solution (1 mL) of
the commercially available integrin αvβ3 targeting peptide c(RGDyK) (0.030 g, 0.048 mmol) (Peptides
International Inc., Kentucky) was added N-succinimidyl
3-(2-pyridyldithio)-propionate (0.020 g, 0.064 mmol) (Thermo Scientific,
IL) and the solution was allowed to stir for 6 h. The solvent was
evaporated, the product neutralized and purified by reverse phase
HPLC using water and acetonitrile solvent mixture and lyophilized.
The resultant white solid was dissolved in DMF (1.0 mL) and dithiothreitol
(0.010 g, 0.065 mmol) was then added. The solution was allowed to
stir for 3 h. The solvent was evaporated and the product neutralized
and purified by reverse phase HPLC using water and acetonitrile solvent
mixture to give c(RGDyK)-SH as a white solid (0.103 g, 0.014 mmol,
29.5%). MS (MALDI) m/z calcd for
C30H45N9O9S: 707.3; found:
708.3 ([M + H]+).