Abstract
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
Current Medicinal Chemistry
Title:Converting Peptides into Drug Leads by Lipidation
Volume: 19 Issue: 11
Author(s): L. Zhang and G. Bulaj
Affiliation:
Keywords: ADME, lipidation, lipidated peptide, lipoamino acids, peptide, peptide SAR, peptide secondary structure, peptide selfassembling, peptide serum stability, peptide synthesis
Abstract: 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.
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Cite this article as:
Zhang L. and Bulaj G., Converting Peptides into Drug Leads by Lipidation, Current Medicinal Chemistry 2012; 19 (11) . https://dx.doi.org/10.2174/092986712799945003
DOI https://dx.doi.org/10.2174/092986712799945003 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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