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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.
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References
Eastman A (2004) Cell cycle checkpoints and their impact on anticancer therapeutic strategies. J Cell Biochem 91:223–231
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 45:394–403
Kawabe T (2004) G2 checkpoint abrogators as anticancer drugs. Mol Cancer Ther 3:513–519
Vogel C, Hager C, Bastians H (2007) Mechanisms of mitotic cell death induced by chemotherapy mediated G2 checkpoint abrogation. Cancer Res 67:339–345
See Also
(2012) CHK1. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 817. doi:10.1007/978-3-642-16483-5_1101
(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_1690
(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_2293
(2012) P53. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 2747. doi:10.1007/978-3-642-16483-5_4331
(2012) PDK1. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 2804. doi:10.1007/978-3-642-16483-5_4426
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© 2012 Springer-Verlag Berlin Heidelberg
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Bastians, H. (2012). UCN-01 Anticancer Drug. In: Schwab, M. (eds) Encyclopedia of Cancer. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-27841-9_6091-2
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DOI: https://doi.org/10.1007/978-3-642-27841-9_6091-2
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Publisher Name: Springer, Berlin, Heidelberg
Online ISBN: 978-3-642-27841-9
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