Small molecule inhibitors of protein kinases in cancer- how to overcome resistance.
Small molecule protein kinase inhibitors show great promise as anti-cancer agents, however, de novo and acquired resistance present problems. These are reviewed and illustrated using the receptor tyrosine kinase, KIT, as an example. Emerging solutions are presented, such as targeting active kinase conformations.
Griffith
R
R
School of Environmental and Life Sciences, Faculty of Science and IT, University of Newcastle, Callaghan NSW 2308, Australia. renate.griffith@newcastle.edu.au
Brown
M N
MN
McCluskey
A
A
Ashman
L K
LK
D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D015195:Drug Design; D019008:Drug Resistance, Neoplasm; D006801:Humans; D015394:Molecular Structure; D009369:Neoplasms / Q000098:blood supply / Q000188:drug therapy*; D009389:Neovascularization, Pathologic / Q000188:drug therapy; D047428:Protein Kinase Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D011494:Protein Kinases / Q000737:chemistry / Q000187:drug effects*; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases