We report the large-scale syntheses (&gt;10g) of pre-PEGylated Fmoc-Lys and Gln amino acids containing between 1-3 triethylene glycol monomethyl ethers utilizing the most common Fmoc-amino acid building blocks. We have site-spefically incorporated these amino acids into peptides up to 30mers in length of several classes and will discuss the consequences of the PEGylation upon the proteolytic resistance and thermal denaturation measured using circular dichroism spectroscopy. We hope that the ready availability of such pre-PEGylated amino acids will promote their utilization in earlier stages of the hit-to-lead optimization in the drug discovery process for peptide therapeutic candidates.

Use of pre-PEGylated Fmoc-Lys and Gln in synthesis of PEGylated peptide analogs of peptide hormone drug candidates with branched or unbranched short, monodiserse PEGs

255th National Meeting (2018)

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