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Modulation of protein-protein interactions for the development of novel therapeutics

Ioanna Petta (UGent) , Sam Lievens (UGent) , Claude Libert (UGent) , Jan Tavernier (UGent) and Karolien De Bosscher (UGent)
(2016) MOLECULAR THERAPY. 24(4). p.707-718
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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.
Keywords
BCL-2 FAMILY PROTEINS, ESTROGEN-RECEPTOR-ALPHA, MENIN-MLL INTERACTION, AMYLOID-BETA PEPTIDE, P53 PATHWAY, NEURODEGENERATIVE DISEASES, CLINICAL DEVELOPMENT, MCL-1 INHIBITORS, SITE INTEGRASE INHIBITOR, SMALL-MOLECULE INHIBITORS

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Citation

Please use this url to cite or link to this publication:

Chicago
Petta, Ioanna, Sam Lievens, Claude Libert, Jan Tavernier, and Karolien De Bosscher. 2016. “Modulation of Protein-protein Interactions for the Development of Novel Therapeutics.” Molecular Therapy 24 (4): 707–718.
APA
Petta, I., Lievens, S., Libert, C., Tavernier, J., & De Bosscher, K. (2016). Modulation of protein-protein interactions for the development of novel therapeutics. MOLECULAR THERAPY, 24(4), 707–718.
Vancouver
1.
Petta I, Lievens S, Libert C, Tavernier J, De Bosscher K. Modulation of protein-protein interactions for the development of novel therapeutics. MOLECULAR THERAPY. 2016;24(4):707–18.
MLA
Petta, Ioanna, Sam Lievens, Claude Libert, et al. “Modulation of Protein-protein Interactions for the Development of Novel Therapeutics.” MOLECULAR THERAPY 24.4 (2016): 707–718. Print.
@article{7236171,
  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.},
  author       = {Petta, Ioanna and Lievens, Sam and Libert, Claude and Tavernier, Jan and De Bosscher, Karolien},
  issn         = {1525-0016},
  journal      = {MOLECULAR THERAPY},
  language     = {eng},
  number       = {4},
  pages        = {707--718},
  title        = {Modulation of protein-protein interactions for the development of novel therapeutics},
  url          = {http://dx.doi.org/10.1038/mt.2015.214},
  volume       = {24},
  year         = {2016},
}

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