Journal
CHEMISTRY & BIOLOGY
Volume 22, Issue 6, Pages 689-703Publisher
CELL PRESS
DOI: 10.1016/j.chembiol.2015.04.019
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Funding
- European Union
- Engineering and Physical Sciences Research Council
- Biotechnology and Biological Sciences Research Council
- Medical Research Council [ML/L007266/1]
- Wellcome Trust
- Higher Education Funding Council for England
- EPSRC [EP/F032773/1, EP/J017639/1]
- EPSRC [EP/J016012/1, EP/J017639/1, EP/F032773/1] Funding Source: UKRI
- MRC [MR/L007266/1, MC_UU_12022/1, MC_UU_12022/8, G1001522] Funding Source: UKRI
- Engineering and Physical Sciences Research Council [EP/F032773/1, EP/J016012/1, EP/J017639/1] Funding Source: researchfish
- Medical Research Council [G1001522, MR/L007266/1, MC_UU_12022/1] Funding Source: researchfish
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Protein-protein interactions (PPIs) underlie the majority of biological processes, signaling, and disease. Approaches to modulate PPIs with small molecules have therefore attracted increasing interest over the past decade. However, there are a number of challenges inherent in developing small-molecule PPI inhibitors that have prevented these approaches from reaching their full potential. From target validation to small-molecule screening and lead optimization, identifying therapeutically relevant PPIs that can be successfully modulated by small molecules is not a simple task. Following the recent review by Arkin et al., which summarized the lessons learnt from prior successes, we focus in this article on the specific challenges of developing PPI inhibitors and detail the recent advances in chemistry, biology, and computation that facilitate overcoming them. We conclude by providing a perspective on the field and outlining four innovations that we see as key enabling steps for successful development of small-molecule inhibitors targeting PPIs.
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