Converting Peptides into Drug Leads by Lipidation
L. Zhang and G. Bulaj
Affiliation: 421 Wakara Way, Suite 360, Salt Lake City, Utah 84108, USA.
Lipidation is a posttranslational modification of proteins that has also found its use in designing peptide drugs. The presence of
a lipid group in peptides modulates their hydrophobicity, secondary structures and self-assembling propensities while retaining their
abilities to bind to target receptors. Lipidation improves peptides’ metabolic stability, membrane permeability, bioavailability, and
changes peptides’ pharmacokinetic and pharmacodynamic properties. Herein, we review the applications of various lipidation strategies
in peptide drug design, the effects of the chain length and anchor position of fatty acids in peptide lipidation, the physicochemical and
biological properties of selected lipidated peptides and the synthesis strategies for peptide lipidation.
Keywords: ADME, lipidation, lipidated peptide, lipoamino acids, peptide, peptide SAR, peptide secondary structure, peptide selfassembling,
peptide serum stability, peptide synthesis
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