review · Chemical Reviews
Peptide drug discovery has expanded significantly over the past twenty years, driven by advances in organic chemistry and biotechnology. These disciplines provide practical tools to produce peptidomimetics, which exhibit superior stability, specificity, and bioavailability relative to standard peptides. Systematic modification of peptide backbones enables the design of molecules with targeted therapeutic characteristics, supported by biotechnological innovations that permit novel chemical transformations. Peptides and peptidomimetics have already demonstrated real-world relevance through their integration into modern pharmacology and clinical medicine. Alongside these achievements, important technical challenges persist across the field. Addressing these obstacles requires identifying critical research priorities and defining clear strategic directions to support the ongoing development of next-generation therapeutic candidates.
Traditional peptides often break down rapidly or fail to reach their targets in the body. Peptidomimetics resolve these limitations by mimicking peptide activity while offering greater chemical stability and improved uptake. Refining these molecules helps drug developers create more durable, highly targeted therapies, ultimately leading to safer and more effective pharmaceutical treatments for a wide variety of human diseases.
The described strategies target applications in drug discovery and therapeutic development, aimed primarily at medicinal chemists, pharmaceutical developers, and biotechnology firms. Because the underlying technologies range from novel backbone modification methodologies to already integrated clinical compounds, the work spans early-stage drug design through to applied pharmacology. Commercial uptake focuses on deploying these synthetic techniques to create bioavailable, stable peptide therapeutics with lower development attrition rates.
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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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DOI: 10.1021/acs.chemrev.4c00989
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