Novel dual Src/Abl inhibitors for hematologic and solid malignancies
作者： Silvia Schenone , Chiara Brullo , Francesca Musumeci , Maurizio Botta
DOI: 10.1517/13543784.2010.499898
关键词: Proto-oncogene tyrosine-protein kinase Src 、 Clinical trial 、 Tyrosine kinase 、 Sequence homology 、 Myeloid leukemia 、 Dasatinib 、 Pharmacology 、 Medicine 、 Enzyme 、 ABL
摘要: Importance of the field: c-Src and Bcr-Abl are two non-receptor or cytoplasmic tyrosine kinases (TKs) that play important roles in development solid hematological malignancies. Indeed, Src is overexpressed hyperactivated a variety tumors, while causative agent chronic myeloid leukemia (CML), where also involved. The enzymes share significant sequence homology remarkable structural resemblance.Areas covered this review: ATP-competitive compounds originally developed as inhibitors, showed to be potent Abl inhibitors. Dasatinib, first dual Src/Abl inhibitor approved by US FDA 2006 for treatment imatinib-resistant CML, currently being tested several clinical trials different tumors. SKI-606 AZD0530 other inhibitors extensively animal models trials, but not entered into therapy yet.What reader will gain: In review we will...
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