Table 1.
Analog | Tail Amino Acid(s) | Nature of the Side Chain | Inhibition of Uterine Growtha % | Inhibition of T47D Cell Proliferationb % |
---|---|---|---|---|
cyclo[EKTOVNOGN] | None | (AFPep) | 38 ± 3* | 51 ± 4* |
cyclo[EKTOVNOGN] S | S | Hydrophilic | 18 ± 2 | 22 ± 6 |
cyclo[EKTOVNOGN] Y | Y | Hydrophilic | 21 ± 2 | 22 ± 3 |
cyclo[EKTOVNOGN] K | K | Hydrophilic | 17 ± 3 | 18 ± 6 |
cyclo[EKTOVNOGN] E | E | Hydrophilic | 18 ± 3 | 20 ± 2 |
cyclo[EKTOVNOGN] FS | FS | Hydrophilic | 7 ± 3 | NA |
cyclo[EKTOVNOGN] YI | YI | Hydrophilic | 9 ± 5 | 24 ± 3 |
cyclo[EKTOVNOGN] F | F | Hydrophobic | 37 ± 2* | 46 ± 2* |
cyclo[EKTOVNOGN] I | I | Hydrophobic | 39 ± 2* | 55 ± 6* |
cyclo[EKTOVNOGN] FI | FI | Hydrophobic | 46 ± 4* | 66 ± 2* |
Analogs with Disrupted Pharmacophores | ||||
cyclo[EKTOVGOGN] | None | None | 14 ± 5 | NA |
cyclo[EKTOVGOGN] FS | FS | Hydrophilic | 3 ± 7 | NA |
All peptides were administered at a dose of 1 μg/mouse intraperitoneally. Values are presented as mean ± S.E. (n = 5).
T47D human cancer cells were treated with the indicated peptides at a concentration of 1 μM. Values are mean ± S.E. (n = 6).
Peptides with inhibition of more than 25 % significantly inhibited estrogen-stimulated growth.
Statistically significantly different from saline control; p < 0.05 Wilcoxon sum of ranks test.