Effects of Modifications on the Immunosuppressive Properties of Cyclolinopeptide A and Its Analogs in Animal Experimental Models

The consequences of manipulations in structure and amino acid composition of native cyclolinopeptide A (CLA) from linen seeds, and its linear precursor on their biological activities and mechanisms of action, are reviewed. The modifications included truncation of the peptide chain, replacement of am...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2021-04, Vol.26 (9), p.2538
Main Authors: Zimecki, Michał, Kaczmarek, Krzysztof
Format: Article
Language:English
Subjects:
Amino acid composition
Amino Acid Sequence - genetics
Amino acids
Analogs
Animal models
Animal research
Animals
Bedding and Linens
Blood
cis-peptide bond
cyclolinopeptide A (CLA)
cyclosporine A
Cyclosporins
edge-to-face
Geometry
immunosuppression
Immunosuppressive Agents - chemistry
Immunosuppressive Agents - pharmacology
In vivo methods and tests
Linen
Models, Animal
NMR
Nuclear magnetic resonance
Peptides
Peptides - chemistry
Peptides - genetics
Peptides - pharmacology
Peptides, Cyclic - chemistry
Peptides, Cyclic - genetics
Peptides, Cyclic - pharmacology
PGE2
Review
Seeds
Seeds - chemistry
Structure-Activity Relationship
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Summary:The consequences of manipulations in structure and amino acid composition of native cyclolinopeptide A (CLA) from linen seeds, and its linear precursor on their biological activities and mechanisms of action, are reviewed. The modifications included truncation of the peptide chain, replacement of amino acid residues with proteinogenic or non-proteinogenic ones, modifications of peptide bond, and others. The studies revealed changes in the immunosuppressive potency of these analogs investigated in a number of in vitro and in vivo experimental models, predominantly in rodents, as well as differences in their postulated mechanism of action. The modified peptides were compared with cyclosporine A and parent CLA. Some of the synthesized and investigated peptides show potential therapeutic usefulness.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules26092538