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The field of protein–protein interaction (PPI) inhibitors has come a long way in a short number of years. It wasn't too long ago that identifying and developing PPI inhibitors was considered as a near insurmountable challenge in drug discovery. However, through systematic research effort and outside the box thinking, in both academia and industry, we not only have a better understanding of the nature of PPIs, we also have a number of tools and technologies for the development and identification of inhibitors. And while the development of PPI inhibitors toward the clinic remains a challenging endeavour, the promise of harnessing the vast target space of PPIs for therapeutic purposes is within grasp.

This book captures the current state-of-the-art approaches to targeting PPIs and contains perspective from both academia and industry. In Chapter 1, Ivarsson et al. detail and discuss the various approaches used for the identification and mapping of PPIs. The following chapter by Modell and Arora details the bioinformatics methods used to classify PPIs, and discusses the approaches used for targeting PPIs. In Chapter 3, Tellers and colleagues give a broad perspective of the challenges in developing PPI inhibitors, as well as reviewing and discussing the advantages and disadvantages of the therapeutic modalities deployed against this target class. In Chapter 4, Rees et al. discuss and detail the potential of small molecules as inhibitors of PPIs. This chapter contains a number of examples as well as techniques being deployed to overcome the difficulties associated with identifying small molecule PPI inhibitors.

This is followed by a chapter detailing and discussing the use of macrocycles as PPI inhibitors by Marsault. In Chapter 6, Tavassoli et al. discuss the use of SICLOPPS libraries in combination with functional screening for the identification of cyclic peptide PPI inhibitors. This is followed by a chapter by Suga et al. detailing the use of mRNA display for the identification of PPI inhibitors. In the following chapter, Pei et al. detail and review the discovery and development of bicyclic peptide inhibitors of PPIs.

Stapled peptides are another important class of PPI inhibitors that hold much therapeutic promise. The current state of the field is reviewed by Grossmann and colleagues in Chapter 9. This is followed by a chapter detailing the use of α-helix mimetics as PPI inhibitors by Wilson.

I am grateful to my co-authors who contributed their knowledge and expertise to this book. I would also like to thank Mikayla Fernholz for assistance with editing the chapters. I hope you enjoy reading the book and find it informative.

Ali Tavassoli

Southampton, UK

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