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Small molecules, big targets: drug discovery faces the protein–protein interaction challenge
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Journal Article
Small molecules, big targets: drug discovery faces the protein–protein interaction challenge
2016
Overview
Key Points
Protein–protein interactions (PPIs) are increasingly being targeted by drug discovery groups, and there exists great scope for therapeutic modulation of this target class in disease.
The array of structurally interacting elements through which proteins interact with one another is wide and resists clear-cut classification. However, broad divisions can be made by grouping interactions based upon the globular or peptidic nature of the proteins.
Some strategies for developing inhibitors against a given PPI may have more traction against certain classes of PPIs than others; for example, fragment-based drug discovery has shown particular promise in targeting bromodomains, as have peptide mimetics in mimicking β-strands.
We examine case studies representative of the various structural types of PPI and discuss the lessons learnt from each.
A summary of current status of inhibitors in clinical trials against different targets is presented.
The biological rationale for targeting protein–protein interactions as a therapeutic strategy is strong, but identifying viable small-molecule drugs to achieve this has proved highly challenging. This article uses examples of successful discovery efforts to illustrate the research strategies that have proved most useful for different classes of protein–protein interactions.
Protein–protein interactions (PPIs) are of pivotal importance in the regulation of biological systems and are consequently implicated in the development of disease states. Recent work has begun to show that, with the right tools, certain classes of PPI can yield to the efforts of medicinal chemists to develop inhibitors, and the first PPI inhibitors have reached clinical development. In this Review, we describe the research leading to these breakthroughs and highlight the existence of groups of structurally related PPIs within the PPI target class. For each of these groups, we use examples of successful discovery efforts to illustrate the research strategies that have proved most useful.
Publisher
Nature Publishing Group UK,Nature Publishing Group
