Recent Applications of Retro-Inverso Peptides

Natural and de novo designed peptides are gaining an ever-growing interest as drugs against several diseases. Their use is however limited by the intrinsic low bioavailability and poor stability. To overcome these issues retro-inverso analogues have been investigated for decades as more stable surro...

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Bibliographic Details
Published in:International journal of molecular sciences 2021-08, Vol.22 (16), p.8677
Main Authors: Doti, Nunzianna, Mardirossian, Mario, Sandomenico, Annamaria, Ruvo, Menotti, Caporale, Andrea
Format: Article
Language:English
Subjects:
Amino acids
anticancer peptides
Antimicrobial agents
Bioavailability
Biological activity
Blood vessels
Cancer
Chirality
drug delivery
Drugs
Hydrogen bonds
IAPP
Immunology
Ligands
peptide antigens
Peptides
retro-inverso peptides
Review
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Summary:Natural and de novo designed peptides are gaining an ever-growing interest as drugs against several diseases. Their use is however limited by the intrinsic low bioavailability and poor stability. To overcome these issues retro-inverso analogues have been investigated for decades as more stable surrogates of peptides composed of natural amino acids. Retro-inverso peptides possess reversed sequences and chirality compared to the parent molecules maintaining at the same time an identical array of side chains and in some cases similar structure. The inverted chirality renders them less prone to degradation by endogenous proteases conferring enhanced half-lives and an increased potential as new drugs. However, given their general incapability to adopt the 3D structure of the parent peptides their application should be careful evaluated and investigated case by case. Here, we review the application of retro-inverso peptides in anticancer therapies, in immunology, in neurodegenerative diseases, and as antimicrobials, analyzing pros and cons of this interesting subclass of molecules.
ISSN:1422-0067
1661-6596
1422-0067
DOI:10.3390/ijms22168677