Journal
FUTURE MEDICINAL CHEMISTRY
Volume 12, Issue 14, Pages 1305-1326Publisher
FUTURE SCI LTD
DOI: 10.4155/fmc-2020-0082
Keywords
epigenetic domains; protein-protein interactions; small-molecule inhibitors
Categories
Funding
- Leukemia and Lymphoma Society [1340-17]
- Kura Oncology, Inc.
- [R01 CA207272]
- [R01 CA226759]
- [R01 CA240514]
- [R01 CA201204]
- [R01 CA160467]
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Epigenetic protein-protein interactions (PPIs) play essential roles in regulating gene expression, and their dysregulations have been implicated in many diseases. These PPIs are comprised of reader domains recognizing post-translational modifications on histone proteins, and of scaffolding proteins that maintain integrities of epigenetic complexes. Targeting PPIs have become focuses for development of small-molecule inhibitors and anticancer therapeutics. Here we summarize efforts to develop small-molecule inhibitors targeting common epigenetic PPI domains. Potent small molecules have been reported for many domains, yet small domains that recognize methylated lysine side chains on histones are challenging in inhibitor development. We posit that the development of potent inhibitors for difficult-to-prosecute epigenetic PPIs may be achieved by interdisciplinary approaches and extensive explorations of chemical space.
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