Lipidization as a tool toward peptide therapeutics

0579354 - ÚOCHB 2024 RIV US eng J - Journal Article
Myšková, Aneta - Sýkora, D. - Kuneš, Jaroslav - Maletínská, Lenka
Lipidization as a tool toward peptide therapeutics.
Drug Delivery. Roč. 30, č. 1 (2023), č. článku 2284685. ISSN 1071-7544. E-ISSN 1521-0464
R&D Projects: GA ČR(CZ) GA21-03691S; GA ČR(CZ) GA22-11155S
Institutional support: RVO:61388963
Keywords : peptide therapeutics * structure modification * lipidization * therapeutic lipopeptides
OECD category: Physiology (including cytology)
Impact factor: 6, year: 2022
Method of publishing: Open access
https://doi.org/10.1080/10717544.2023.2284685

Peptides, as potential therapeutics continue to gain importance in the search for active substances for the treatment of numerous human diseases, some of which are, to this day, incurable. As potential therapeutic drugs, peptides have many favorable chemical and pharmacological properties, starting with their great diversity, through their high affinity for binding to all sort of natural receptors, and ending with the various pathways of their breakdown, which produces nothing but amino acids that are nontoxic to the body. Despite these and other advantages, however, they also have their pitfalls. One of these disadvantages is the very low stability of natural peptides. They have a short half-life and tend to be cleared from the organism very quickly. Their instability in the gastrointestinal tract, makes it impossible to administer peptidic drugs orally. To achieve the best pharmacologic effect, it is desirable to look for ways of modifying peptides that enable the use of these substances as pharmaceuticals. There are many ways to modify peptides. Herein we summarize the approaches that are currently in use, including lipidization, PEGylation, glycosylation and others, focusing on lipidization. We describe how individual types of lipidization are achieved and describe their advantages and drawbacks. Peptide modifications are performed with the goal of reaching a longer half-life, reducing immunogenicity and improving bioavailability. In the case of neuropeptides, lipidization aids their activity in the central nervous system after the peripheral administration. At the end of our review, we summarize all lipidized peptide-based drugs that are currently on the market.
Permanent Link: https://hdl.handle.net/11104/0348192