Journal
TRENDS IN PHARMACOLOGICAL SCIENCES
Volume 36, Issue 7, Pages 422-439Publisher
ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tips.2015.04.005
Keywords
cancer; protein kinase; lipid kinase; tyrosine kinase; serine/threonine kinase; crystal structure
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Funding
- Lundbeck Foundation [R140-2013-13835]
- Lundbeck Foundation [R141-2013-13835] Funding Source: researchfish
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Kinases have emerged as one of the most intensively pursued targets in current pharmacological research, especially for cancer, due to their critical roles in cellular signaling. To date, the US FDA has approved 28 small-molecule kinase inhibitors, half of which were approved in the past 3 years. While the clinical data of these approved molecules are widely presented and structure activity relationship (SAR) has been reported for individual molecules, an updated review that analyzes all approved molecules and summarizes current achievements and trends in the field has yet to be found. Here we present all approved small-molecule kinase inhibitors with an emphasis on binding mechanism and structural features, summarize current challenges, and discuss future directions in this field.
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