Small molecule inhibitors of the class 1 receptor tyrosine kinase family
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Updated: Aug 11, 2026

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
Published on: September 18, 2013
G Stuart Cockerill1, Karen E Lackey
1Drug Discovery, Arrow Therapeutics, Britannia House, 7 Trinity Street, London. SE1 1DS UK and GlaxoSmithKline, Discovery Research Kinase Chemistry, 5 Moore Dr, Research Triangle Park, NC 27709, USA. jacques.dumas.b@bayer.com
Abstract:
This review covers literature describing research progress in erbB family tyrosine kinase inhibition over the last year. Excellent recent reviews are available, thus we have focussed on current developments of leading small molecule drug candidates as well as their erbB family inhibition profile. The most advanced erbB family tyrosine kinase (TK) inhibitors are demonstrating promising anti-cancer activity in clinical trials and are discussed. Several inhibition strategies are emerging: EGFR TK selective, irreversible TK inhibition and dual EGFR/erbB2 TK inhibitors. While small structural differences are seen in the leading compounds, the variations in their inhibition profiles and compound properties suggest that biological systems judge structural diversity differently. The readers' attention is drawn to common issues of selectivity and potency generally encountered with kinase inhibitors.
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