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Abstract
Based on in vitro assays, we performed a High Throughput Screening (HTS) to identify kinase inhibitors among 10,000 small chemical compounds. In this didactic paper, we describe step-by-step the approach to validate the hits as well as the major pitfalls encountered in the development of active molecules. We propose a decision tree that could be adapted to most in vitro HTS.
Highlights
Aurora kinases are a family of serine/threonine protein kinases that play a key role in mitotic progression [1,2]
In the present review we describe step-by-step the high throughput screening (HTS) performed for selecting aurora kinase inhibitors in the French patrimonial library [14]
We selected molecules that inhibit aurora kinase by more than 80% at 15 μM
Summary
Aurora kinases are a family of serine/threonine protein kinases that play a key role in mitotic progression [1,2]. Aurora kinases are over-expressed in many cancers, including primary colon and breast cancers [1,9]. In light of these observations, aurora kinases have emerged as potential “druggable” targets for anti-cancer therapy and many small molecule inhibitors of aurora kinase have been developed [10,11,12,13,14]. Several of these ATP-competitive inhibitors are currently in clinical development. The approach followed to validate the hits is outlined and a decision tree is proposed
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