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A Tripeptide-Stabilized Nanoemulsion of Oleic Acid

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Advances in Peptidomimetics for Next-Generation Therapeutics: Strategies, Modifications, and Applications.

Lucia Lombardi^1,2, Valentina Del Genio³, Fernando Albericio^4,5

¹Department of Chemical Engineering, Imperial College London, South Kensington, London SW7 2AZ, U.K.

Chemical Reviews

|July 23, 2025

Summary

Peptide drug discovery is advancing rapidly, using organic chemistry and biotechnology to create more stable and effective peptidomimetics for medicine. This review explores methods, applications, and future research directions for peptide therapeutics.

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Area of Science:

Medicinal Chemistry
Biotechnology
Pharmacology

Background:

Peptide drug discovery has seen significant growth over the last 20 years.
Conventional peptides face limitations in stability, specificity, and bioavailability.
Peptidomimetics offer enhanced properties compared to traditional peptides.

Purpose of the Study:

To systematically review methodologies for modifying peptide backbones.
To highlight advances in peptide modification through biotechnology.
To discuss the practical applications and future directions of peptide-based therapeutics.

Main Methods:

Examination of organic chemistry and biotechnology approaches for peptide backbone modification.
Review of literature on recent innovations in molecular transformations.
Analysis of case studies on peptide and peptidomimetic integration in medicine.

Main Results:

Identification of key strategies for enhancing peptide stability, specificity, and bioavailability.
Demonstration of successful applications of modified peptides in pharmacology.
Evaluation of current achievements and existing challenges in the field.

Conclusions:

Peptidomimetics represent a promising avenue for developing next-generation therapeutics.
Continued research in peptide modification and biotechnology is crucial.
Strategic directions are proposed for advancing peptide-based drug development.