Recent advances in polymerization strategies have led to the development of novel polymer-(poly)peptide biohybrid materials with potential application in the field of macromolecular therapeutics. In this current work, comb-shaped a-aldehyde poly(monomethoxy polyethylene glycol)methacrylates (p(mPEG)MA) with molecular masses in the 6.5-109 kDa range were prepared and conjugated, via reductive amination, to the Cys1 N-terminus of salmon calcitonin (sCT), a calcitropic hormone currently administered for the treatment of a number of hypercalcaemia-related diseases. The conjugation site was determined by tryptic digestion of the sCT-p(mPEG 1100 )MA biohybrids in conjunction with LC-MS MALDI-TOF spectrometry. Preliminary in vitro biological tests show that the polymer conjugation does not interfere with the biological activity of the sCT.
A general and robust method for the incorporation of aspartates with a thioacid side chain into peptides has been developed. Pseudoproline tripeptides served as building blocks for the efficient fluorenylmethyloxycarbonyl (Fmoc) solid‐phase synthesis of thioacid‐containing peptides. These peptides were readily converted to complex N‐glycopeptides by using a fast and chemoselective one‐pot deprotection/ligation procedure. Furthermore, a novel side reaction that can lead to site‐selective peptide cleavage using thioacids (CUT) was discovered and studied in detail.
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