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Aliagas-Martin, Ignacio; Burdick, Dan; Corson, Laura; Dotson, Jennafer; Drummond, Jason; Fields, Carter; Huang, Oscar W; Hunsaker, Thomas; Kleinheinz, Tracy; Krueger, Elaine; Liang, Jun; Moffat, John; Phillips, Gail; Pulk, Rebecca; Rawson, Thomas E; Ultsch, Mark; Walker, Leslie; Wiesmann, Christian; Zhang, Birong; Zhu, Bing-Yan; Cochran, Andrea G
Journal of medicinal chemistry, 05/2009, Letnik: 52, Številka: 10Journal Article
The two major Aurora kinases carry out critical functions at distinct mitotic stages. Selective inhibitors of these kinases, as well as pan-Aurora inhibitors, show antitumor efficacy and are now under clinical investigation. However, the ATP-binding sites of Aurora A and Aurora B are virtually identical, and the structural basis for selective inhibition has therefore not been clear. We report here a class of bisanilinopyrimidine Aurora A inhibitors with excellent selectivity for Aurora A over Aurora B, both in enzymatic assays and in cellular phenotypic assays. Crystal structures of two of the inhibitors in complex with Aurora A implicate a single amino acid difference in Aurora B as responsible for poor inhibitory activity against this enzyme. Mutation of this residue in Aurora B (E161T) or Aurora A (T217E) is sufficient to swap the inhibition profile, suggesting that this difference might be exploited more generally to achieve high selectivity for Aurora A.
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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Vir: Osebne bibliografije
in: SICRIS
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