TY - JOUR
T1 - Stabilization of protein-protein interaction complexes through small molecules
AU - Zarzycka, Barbara
AU - Kuenemann, Melaine A.
AU - Miteva, Maria A.
AU - Nicolaes, Gerry A. F.
AU - Vriend, Gert
AU - Sperandio, Olivier
PY - 2016/1
Y1 - 2016/1
N2 - 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.
AB - 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.
U2 - 10.1016/j.drudis.2015.09.011
DO - 10.1016/j.drudis.2015.09.011
M3 - Article
C2 - 26434617
SN - 1359-6446
VL - 21
SP - 48
EP - 57
JO - Drug Discovery Today
JF - Drug Discovery Today
IS - 1
ER -