Gly-Lys-Aib-Gly-Lys-Aib-Gly-Lys-Aib-Gly-CONH2. |
| Nucant 6L: N6L |
| Presents hexavalently the pseudo-tripeptide Lysψ(CH2N)-Pro-Arg (all bonds in L position) coupled to a polypeptide template as in N6. |
HB-19 and related Nucant pseudopeptides present pentavalently or hexavalently the pseudo-tripeptide Lysψ(CH2N)-Pro-Arg; ψ(CH2N) stands for a reduced peptide [9,16,43,44]. N6L has a similar template as N6 but the Lysψ-Pro units of the pseudo-tripeptide Lysψ(CH2N)-Pro-Arg moieties are all in L configuration, while in N6 the Lysψ-Pro units are a mixture in L and D configuration [44,49]. The nucleolin blocking affinity of constructs that present hexavalently the pseudo-tripeptide Lysψ(CH2N)-Pro-Arg (N6, N6L and N7) is 2-3 fold higher compared to the constructs that present pentavalently the same pseudo-tripeptide (HB-19 and N3).