Advances inPeptidomimetics for Next-Generation Therapeutics:Strategies, Modifications, and Applications

Over the past two decades, peptide drug discovery has experienced a remarkable renaissance, with organic chemistry and biotechnology emerging as pivotal tools for developing peptidomimetics that exhibit improved stability, specificity, and bioavailability compared to conventional peptides. This review systematically examines methodologies for modifying peptide backbones to achieve targeted properties, highlighting recent advances facilitated by modern biotechnological innovations for novel molecular transformations. Additionally, the review emphasizes the practical applications of peptides and peptidomimetics, showcasing their successful integration into medicine and pharmacology. This manuscript evaluates achievements and challenges in the field and identifies critical areas for further research. Its overarching aim is to synthesize current knowledge and propose strategic directions for advancing peptide-based therapeutics.

Publication Details

Journal
Figshare
Published
2025-07-23
DOI
https://doi.org/10.1021/acs.chemrev.4c00989.s001
Primary Topic
Chemical Synthesis and Analysis
Type
article
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article

Advances inPeptidomimetics for Next-Generation Therapeutics:Strategies, Modifications, and Applications

Figshare
Chemical Synthesis and Analysis
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Advances inPeptidomimetics for Next-Generation Therapeutics:Strategies, Modifications, and Applications

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Abstract

Over the past two decades, peptide drug discovery has experienced a remarkable renaissance, with organic chemistry and biotechnology emerging as pivotal tools for developing peptidomimetics that exhibit improved stability, specificity, and bioavailability compared to conventional peptides. This review systematically examines methodologies for modifying peptide backbones to achieve targeted properties, highlighting recent advances facilitated by modern biotechnological innovations for novel molecular transformations. Additionally, the review emphasizes the practical applications of peptides and peptidomimetics, showcasing their successful integration into medicine and pharmacology. This manuscript evaluates achievements and challenges in the field and identifies critical areas for further research. Its overarching aim is to synthesize current knowledge and propose strategic directions for advancing peptide-based therapeutics.

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Industry, innovation and infrastructure
Openalex Percentile: Top 60%
Chemical Synthesis and Analysis
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Advances inPeptidomimetics for Next-Generation Therapeutics:Strategies, Modifications, and Applications · Figshare (2025) | TGRS Research Map | TGRS