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KKB Hot Article: Targeting cancer with small molecule kinase inhibitors |
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Written by KKB
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Tuesday, 20 April 2010 19:43 |
| Citation: Targeting cancer with small molecule kinase inhibitors |
Authors: Zhang J, Yang PL, Gray NS.
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| PubMed PMID: 19104514 |
Abstract: Deregulation of kinase activity has emerged as a major mechanism by which cancer cells evade normal physiological constraints on growth and survival. To date, 11 kinase inhibitors have received US Food and Drug Administration approval as cancer treatments, and there are considerable efforts to develop selective small molecule inhibitors for a host of other kinases that are implicated in cancer and other diseases. Herein we discuss the current challenges in the field, such as designing selective inhibitors and developing strategies to overcome resistance mutations. This Review provides a broad overview of some of the approaches currently used to discover and characterize new kinase inhibitors.
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Targets: ABL1, AURKA, AURKB, CDK2, EGFR, IGF1R, INSR, KIT, NTRK1, RET, RPS6KA1, RPS6KA3 Number of SAR data points: 12 Number of Targets: 12
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Last Updated on Saturday, 20 August 2011 00:06 |