Giovanna Zinzalla1, David E Thurston. 1. The School of Pharmacy, University of London, 29-39 Brunswick Square, London, UK. giovanna.zinzalla@pharmacy.ac.uk
Abstract
BACKGROUND: Over the last two decades, an increasing research effort in academia and industry has focused on the modulation (both inhibition and stabilization) of protein-protein interactions (PPIs) in order to develop novel therapeutic approaches and target-selective agents in drug discovery. DISCUSSION: The diversity and complexity of highly dynamic systems such as PPIs present many challenges for the identification of drug-like molecules with the ability to modulate the PPI with the necessary selectivity and potency. In this review, a number of these strategies will be presented along with a critical overview of the challenges and potential solutions relating to the exploitation of PPIs as molecular targets. CONCLUSIONS: Both traditional drug discovery approaches and some more recently developed innovative strategies have already provided valuable tools for the discovery of PPI modulators, and a number of successful examples have highlighted the potential of targeting PPIs for therapeutic intervention, especially in the oncology area.
BACKGROUND: Over the last two decades, an increasing research effort in academia and industry has focused on the modulation (both inhibition and stabilization) of protein-protein interactions (PPIs) in order to develop novel therapeutic approaches and target-selective agents in drug discovery. DISCUSSION: The diversity and complexity of highly dynamic systems such as PPIs present many challenges for the identification of drug-like molecules with the ability to modulate the PPI with the necessary selectivity and potency. In this review, a number of these strategies will be presented along with a critical overview of the challenges and potential solutions relating to the exploitation of PPIs as molecular targets. CONCLUSIONS: Both traditional drug discovery approaches and some more recently developed innovative strategies have already provided valuable tools for the discovery of PPI modulators, and a number of successful examples have highlighted the potential of targeting PPIs for therapeutic intervention, especially in the oncology area.
Authors: Fang Bai; Faruck Morcos; Ryan R Cheng; Hualiang Jiang; José N Onuchic Journal: Proc Natl Acad Sci U S A Date: 2016-11-29 Impact factor: 11.205
Authors: Laurence Leherte; Axel Petit; Denis Jacquemin; Daniel P Vercauteren; Adèle D Laurent Journal: J Comput Aided Mol Des Date: 2018-10-28 Impact factor: 3.686