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The selectivity issue of aurora kinase inhibitors |
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17 Sep 2007 |
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Aurora kinases are a family of protein kinases essential for mitosis or cell division. Aurora isoforms A and B are overexpressed and/or amplified in many tumor types, but have different localizations and roles during the cell cycle. At present at least 11 different aurora kinase inhibitors are in clinical development for haematological and solid tumors. Another three aurora kinase inhibitors prepare for IND filing. The most advanced inhibitors of this molecular target are aurora pan-kinase inhibitors with the necessity of intravenous administration. Next generation aurora kinase inhibitors are more selective and target aurora A and B kinase and aim at oral administration. Mono-selective inhibitors prefer aurora A kinase over B kinase. Several approaches include aurora A and B kinase inhibition in a dual or multi-targeting approach. Merck & Co is among the driving forces in the field with three aurora kinase inhibitors in clinical development.
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