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Protein–protein interactions play a crucial role in many biochemical processes. They have emerged as a new class of drug targets. Small molecule inhibitors are available, but often challenging to develop as protein–protein interaction inhibitors. Peptides have long been considered to possess undesirable properties that are unsuitable for drugs targeting intracellular drug targets. However, over the last few decades, many of these obstacles have been overcome. In this chapter, we describe recent developments in targeting protein–protein interactions using conformationally stabilized α-helical peptides. Some of these peptides have now entered clinical trials.

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