Stabilization of protein-protein interactions by small molecules

F. Giordanetto, A. Schäfer, C. Ottmann

Onderzoeksoutput: Bijdrage aan tijdschriftTijdschriftartikelpeer review

33 Citaten (Scopus)
5948 Downloads (Pure)

Samenvatting

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.
Originele taal-2Engels
Pagina's (van-tot)1812-1821
Aantal pagina's10
TijdschriftDrug Discovery Today: Technologies
Volume19
Nummer van het tijdschrift11
DOI's
StatusGepubliceerd - 2014

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