The long-awaited structure of HIPK2
- Author(s)
- Murphy, JM;
- Details
- Publication Year 2019-09-13,Volume 294,Issue #37,Page 13560-13561
- Journal Title
- Journal of Biological Chemistry
- Publication Type
- Journal Article
- Abstract
- Homeodomain-interacting protein kinases (HIPKs) are kinases that phosphorylate transcription factors involved in cell proliferation, differentiation, and apoptosis. Their structures have been long sought because of their potential as drug targets in cancers and fibrosis. Agnew and colleagues present the first crystal structure of the HIPK2 kinase domain, complexed with the small-molecule inhibitor CX-4945, revealing important structural differences from related protein kinases of the DYRK family. This structure provides a starting point to exploit HIPK2's distinct structural features to develop selective small-molecule inhibitors of this kinase.
- Publisher
- ASBMB
- Research Division(s)
- Inflammation
- PubMed ID
- 31519758
- Link To PubMed Central Version
- https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6746442/
- Publisher's Version
- https://doi.org/10.1074/jbc.H119.010675
- NHMRC Grants
- NHMRC/1105754, NHMRC/1124735, NHMRC/1124737,
- Terms of Use/Rights Notice
- Refer to copyright notice on published article.
Creation Date: 2019-09-20 10:16:25
Last Modified: 2020-02-03 08:27:03