Encyclopedia of Cancer

Living Edition
| Editors: Manfred Schwab

UCN-01 Anticancer Drug

  • Holger Bastians
Living reference work entry
DOI: https://doi.org/10.1007/978-3-642-27841-9_6091-2

Synonyms

Definition

UCN-01 is an indolocarbazole compound originally isolated from Streptomyces spec. cultures, similar to staurosporine, but with an additional hydroxy group on the lactam ring (Fig. 1). It acts as an ATP competitive inhibitor targeting several kinases including protein kinase C (PKC), cyclin-dependent kinases, and Chk1 and shows high preclinical and clinical antitumor activity. UCN-01 can abrogate DNA damage-induced cell cycle arrest in S and G2 phases of the cell cycle and thereby sensitize tumor cells to DNA damage-induced toxicity. Currently, several phase I/II clinical trials explore UCN-01 as a stand-alone therapy or in combination with various DNA-damaging chemotherapeutic drugs.

Keywords

Aurora Kinase Spindle Assembly Checkpoint Spindle Checkpoint Mitotic Catastrophe Chk1 Kinase 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
This is a preview of subscription content, log in to check access.

References

  1. Eastman A (2004) Cell cycle checkpoints and their impact on anticancer therapeutic strategies. J Cell Biochem 91:223–231CrossRefPubMedGoogle Scholar
  2. Fuse E, Kuwabara T, Sparreboom A et al (2005) Review of UCN-01 development: a lesson in the importance of clinical pharmacology. J Clin Pharmacol 45:394–403CrossRefPubMedGoogle Scholar
  3. Kawabe T (2004) G2 checkpoint abrogators as anticancer drugs. Mol Cancer Ther 3:513–519PubMedGoogle Scholar
  4. Vogel C, Hager C, Bastians H (2007) Mechanisms of mitotic cell death induced by chemotherapy mediated G2 checkpoint abrogation. Cancer Res 67:339–345CrossRefPubMedGoogle Scholar

See Also

  1. (2012) CHK1. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 817. doi:10.1007/978-3-642-16483-5_1101Google Scholar
  2. (2012) DNA replication. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 1141. doi:10.1007/978-3-642-16483-5_1690Google Scholar
  3. (2012) G2 checkpoint abrogation. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 1484. doi:10.1007/978-3-642-16483-5_2293Google Scholar
  4. (2012) P53. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 2747. doi:10.1007/978-3-642-16483-5_4331Google Scholar
  5. (2012) PDK1. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 2804. doi:10.1007/978-3-642-16483-5_4426Google Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 2012

Authors and Affiliations

  1. 1.Abt. Molekulare OnkologieUniversitätsmedizin GöttingenGöttingenGermany