title: Stabilization of protein-protein interaction complexes through small molecules.
abstract: 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.
authors.affiliation: Department of Biochemistry, Cardiovascular Research Institute Maastricht (CARIM), Maastricht University, Maastricht, The Netherlands.
authors.forename: Barbara
authors.initials: B
authors.lastname: Zarzycka
authors.affiliation: Université Paris Diderot, Sorbonne Paris Cité, UMRS 973 Inserm, Paris 75013, France; Inserm, U973, Paris 75013, France.
authors.forename: Mélaine A
authors.initials: MA
authors.lastname: Kuenemann
authors.affiliation: Université Paris Diderot, Sorbonne Paris Cité, UMRS 973 Inserm, Paris 75013, France; Inserm, U973, Paris 75013, France.
authors.forename: Maria A
authors.initials: MA
authors.lastname: Miteva
authors.affiliation: Department of Biochemistry, Cardiovascular Research Institute Maastricht (CARIM), Maastricht University, Maastricht, The Netherlands.
authors.forename: Gerry A F
authors.initials: GAF
authors.lastname: Nicolaes
authors.affiliation: Centre for Molecular and Biomolecular Informatics (CMBI), Radboudumc, PO Box 9101, 6500 HB Nijmegen, The Netherlands.
authors.forename: Gert
authors.initials: G
authors.lastname: Vriend
authors.affiliation: Université Paris Diderot, Sorbonne Paris Cité, UMRS 973 Inserm, Paris 75013, France; Inserm, U973, Paris 75013, France; Faculté de Pharmacie, CDithem, 1 rue du Prof. Laguesse, 59000 Lille, France. Electronic address: olivier.sperandio@inserm.fr.
authors.forename: Olivier
authors.initials: O
authors.lastname: Sperandio
mesh_terms: D055592:Biophysical Phenomena / Q000187:drug effects; D006801:Humans; D011485:Protein Binding / Q000187:drug effects*; D060066:Protein Interaction Maps / Q000187:drug effects*; D054852:Small Molecule Libraries / Q000494:pharmacology*
chemical_list: D054852:Small Molecule Libraries