Inhibition of TSP-1 binding to CD36 by Mal II peptides
Peptide | IC50 | |
---|---|---|
Cell binding | Solid phase | |
nM | ||
Unmodified Mal II | >10,000 | 1,000 |
d-Ser5-Mal II, 19-mer | 6.22 ± 5.02 | 7.4 ± 4.2 |
d-IIe15 Mal II variants | ||
Original 19-mer | 20.8 ± 12.3 | 12.5 ± 3.3 |
Nonapeptide | 15.4 ± 8.9 | 12.8 ± 4.2 |
Ethylamide-capped heptapeptide | 6.8 ± 4.1 | 4.6 ± 3.3 |
Retro-inverso | 11.2 ± 5.8 | 28.4 ± 5.4 |
Binding of 125I-labeled TSP-1 (20 μg/ml) to a confluent monolayer of Bowes melanoma cells expressing CD36 or to solid-phase fusion protein expressing CD36 amino acids 93 to 155 immobilized on plastic was competed with increasing concentrations of hyperpurified inactive Mal II or various Mal II analogs. IC50 values were determined using the ENZFITTER curve-fitting program.