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. Author manuscript; available in PMC: 2012 Dec 1.
Published in final edited form as: Peptides. 2011 Oct 12;32(12):2504–2510. doi: 10.1016/j.peptides.2011.10.007

Table 1.

Antiestrotrophic activity of AFPep and ring-and-tail analogs.

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
a

All peptides were administered at a dose of 1 μg/mouse intraperitoneally. Values are presented as mean ± S.E. (n = 5).

b

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.