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Updated: Dec 26, 2025

Peptide-based Identification of Functional Motifs and their Binding Partners

Peptide-based Identification of Functional Motifs and their Binding Partners

Published on: June 30, 2013

Mechanisms Inspired Targeting Peptides.

Yunsheng Yuan¹

¹School of Pharmacy, Engineering Research Center of Cell and Therapeutic Antibody, Ministry of Education, Shanghai Jiao Tong University, Shanghai, 200240, China. yunsheng@sjtu.edu.cn.

Advances in Experimental Medicine and Biology

|March 19, 2020

Summary

Peptides are versatile molecules used to develop cancer immune checkpoint (CIP) inhibitors. These targeting peptides enhance anti-tumor immune responses and offer potential for drug delivery and diagnosis in cancer therapy.

Keywords:

Peptides Peptidic inhibitors Random peptide libraries Targeted delivery Targeted protein degradation

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Area of Science:

Biochemistry
Immunology
Drug Discovery

Background:

Peptides, composed of amino acids, exhibit diverse structures (linear, cyclic) and high affinity for target proteins.
Over 13,000 natural peptides are known, with artificial libraries offering vast diversity (up to 1x10^13).
Cancer immune checkpoint (CIP) inhibitors are crucial in tumor therapy, with peptides emerging as key modulators.

Purpose of the Study:

To explore the application of peptides in targeting cancer immune checkpoints (CIPs).
To highlight the role of peptides in enhancing anti-tumor immunity and their potential in cancer therapeutics.
To discuss peptide-based strategies for drug delivery and diagnosis in cancer immunotherapy.

Main Methods:

Designing peptides based on three-dimensional protein structures.
Selecting peptides using random peptide libraries in biological display systems.
Developing peptides to inhibit protein-protein interactions and regulate protein degradation.

Main Results:

Peptides effectively target ligands or receptors in CIPs.
Targeting peptides inhibit protein-protein interactions, enhancing CD8+ cytotoxic T-lymphocyte (CTL) activation.
Examples like PKHB1, Ar5Y4, TPP1, PD-LYSO, and PD-PALM demonstrate peptide efficacy.

Conclusions:

Peptides are promising agents for developing novel cancer immune checkpoint inhibitors.
Peptide-based therapeutics can modulate the tumor microenvironment and improve anti-tumor immunity.
Targeting peptides hold significant potential for advanced cancer treatment, including targeted drug delivery and diagnostics.