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.
Export Options
About this article
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 |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Functional Imaging of Evaluation of Diabetic Gastroparesis
Current Diabetes Reviews EDITORIAL [Hot Topic-I: Molecular and Pharmacological Aspects of Existing and Experimental Bone Anabolic Therapies (Guest Editor: Naibedya Chattopadhyay)]
Current Molecular Pharmacology Biosynthetic Pathways of Plastid-Derived Organelles as Potential Drug Targets Against Parasitic Apicomplexa
Current Drug Targets - Immune, Endocrine & Metabolic Disorders Targeting <i>Plasmodium Metabolism</i> to Improve Antimalarial Drug Design
Current Protein & Peptide Science Anti-cancer and Anti-angiogenic Properties of Various Natural Pentacyclic Tri-terpenoids and Some of their Chemical Derivatives
Current Organic Chemistry Molecular Imaging of Cancer with Radiolabeled Peptides and PET
Anti-Cancer Agents in Medicinal Chemistry Factors Influencing Adherence Among Youth with Type-1-Diabetes Mellitus - The Hungarian Case
Current Diabetes Reviews Imaging Assessment of Local Brain Metabolic Response to Changing Load During Exercise in Humans
Current Medical Imaging Editorial (Thematic Issue: Antiplatelet Treatment in Cardiovascular Disease: New Insights)
Current Pharmaceutical Design Dextran-based Nanocarriers for Delivery of Bioactives
Current Pharmaceutical Design Patients’ Induced Pluripotent Stem Cells to Model Drug Induced Adverse Events: A Role in Predicting Thiopurine Induced Pancreatitis?
Current Drug Metabolism Diet Effects on Atherosclerosis in Mice
Current Drug Targets Food-Derived Advanced Glycation end Products (AGEs): A Novel Therapeutic Target for Various Disorders
Current Pharmaceutical Design Testosterone, Estradiol, and Sex Hormone-Binding Globulin in Alzheimer’s Disease: A Meta-Analysis
Current Alzheimer Research Elevated Urinary Tissue Inhibitor of Metalloproteinase-2 and Insulin-Like Growth Factor Binding Protein-7 Predict Drug-Induced Acute Kidney Injury
Current Drug Metabolism C-11 Radiochemistry in Cancer Imaging Applications
Current Topics in Medicinal Chemistry Inflammation and Chronic Heart Failure: From Biomarkers to Novel Anti-inflammatory Therapeutic Strategies
Medicinal Chemistry Cognitive Dysfunction in Depression – Pathophysiology and Novel Targets
CNS & Neurological Disorders - Drug Targets Strategies Targeting Soluble β-Amyloid Oligomers and their Application to Early Diagnosis of Alzheimer’s Disease
Current Alzheimer Research Halving Your Cake and Eating it, Too: A Case-based Discussion and Review of Metabolic Rehabilitation for Obese Adults with Diabetes
Current Diabetes Reviews