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Characterization of a highly selective inhibitor of the Aurora kinases
- Source :
- Bioorganic & Medicinal Chemistry Letters. 27:4405-4408
- Publication Year :
- 2017
- Publisher :
- Elsevier BV, 2017.
-
Abstract
- Aurora kinases play an essential role in mitosis and cell cycle regulation. In recent years Aurora kinases have proved popular cancer targets and many inhibitors have been developed. The majority of these clinical candidates are multi-targeted, rendering them inappropriate as tools for studying Aurora kinase mediated signaling. Here we report discovery of a highly selective inhibitor of Aurora kinases A, B and C, with potent cellular activity and minimal off-target activity (PLK4). The X-ray co-crystal structure of Aurora A in complex with compound 2 is reported, and provides insights into the structural determinants of ligand binding and selectivity.
- Subjects :
- 0301 basic medicine
PLK4
Clinical Biochemistry
Aurora inhibitor
Pharmaceutical Science
Antineoplastic Agents
macromolecular substances
Biochemistry
Structure-Activity Relationship
03 medical and health sciences
0302 clinical medicine
Aurora kinase
Aurora Kinases
Cell Line, Tumor
Drug Discovery
Humans
Transferase
Protein Kinase Inhibitors
Molecular Biology
Mitosis
Cell Proliferation
Dose-Response Relationship, Drug
Molecular Structure
Kinase
Chemistry
Organic Chemistry
Cell cycle
Highly selective
Cell biology
enzymes and coenzymes (carbohydrates)
030104 developmental biology
030220 oncology & carcinogenesis
embryonic structures
Molecular Medicine
Drug Screening Assays, Antitumor
biological phenomena, cell phenomena, and immunity
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 27
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....83d5823ee4e428302c7d1139190e2fb4