TABLE 1.
DBF-based compounds
Solubility was assessed at 5, 20, 50, and 100 µM compound in 20 mM Kphos buffer, pH 7.0, with 1% TFE, 1% glycerol, 2% NP40, and 150 mM NaCl. Solubilities are reported as >100 µM or <50 µM, depending upon whether a given compound followed Beer’s law up to 100 µM or only up to 50 µM, respectively. Proliferation of endothelial cells is reported in terms of IC50 values (µM) for each compound. Bold letters indicate amino acids in the sequence that have been modified/changed.
Name | Sequence | Solubility | IC50 |
---|---|---|---|
µM | µM | ||
Anginex | ANIKLSVQMKLFKRHLKWKIIVKLND | >100 | 4 |
6DBF7 | SVQMKL-[DBF]-IIVKLND | <50 | 22 |
Single alanine substitution of 6DBF7 | |||
DB1 | AVQMKL-[DBF]-IIVKLND | >100 | 19 |
DB2 | SAQMKL-[DBF]-IIVKLND | <50 | 64 |
DB3 | SVAMKL-[DBF]-IIVKLND | <50 | 28 |
DB4 | SVQAKL-[DBF]-IIVKLND | >100 | 13 |
DB5 | SVQMAL-[DBF]-IIVKLND | >100 | 202 |
DB6 | SVQMKA-[DBF]-IIVKLND | >100 | 27 |
DB7 | SVQMKL-[DBF]-AIVKLND | <50 | 19 |
DB8 | SVQMKL-[DBF]-IAVKLND | >100 | 29 |
DB9 | SVQMKL-[DBF]-IIAKLND | >100 | 31 |
DB10 | SVQMKL-[DBF]-IIVALND | >100 | 74 |
DB11 | SVQMKL-[DBF]-IIVKAND | <50 | 28 |
DB12 | SVQMKL-[DBF]-IIVKLAD | <50 | 22 |
DB13 | SVQMKL-[DBF]-IIVKLNA | <50 | 10 |
Double alanine substitution of 6DBF7 | |||
DB14 | SVQAKL-[DBF]-IIVKLNA | >100 | 8 |
DB15 | SVQAKL-[DBF]-AIVKLND | <50 | 9 |
DB16 | SVQMKL-[DBF]-AIVKLNA | >100 | 5 |
Triple alanine substitution of 6DBF7 | |||
DB17 | SVQAKL-[DBF]-AIVKLNA | <50 | 9 |
Norleucine substitution for Lys in 6DBF7 | |||
DB18 | SVQMNleL-[DBF]-IIVKLNA | <50 | 9 |
DB30 | SVQMKL-[DBF]- NleIVKLNA | <50 | 3 |
DB19 | SVQMKL-[DBF]-IIVNleLNA | <50 | 15 |
DB29 | SVQMNleL-[DBF]-IIVNleLNA | <50 | 20 |
Norvaline substitution for Val, Met, Leu, or Ile (branched to linear alkyl) in 6DBF7 | |||
DB25 | SNvaQMKL-[DBF]-IIVKLNA | >100 | 10 |
DB21 | SVQNvaKL-[DBF]-IIVKLNA | >100 | 3 |
DB22 | SVQMKNva-[DBF]-IIVKLNA | <50 | 4 |
DB23 | SVQMKL-[DBF]- NvaIVKLNA | <50 | 3 |
DB26 | SVQMKL-[DBF]-IIVKNvaNA | <50 | 5 |
DB24 | SVQMKL-[DBF]-IINvaKLNA | <50 | 3 |
DB27 | SVQMKL-[DBF]-IIVKLNNva | <50 | 4 |
DB28 | SVQNvaKNva-[DBF]- NvaINvaKLNA | <50 | 5 |