Abstract
Ala213 Leu83 Glu211 Glu81 Gln85 The optimisation of fragments to low nanomolar inhibitors can be achieved with a limited number of compounds, particularly if good structural data are available.3 In this work X-ray crystallographic structures were generated using a novel soakable form of Aurora A. Aurora kinases play a key role in the regulation of mitosis and in recent years have become attractive targets for the treatment of cancer.4 In addition to Aurora A and Aurora B, AT9283 was also found to inhibit a number of other kinases including JAK2 and imatinib-resistant Abl (T315I). AT9283 demonstrated in vivo efficacy in mouse xenograft models and is currently under evaluation in Phase I/II clinical trials.
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