Anti-Cancer Agents in Medicinal Chemistry

(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Michelle Prudhomme  
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex


Brutons Tyrosine Kinase as a New Therapeutic Target

Author(s): Fatih M. Uckun, Heather E. Tibbles, Alexei O. Vassilev.


Targeting Brutons tyrosine kinase (BTK) with a small molecule inhibitor may be useful in treatment of BTK-expressing malignancies because of the anti-apoptotic function of BTK in cancer cells. Furthermore, BTK inhibitors also exhibit anti-thrombotic properties that may be desirable in the context of the increased risk of thromboembolic complications in cancer patients. This review will focus on the role of BTK in drug resistance in cancer, thromboembolism, and various pathologic immune responses, such as graft versus host disease. The therapeutic potential of targeting BTK is illustrated by discussion of the biologic activity profile of the rationally designed BTK inhibitor LFM-A13.

Keywords: Rational drug design, tyrosine kinases, BTK, cancer, thromboembolism

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Article Details

Year: 2007
Page: [624 - 632]
Pages: 9
DOI: 10.2174/187152007784111331
Price: $58