Stabilization of protein-protein interactions by small molecules

F. Giordanetto, A. Schäfer, C. Ottmann

Research output: Contribution to journalArticleAcademicpeer-review

32 Citations (Scopus)
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Abstract

Protein–protein interactions (PPIs) are implicated in every disease and mastering the ability to influence PPIs with small molecules would considerably enlarge the druggable genome. Whereas inhibition of PPIs has repeatedly been shown to work successfully, targeted stabilization of PPIs is underrepresented in the literature. This is all the more surprising because natural products like FK506, rapamycin, brefeldin, forskolin and fusicoccin confer their physiological activity by stabilizing specific PPIs. However, recently a number of very interesting synthetic molecules have been reported from drug discovery projects that indeed achieve their desired activities by stabilizing either homo- or hetero-oligomeric complexes of their target proteins.
Original languageEnglish
Pages (from-to)1812-1821
Number of pages10
JournalDrug Discovery Today: Technologies
Volume19
Issue number11
DOIs
Publication statusPublished - 2014

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