Stabilization of protein-protein interaction complexes through small molecules

Barbara Zarzycka, Melaine A. Kuenemann, Maria A. Miteva, Gerry A. F. Nicolaes, Gert Vriend, Olivier Sperandio*

*Corresponding author for this work

Research output: Contribution to journalArticleAcademicpeer-review


Most of the small molecules that have been identified thus far to modulate protein-protein interactions (PPIs) are inhibitors. Another promising way to interfere with PPI-associated biological processes is to promote PPI stabilization. Even though PPI stabilizers are still scarce, stabilization of PPIs by small molecules is gaining momentum and offers new pharmacological options. Therefore, we have performed a literature survey of PPI stabilization using small molecules. From this, we propose a classification of PPI stabilizers based on their binding mode and the architecture of the complex to facilitate the structure-based design of stabilizers.
Original languageEnglish
Pages (from-to)48-57
JournalDrug Discovery Today
Issue number1
Publication statusPublished - Jan 2016

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