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Recent Progress of Src SH2 and SH3 Inhibitors as Anticancer Agents

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Src family tyrosine kinases (SFKs) play key roles in regulating signal transduction in cellular processes. However, hyper-activated SFKs lead to uncontrolled cell proliferation and cancers. For both Src SH2 and SH3 domains involve in the regulation of tumorigenesis signal pathways, the SH2 and SH3 inhibition strategies are expected to block the protein-protein interactions between SFKs and their corporation proteins to abolish the signal transduction. Many inhibitors of SH2 and SH3 domain have been identified. Herein, some predominant examples of these inhibitors are reviewed.

Keywords: Protein tyrosine kinases; SH2; SH3; Src kinases; inhibitor; nonpeptide; peptidomimetic; progress

Document Type: Research Article


Affiliations: Department of Biochemistry and Molecular Biology, Faculty of Basic Medical Sciences, Second Military Medical University, 800 Xiangyin Road, Shanghai 200433, P.R., China.

Publication date: April 1, 2010

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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