Novel imatinib derivatives with altered specificity between Bcr-Abl and FMS, KIT, and PDGF receptors.

Journal article

Imatinib is a clinically important ATP analogue inhibitor that targets the tyrosine kinase domain of the intracellular Abl kinase and the PDGF receptor family. Imatinib has revolutionised the treatment of chronic myeloid leukaemia, which is caused by the oncogene Bcr-Abl and certain solid tumours that harbor oncogenic mutations of the PDGF receptor family. As a leading kinase inhibitor, imatinib also provides an excellent model system to investigate how changes in drug design impact biologica...

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Authors: Skobridis, K; Kinigopoulou, M; Theodorou, V; Giannousi, E; Russell, A

• Journal: ChemMedChem
• Volume: 5
• Issue: 1
• Pages: 130-139
• Publication date: 2010-01-01
• DOI: 10.1002/cmdc.200900394
• EISSN: 1860-7187
• ISSN: 1860-7179
• Language: English
• Keywords: Binding Sites; Humans; Antineoplastic Agents; Animals; Benzamides; Piperazines; Substrate Specificity; Receptor, Macrophage Colony-Stimulating Factor; Cell Line, Tumor; Mice; Receptors, Platelet-Derived Growth Factor; Pyrimidines; Fusion Proteins, bcr-abl; Protein Kinase Inhibitors; K562 Cells; Phosphorylation; Drug Design; Proto-Oncogene Proteins c-kit; Computer Simulation