Drug Discovery Today: Technologies
Vol. 10, No. 4 2013
Editors-in-Chief Kelvin Lam – Blue Sky Biotech, Inc., Worcester, MA Henk Timmerman – Vrije Universiteit, The Netherlands DRUG DISCOVERY
TODAY
TECHNOLOGIES
Modulation of protein–protein interactions
Probing structural adaptivity at PPI interfaces with small molecules Christopher G. Wilson, Michelle R. Arkin* University of California, QB3 Fifth Floor South 503E, 1700 4th Street, Box 2552, San Francisco, CA 94158, United States
There is strong interest in developing small molecules
which complementary technologies work together to
that modulate protein-protein interactions (PPI), since
identify starting points for chemical biology and drug
such compounds could serve as drug leads or as probes
discovery.
of protein function. Fragment-based ligand discovery has been a particularly useful approach for modulating PPI. Fragments are typically
Vol. 10, No. 4 2013
Editors-in-Chief Kelvin Lam – Blue Sky Biotech, Inc., Worcester, MA Henk Timmerman – Vrije Universiteit, The Netherlands DRUG DISCOVERY
TODAY
TECHNOLOGIES
Modulation of protein–protein interactions
Probing structural adaptivity at PPI interfaces with small molecules Christopher G. Wilson, Michelle R. Arkin* University of California, QB3 Fifth Floor South 503E, 1700 4th Street, Box 2552, San Francisco, CA 94158, United States
There is strong interest in developing small molecules
which complementary technologies work together to
that modulate protein-protein interactions (PPI), since
identify starting points for chemical biology and drug
such compounds could serve as drug leads or as probes
discovery.
of protein function. Fragment-based ligand discovery has been a particularly useful approach for modulating PPI. Fragments are typically
