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Emerging strategies to access peptide macrocycles from genetically encoded polypeptides
Jessica M Smith1, John R Frost, Rudi Fasan
1Department of Chemistry, University of Rochester, Rochester, New York 14627, USA.
The Journal of Organic Chemistry
|March 23, 2013
Summary
Macrocyclic peptides are promising scaffolds for developing new therapeutics and chemical probes. Researchers are advancing methods to create these complex molecules from ribosomal polypeptides, overcoming key challenges in synthesis and functionalization.
Area of Science:
- Biochemistry
- Medicinal Chemistry
- Molecular Biology
Background:
- Macrocyclic peptides are increasingly recognized for their potential as therapeutic agents and chemical probes.
- Ribosomally produced polypeptides offer a versatile starting point for macrocycle synthesis.
Purpose of the Study:
- To review modern strategies for synthesizing macrocyclic peptides from ribosomal polypeptides.
- To discuss challenges and solutions in macrocyclization of unprotected precursors.
- To highlight the expansion of functional diversity in macrocyclic peptides.
Main Methods:
- Overview of contemporary synthetic methodologies for macrocyclic peptide generation.
- Discussion of techniques for managing unprotected polypeptide precursors during macrocyclization.
- Exploration of methods to incorporate non-canonical amino acids and expand functional space.
Main Results:
- Successful strategies have been developed to synthesize macrocyclic peptides from ribosomal polypeptides.
- Key challenges in macrocyclization, such as handling unprotected precursors, have been addressed.
- Methodologies enable the creation of macrocyclic peptides with expanded functional diversity beyond canonical amino acids.
Conclusions:
- Advanced strategies facilitate the efficient synthesis of macrocyclic peptides from ribosomal polypeptides.
- These methods overcome significant hurdles in macrocyclization and functionalization.
- The developed approaches are crucial for discovering novel bioactive molecules and therapeutics.
