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Volasertib Inhibition Infographic thumb
 
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Volasertib* (compound code BI 6727)
Volasertib* (compound code BI 6727) is an investigational, potent, and selective inhibitor in vitro of PLK1, an important regulator of the cell cycle.
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Volasertib* and Polo-like kinase (Plk) Inhibition Infographic

01.05.2011

Volasertib*, a Boehringer Ingelheim investigational compound, is a potential first-in-class selective cell cycle kinase inhibitor targeting Plk1.

How is Plk 1 involved in the cell cycle process?
Cell division is essential for many of the body's functions, including reproduction, growth and tissue repair.1 Plk1 plays a role in several important steps during cell division, including the passage of cells through mitosis.2,3

Mode of action of volasertib*
In cancer, over-expression of Plk1 is associated with aggressive tumour growth and a poor prognosis in many cancers.4,5 Volasertib* is highly selective and works by inhibiting the activity of Plk1.6 Inhibition of Plk1 induces mitotic arrest (referred to as Polo Arrest) and apoptosis (cell death) in in-vivo tumour models, resulting in growth inhibition and tumour regression.7,8

*Volasertib (compound code BI 6727) is an investigational compound. Its safety and efficacy has not yet been fully established.

1. Johnson, D.G. Cyclins and cell cycle checkpoints. Annu Rev Pharmacol Toxicol.1999;39(1):295-312.
2. Schmit TL, Zhong W, Setaluri V, Spiegelman VS, Ahmad N. J Invest Dermatol. 2009;129(12):2843-2853.
3. Strebhardt K, Ullrich A. Tareting polo-like kinase 1 for cancer therapy. Nat Rev Cancer.2006;6(4):321-330.
4. Schöffski P. Polo-Like Kinase (PLK) Inhibitors in Preclinical and Early Clinical Development in Oncology. Oncologist. 2009;14(6):559-570.
5. Takai N, Hamanaka R, Yoshimatsu J, Miyakawa I. Oncogene. 2005;24(2):287-291.
6. Rudolph D, Steegmaier M, Hoffmann M, et al. Clin Cancer Res. 2009;15(9):3094-3102.
7. Liu X, Erikson RL.Polo-like kinase (Plk)1 depletion induces apoptosis in cancer cells. Proc Natl Acad Sci USA 2003;100: 5789-5794.
8. Lenart P, Petronczki M, Steegmaier M, et al. Curr Biol. 2007;17(4):304-315.
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