Table 1.
The effects of IGF1R juxtamembrane domain analogues on the growth of MCF-7 breast cancer cells.
| Peptide | Peptide Sequence | GI50 [µM][[a]] |
TGI [µM] |
|---|---|---|---|
| 1 | Pal-HRKRNNSRLGNG-NH2 | 1.8±0.05 | N/A |
| 2 | Pal-HRKRNNSRLG-NH2 | 1.3±0.05 | N/A |
| 3 | Pal-HRKRNNSRLGNGVLYASVN-NH2 | 1.0±0.05 | 1.55±0.1 |
| 4 | Pal-HRKRNNSRLGNGVLYASVNPEYFSAA-NH2 | 1.0±0.05 | N/A |
| 23 | Pal-HRKRNNSRLGNGVLYASVNP-NH2 | 0.1±0.05 | N/A |
| 5 | Pal-HRKRNNSRLGNGVLYASV-NH2 | 0.45±0.05 | 1.45±0.3 |
| 6 | Pal-VHRKRNNSRLGNGVLYASV-NH2 | 0.25±0.03 | 1.05±0.1 |
| 7 | Pal-HRKRNNSRLGNGVLYAS-NH2 | 1.45±0.1 | 4.1±0.3 |
| 8 | Pal-HRKRNNSRLGNGVLYA-NH2 | 1.4±0.1 | N/A |
| 9 | Pal-HRKRNNSRLGNGVLY-NH2 | 1.65±0.1 | N/A |
| 10 | Pal-HRKRNNSRLGNGVL-NH2 | 1.8±0.1 | N/A |
| 11 | Pal-HRKRNNSRLGNGV-NH2 | 2.5±0.1 | N/A |
| 24 | Pal-VFHRKRNNSRLGNGVLYASVN-NH2 | 0.1±0.05 | 1.1±0.1 |
| 12 | Pal-RKRNNSRLGNGVLYASVN-NH2 | 1.2±0.1 | 2.7±0.3 |
| 13 | Pal-KRNNSRLGNGVLYASVN-NH2 | 0.08±0.007 | 0.5±0.08 |
| 14 | Pal-RNNSRLGNGVLYASVN-NH2 | 0.1±0.004 | 0.4±0.02 |
| 27 | Pal-KRNNSRLGNGVLY-NH2 | 1.1±0.06 | 2.5±0.5 |
| 16 | Pal-RNNSRLGNGVLY-NH2 | 0.07±0.005 | 0.5±0.02 |
| 15 | Pal-NNSRLGNGVLY-NH2 | 0.1±0.01 | 1.5±0.05 |
| 17 | Pal-NSRLGNGVLY-NH2 | 0.2±0.01 | 1.5±0.1 |
| 19 | Pal-SRLGNGVLY-NH2 | 0.15±0.05 | 2.0±0.1 |
| 20 | Pal-RLGNGVLY-NH2 | 0.2±0.006 | N/A |
| 18 | Ac-YLVGNGLRSNNRK-(ε-Pal)[All D-] | 0.04±0.001 | 0.4±0.02 |
| 22 | Pal-YLVGNGLRSNNR-NH2[All D-] | 0.04±0.001 | 0.5±0.025 |
| 21 | Pal-VSAYLVGNGLRSNNR-NH2[All D-] | 0.04±0.001 | 0.1±0.005 |
| IR-2 | Pal-RQPDGPLGPLY-NH2 | 0.06±0.001 | 0.4±0.05 |
[a]
Cells were exposed to compounds for 48 hours and cell number was determined with the help of MTT assay. GI50 corresponds to concentrations causing 50% reduction in growth rate. TGI is a concentration causing total growth inhibition.