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Unlocking the Potential of Retro-Inverso (RI) Peptides as Future Drug Candidates
Open accessAbstract
Background: With the rising demand for peptide-based drugs, enhancing their stability against proteolytic degradation has become a critical challenge. Strategies to improve peptide stability include cyclization, substitution of L-amino acids with D-amino acids, incorporation of β-amino acids, and various formulation techniques. An innovative approach involves modifying the peptide backbone by reversing the amide bond direction and inverting the stereochemistry of amino acids in the same segment. This approach results in the formation of retro-inverso peptides, which offer increased stability, permeability, and cellular uptake. Purpose: The aim of this review is to provide a comprehensive analysis of retro-inverso peptides, focusing on their concept, synthesis, and applications as potential therapeutic agents, drug delivery systems, and in aesthetic applications. Methods: The review explores the theoretical underpinnings of retro-inverso peptide design and its application to both linear and cyclic peptides. The synthesis strategies of retro-inverso peptides are discussed in detail, along with their formulation and practical utility in various biomedical fields. Results: Retro-inverso peptides show promise in enhancing peptide stability and improving biological properties such as permeability and cellular uptake. Their unique structure offers advantages in drug development and potential as therapeutic agents or drug carriers. Conclusion: Retro-inverso peptides represent a valuable strategy for overcoming the limitations of conventional peptides, especially regarding stability and bioavailability. This review highlights their potential in therapeutic development and other applications, reinforcing the importance of continued research and innovation in peptide chemistry.
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Metadata
- Authors
- Al Musaimi, O.
- Venue
- International Journal of Peptide Research and Therapeutics
- Published
- 2024-09-10
- Volume
- 30
- Issue
- 5
- ISSN
- 1573-3149 (ISSN-L)
- 1573-3904
- OpenAlex
- W4402400639
- Cited by
- 18
- References
- 80
- Citations by year
- 2026: 6 · 2025: 11 · 2024: 1
- FWCI
- 2.44
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Locations
- International Journal of Peptide Research and Therapeutics (publishedVersion, cc-by)
- Newcastle University ePrints (Newcastle Univesity) (cc-by)
- Topics
- Physical Sciences › Chemistry › Organic Chemistry › Chemical Synthesis and Analysis
- Physical Sciences › Materials Science › Biomaterials › Supramolecular Self-Assembly in Materials
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Biochemical and Structural Characterization
- Keywords
- retro-inverso peptides, peptide stability, proteolysis, peptide synthesis, cyclic peptides, D-amino acids, β-amino acids, peptide permeability, cellular uptake, drug delivery systems, bioavailability
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Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
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