Aurora-A kinase inhibitor scaffolds and binding modes
Aurora kinases (A–C) belong to the serine/threonine protein kinase family. In recent years, the constitutive or elevated expression of Aurora kinases has been found in cancer cells and oncogene transfected cells. In this review, we summarize the common binding modes of Aurora-A kinase inhibitors, th...
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Veröffentlicht in: | Drug discovery today 2011-03, Vol.16 (5), p.260-269 |
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description | Aurora kinases (A–C) belong to the serine/threonine protein kinase family. In recent years, the constitutive or elevated expression of Aurora kinases has been found in cancer cells and oncogene transfected cells. In this review, we summarize the common binding modes of Aurora-A kinase inhibitors, the hot spot residues in the binding sites and the privileged inhibitor structures. Our review of the reported chemical scaffolds of Aurora-A kinase inhibitors and their binding modes could provide a useful framework from which new design strategies for inhibitors might be assessed or developed. |
doi_str_mv | 10.1016/j.drudis.2010.12.003 |
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In recent years, the constitutive or elevated expression of Aurora kinases has been found in cancer cells and oncogene transfected cells. In this review, we summarize the common binding modes of Aurora-A kinase inhibitors, the hot spot residues in the binding sites and the privileged inhibitor structures. Our review of the reported chemical scaffolds of Aurora-A kinase inhibitors and their binding modes could provide a useful framework from which new design strategies for inhibitors might be assessed or developed.</description><subject>Animals</subject><subject>Aurora Kinases</subject><subject>Binding Sites</subject><subject>Biological and medical sciences</subject><subject>Drug Delivery Systems</subject><subject>Drug Design</subject><subject>General pharmacology</subject><subject>Humans</subject><subject>Medical sciences</subject><subject>Neoplasms - drug therapy</subject><subject>Neoplasms - physiopathology</subject><subject>Pharmaceutical technology. 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subjects | Animals Aurora Kinases Binding Sites Biological and medical sciences Drug Delivery Systems Drug Design General pharmacology Humans Medical sciences Neoplasms - drug therapy Neoplasms - physiopathology Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Protein Binding Protein Kinase Inhibitors - pharmacology Protein-Serine-Threonine Kinases - antagonists & inhibitors |
title | Aurora-A kinase inhibitor scaffolds and binding modes |
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