Table 1.
Analogues of peptide 1 (LXW7) and Their IC50*
| Peptide # (Peptide name) | Sequences | IC50(μM) | Peptide # (Peptide name) | Sequences | IC50(μM) |
|---|---|---|---|---|---|
| 1 (LXW7) | cGRGDdvc-NH2 | 0.46 | 1 (LXW7) | cGRGDdvc-NH2 | 0.46 |
| 2 (LXW9) | CGRGDdvc-NH2 | 4.62 | 22 (LXW90) | R5-cGRGDdvc-NH2 | 1.4 |
| 3 (LXW10) | cGRGDdvC-NH2 | 7.45 | 23 (LXW80) | R6-cGRGDdvc-NH2 | 0.50 |
| 4 (LXW11) | CGRGDdvC-NH2 | >20 | 24 (LXW81) | R7-cGRGDdvc-NH2 | 1.36 |
| 5 (LXW20) | DPen-GRGDdvc-NH2 | 5.04 | 25 (LXW82) | R8-cGRGDdvc-NH2 | 1.14 |
| 6 (LXW21) | cGRGDdv-DPen-NH2 | 2.57 | 26 (LXW83) | R9-cGRGDdvc-NH2 | 0.74 |
| 7 (LXW19) | DPen-GRGDdv-DPen-NH2 | 1.86 | 27 (LXW85) | R10-cGRGDdvc-NH2 | 0.55 |
| 8 (LXW13) | caRGDdvc-NH2 | 3.57 | 28 (LXW86) | R11-cGRGDdvc-NH2 | 0.56 |
| 9 (LXW15) | c-βala-RGDdvc-NH2 | 5.06 | 29 (LXW92) | R12-cGRGDdvc-NH2 | 1.5 |
| 10 (LXW51) | cG-HoArg-GDdvc-NH2 | >20 | 30 (LXW89) | R13-cGRGDdvc-NH2 | 0.76 |
| 11 (LXW59) | cG-Agb-GDdvc-NH2 | >20 | 31 (LXW84) | R14-cGRGDdvc-NH2 | 0.64 |
| 12 (LXW58) | cG-Agp-GDdvc-NH2 | >20 | 32 (LXW14) | c-Sar-RGDdvc-NH2 | 1.92 |
| 13 (LXW25) | cGRGDd-DAbu-c-NH2 | 0.64 | 33 (LXW53) | cG-(NMe)Arg-GDdvc-NH2 | 0.63 |
| 14 (LXW26) | cGRGDdic-NH2 | 1.84 | 34 (LXW54) | cGR-Sar-Ddvc-NH2 | >20 |
| 15 (LXW16) | cGRGDd-DAgl-c-NH2 | 2.38 | 35 (LXW55) | cGRG-(NMe)Asp-dvc-NH2 | >20 |
| 16 (LXW17) | cGRGDd-DPra-c-NH2 | 2.46 | 36 (LXW24) | cGRGD-D(NMe)Asp-vc-NH2 | 10 |
| 17 (LXW18) | cGRGDd-DBug-c-NH2 | 0.31 | 37 (LXW22) | cGRGDd-D(NMe)Val-c-NH2 | 0.63 |
| 18 (LXW12) | R1-cGRGDdvc-NH2 | 1.12 | 38 (LXW63) | cGRGDd-DIng-c-NH2 | 0.32 |
| 19 (LXW76) | R2-cGRGDdvc-NH2 | 0.71 | 39 (LXW48) | cGRGDd-DBta-c-NH2 | 0.25 |
| 20 (LXW77) | R3-cGRGDdvc-NH2 | 2.7 | 40 (LXW64) | cGRGDd-DNal1-c-NH2 | 0.07 |
| 21 (LXW78) | R4-cGRGDdvc-NH2 | 2.9 | 41 (LXW65) | cGRGDd-DNal2-c-NH2 | 0.13 |
*
IC50 of the peptide is the concentration of peptide needed to inhibit 0.5 μM biotinylated LXW7 binding to K562/αvβ3+ cells by half.