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
Hauptverfasser: Yan, Aixia, Wang, Liyu, Xu, Shuyu, Xu, Jun
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creator Yan, Aixia
Wang, Liyu
Xu, Shuyu
Xu, Jun
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.
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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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