Identification of Macrocyclic Peptide Families from Combinatorial Libraries Containing Noncanonical Amino Acids Using Cheminformatics and Bioinformatics Inspired Clustering

Article Biochemistry & Molecular Biology

Targeted degradation via direct 26S proteasome recruitment

Charlene Bashore et al.

Summary: Engineered destruction of target proteins by recruitment to the cell's degradation machinery has emerged as a promising strategy in drug discovery.

NATURE CHEMICAL BIOLOGY (2023)

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Article Chemistry, Medicinal

PepSeA: Peptide Sequence Alignment and Visualization Tools to Enable Lead Optimization

Javier L. Baylon et al.

Summary: Therapeutic peptides offer potential advantages in drug discovery due to their selectivity, affinity, and ability to target undruggable proteins. However, current molecular design capabilities for peptide programs are limited. The development of PepSeA tool, an open-source platform, addresses this limitation and enables faster decision making in lead optimization in pharmaceutical settings.

JOURNAL OF CHEMICAL INFORMATION AND MODELING (2022)

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Review Chemistry, Multidisciplinary

Cyclic Peptides as Drugs for Intracellular Targets: The Next Frontier in Peptide Therapeutic Development

Laura K. Buckton et al.

Summary: Developing macrocyclic peptides that can reach intracellular targets is a significant challenge, and current chemical strategies can improve cell permeability, but often at the expense of biological activity.

CHEMISTRY-A EUROPEAN JOURNAL (2021)

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Review Chemistry, Multidisciplinary

The RaPID Platform for the Discovery of Pseudo-Natural Macrocyclic Peptides

Yuki Goto et al.

Summary: The RaPID system has enabled rapid discovery of novel macrocyclic peptides with high affinity and specificity, suitable for various biochemical applications and drug development. The integration of the FIT system with mRNA display technology has expanded the structural diversity of peptides and allowed for the incorporation of exotic building blocks. The potential of these peptides as drug leads is demonstrated by their pharmacological activities in animal models and inhibition of intracellular proteins.

ACCOUNTS OF CHEMICAL RESEARCH (2021)

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Article Multidisciplinary Sciences