Targeting Protein-Protein Interactions for Drug Discovery

Jian Zhang

• Publisher: Wiley-VCH
• Year: 2025
• Print ISBN: 9783527353606
• eBook ISBN: 9783527845804
• Edition: 1
• Topic: Medicine
• Subtopic: Pharmacology

Up-to-date reference surveying the latest advances in the structural understanding of protein-protein interactions and developments in drug discovery and therapeutics

Targeting Protein–Protein Interactions for Drug Discovery provides a systematic and comprehensive overview of protein-protein interactions (PPIs), reviewing foundational concepts, advanced methodologies, and emerging therapeutic strategies, reflecting the multidisciplinary nature of PPI research.

This book discusses computational methods for predicting PPI structures, with a special emphasis on protein docking and deep learning-based approaches, diverse chemical scaffolds for PPI modulation, including foldamers as inhibitors of aberrant PPIs and sulfonyl-?-AApeptides as novel modulators, and the development and application of stapled peptides as modulators of intracellular PPIs, offering enhanced stability, binding affinity, and cellular permeability.

Readers will also find information on cyclic peptides, focusing on their unique conformational stabilization and therapeutic potential across a range of diseases, small molecule inhibitors targeting BCL-family proteins, revealing their potential in cancer therapy, molecular glues as activators for PPIs, categorized into degraders, stabilizers, and inhibitors based on their biological effects, and the targeting of the APC–Asef interaction for drug discovery in colorectal cancer therapy, offering a case study of specificity and clinical relevance.

Targeting Protein–Protein Interactions for Drug Discovery explores sample topics including:

• Challenges and strategies of drug discovery targeting PPIs, including high-throughput screening and structure-based drug design
• Fluorescence resonance energy transfer (FRET) technology, a powerful tool for real-time analysis of molecular interactions in live cells
• Utility of mass spectrometry (MS) for large-scale mapping of PPI networks with high sensitivity and resolution
• Proximity ligation assays (PLA) for detecting PPIs in situ, emphasizing spatial precision and adaptability for multiplexed detection
• Application of surface plasmon resonance (SPR) for characterizing PPI specificity, affinity, and kinetics

Exploring both classical and novel approaches to PPI characterization and modulation, Targeting Protein–Protein Interactions for Drug Discovery offers a comprehensive reference for researchers aiming to unlock the therapeutic potential of PPIs along with educators and students engaged in the study of cellular mechanisms, drug discovery, and biotechnology.

Table of contents

• Cover
• Title Page
• Copyright
• Contents
• Preface
• Chapter 1 Exploring Protein–Protein Interactions: Concepts, Methods, and Implications
• Chapter 2 Overview of Drug Discovery Targeting PPI Systems
• Chapter 3 Fluorescence Resonance Energy Transfer Technology and its Applications
• Chapter 4 Dissect Protein Interactions Using Mass Spectrometry
• Chapter 5 Detection of Protein–Protein Interactions In Situ via Proximity Ligation Assay
• Chapter 6 Application of Surface Plasmon Resonance in the Characterization of Protein–Protein Interactions
• Chapter 7 Computational Methods for Protein–Protein Interactions
• Chapter 8 Foldamers as Inhibitors of Aberrant Protein–Protein Interactions
• Chapter 9 Application of Sulfonyl‐γ‐AApeptides for PPI Drug Discovery
• Chapter 10 Introduction of the Application of Stapled Peptides in Protein–Protein Interactions Drug Discovery and Their Successful Examples
• Chapter 11 Cyclic Peptides for PPI Drug Discovery
• Chapter 12 Small Molecule Inhibitors Targeting Protein–Protein Interactions in the BCL Protein
• Chapter 13 Molecular Glues as Activators for PPI
• Chapter 14 Targeting APC–Asef Protein–Protein Interaction for Drug Discovery in Colorectal Cancer Therapy
• Chapter 15 Computational Methods Applied to Drug Discovery of Protein–Protein Interaction Systems
• Index
• EULA