Table 1.
Composition of bivalent ligands
| Compound | Androgen | Linker | AF-2 peptide |
|---|---|---|---|
| Linker length | |||
| SPEP-1 | DHT | GGGGG | SSRFGSLFAG |
| SPEP-2 | DHT | GGGGGG | SSRFGSLFAG |
| SPEP-3 | DHT | GGGG | SSRFGSLFAG |
| SPEP-9 | DHT | GGGGGGGGGG | SEKFAALFQSY |
| Modified FXXLF | |||
| SPEP-4 | DHT | GGGGG | SEKFQNLFQSY |
| SPEP-5 | DHT | GGGGG | SEKFAALFQSY |
| SPEP-6 | DHT | GGGGG | SEKFKLLFQSY |
| γ-Abu-Ahx | |||
| SPEP-10 | DHT | G-γ-Abu-Ahx | SEKFAALFQSY |
| SPEP-27 | DHT | G-γ-Abu-Ahx | SEKFKLLFQSY |
| Unnatural amino acids in AF-2 peptide | |||
| SPEP-11 | DHT | GGGGG | SEK-Cha-AALFQSY 1 |
| SPEP-12 | DHT | GGGGG | SEKFAAL-Nal-QSY 2 |
| SPEP-13 | DHT | GGGGG | SEK-Cha-AAL-Nal-QSY |
| SPEP-19 | DHT | G-γ-Abu-Ahx | SEK-Cha-AAL-Nal-QSY |
| SPEP-21 | DHT | G-γ-Abu-Ahx | SEK-Nal-AAL-Nal-QSY |
| SPEP-22 | DHT | G-γ-Abu-Ahx | SEK-Cha-AAL-Cha-QSY |
| XXLL motif | |||
| SPEP-23 | DHT | G-γ-Abu-Ahx | SEKLAALLQSY |
| SPEP-24 | DHT | G-γ-Abu-Ahx | SEKLAALFQSY |
| SPEP-26 | DHT | G-γ-Abu-Ahx | SHKLVQLLQSY |
| AF-2 peptide, reduced charge | |||
| SPEP-20 | DHT | G-γ-Abu-Ahx | SNQFAALFQSY |
| SPEP-25 | DHT | G-γ-Abu-Ahx | SE-LYS(z)-FAALFQSY 3 |
| SPEP-29 | DHT | G-γ-Abu-Ahx | SQKFAALFQSY |
| SPEP-35 | DHT | G-γ-Abu-Ahx | SEQFAALFQSY |
| SPEP-36 | DHT | G-γ-Abu-Ahx | SNKFAALFQSY |
| Fatty acid | |||
| SPEP-38 | DHT | G-γ-Abu-Ahx | SEK(octanoic-acid)FAALFQSY |
| SPEP-41 | DHT | G-γ-Abu-Ahx | SEK(hexanoic-acid)LAALFQSY |
| SPEP-42 | DHT | G-γ-Abu-Ahx | SEK(octanoic-acid)LAALFQSY |
| SPEP-43 | DHT | G-γ-Abu-Ahx | SEK(decanoic acid)LAALFQSY |
| Stapled AF-2 peptide | |||
| HGSF-1 | DHT | G-γ-Abu-Ahx | SEKFAALFASY4 |
| HGSF-2 | DHT | G-γ-Abu-Ahx | SEKLAALFASY4 |
1Cha, Cyclohexyl Alanine,
2Nal, Napthyl Alanine,
3N-ε-benzyloxycarbonyl lysine
4The underlined residues are the olefinic alanines that were stapled