G. Saberwal et al., STUDIES ON THE SYNTHESIS OF THE TOXINS, PARDAXIN, DELTA-TOXIN AND THEIR ANALOGS BY SOLID-PHASE METHODS, Proceedings of the Indian Academy of Sciences. Chemical sciences, 106(5), 1994, pp. 1109-1121
Studies in our laboratory have been directed towards understanding the
mechanism of action of two hydrophobic toxins, pardaxin comprising 33
residues and delta-toxin comprising 26 residues. Since isolation of t
hese peptides in large amounts from natural sources is not convenient,
we have explored synthetic approaches to get these peptides as well a
s their analogs. We have used chemistry specific to fluorenylmethoxyca
rbonyl (Fmoc) and t-butyloxycarbonyl (Boc) amino acids. Synthesis spec
ific for Fmoc amino acids was carried out manually as well as on a sem
i-automated continuous now peptide synthesizer. Synthesis specific for
Boc amino acids was carried out manually. The protocols used by us ha
ve yielded 15-33 residue peptides which are of high purity. Even in pe
ptides where heterogeneity was present, pure peptide could be obtained
in good yields using simple gradients in fast performance liquid chro
matography. The synthesis of pardaxin, delta-toxin and several analogs
should help in identifying the molecular determinants of biological a
ctivity.