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Macrocyclic Peptides as Drug Candidates: Recent Progress and Remaining Challenges.
Alexander A Vinogradov1, Yizhen Yin1, Hiroaki Suga1
1Department of Chemistry, Graduate School of Science , The University of Tokyo , 7-3-1 Hongo , Bunkyo-ku, Tokyo 113-0033 , Japan.
Journal of the American Chemical Society
|February 16, 2019
Summary
Peptide therapeutics show promise but face challenges with stability and delivery. This review explores strategies like macrocyclization and non-native amino acids to enhance peptide drug properties for improved therapeutic success.
Area of Science:
- Medicinal Chemistry
- Drug Discovery
- Biotechnology
Background:
- Peptides are attractive therapeutics due to synthetic accessibility and specific binding.
- Poor metabolic stability and cell permeability limit the clinical success of peptide drugs.
- Targeting 'undruggable' protein surfaces is a key advantage of peptide therapeutics.
Purpose of the Study:
- To review strategies for improving peptide drug properties.
- To analyze progress and challenges in enhancing peptide pharmacology.
- To discuss balancing conflicting considerations for optimal peptide drug candidates.
Main Methods:
- Review of macrocyclization techniques for peptide drug development.
- Analysis of non-proteogenic amino acid incorporation in peptide design.
- Examination of conjugation strategies to improve peptide drug characteristics.
Main Results:
- Macrocyclization, non-native amino acids, and conjugation enhance peptide metabolic stability and cell permeability.
- These modifications can overcome limitations of de novo discovered bioactive peptides.
- Recent progress demonstrates feasibility of improving individual pharmacological properties.
Conclusions:
- Optimizing peptide drug candidates requires balancing multiple pharmacological properties.
- Interfacing conflicting considerations is crucial for advancing peptide therapeutics.
- Strategic modifications offer a pathway to overcome inherent peptide limitations for drug development.
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