title: Modulation of Protein-Protein Interactions for the Development of Novel Therapeutics.
abstract: Protein-protein interactions (PPIs) underlie most biological processes. An increasing interest to investigate the unexplored potential of PPIs in drug discovery is driven by the need to find novel therapeutic targets for a whole range of diseases with a high unmet medical need. To date, PPI inhibition with small molecules is the mechanism that has most often been explored, resulting in significant progress towards drug development. However, also PPI stabilization is gradually gaining ground. In this review, we provide a focused overview of a number of PPIs that control critical regulatory pathways and constitute targets for the design of novel therapeutics. We discuss PPI-modulating small molecules that are already pursued in clinical trials. In addition, we review a number of PPIs that are still under preclinical investigation but for which preliminary data support their use as therapeutic targets.
authors.affiliation: Receptor Research Laboratories, Cytokine Receptor Lab (CRL), VIB Department of Medical Protein Research, Ghent, Belgium.|Department of Biochemistry, Ghent University, Ghent, Belgium.|Inflammation Research Center, VIB, Ghent, Belgium.|Department of Biomedical Molecular Biology, Ghent University, Ghent, Belgium.
authors.forename: Ioanna
authors.initials: I
authors.lastname: Petta
authors.affiliation: Receptor Research Laboratories, Cytokine Receptor Lab (CRL), VIB Department of Medical Protein Research, Ghent, Belgium.|Department of Biochemistry, Ghent University, Ghent, Belgium.
authors.forename: Sam
authors.initials: S
authors.lastname: Lievens
authors.affiliation: Inflammation Research Center, VIB, Ghent, Belgium.|Department of Biomedical Molecular Biology, Ghent University, Ghent, Belgium.
authors.forename: Claude
authors.initials: C
authors.lastname: Libert
authors.affiliation: Receptor Research Laboratories, Cytokine Receptor Lab (CRL), VIB Department of Medical Protein Research, Ghent, Belgium.|Department of Biochemistry, Ghent University, Ghent, Belgium.
authors.forename: Jan
authors.initials: J
authors.lastname: Tavernier
authors.affiliation: Receptor Research Laboratories, Cytokine Receptor Lab (CRL), VIB Department of Medical Protein Research, Ghent, Belgium.|Department of Biochemistry, Ghent University, Ghent, Belgium.|Receptor Research Laboratories, Nuclear Receptor Lab (NRL), VIB Department of Medical Protein Research, Ghent, Belgium.
authors.forename: Karolien
authors.initials: K
authors.lastname: De Bosscher
mesh_terms: D000818:Animals; D055808:Drug Discovery / Q000379:methods*; D004353:Drug Evaluation, Preclinical; D053263:Gene Regulatory Networks / Q000187:drug effects*; D006801:Humans; D011485:Protein Binding / Q000187:drug effects*; D025941:Protein Interaction Mapping; D011506:Proteins / Q000378:metabolism
chemical_list: D011506:Proteins