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Publication : mTOR kinase inhibitors as potential cancer therapeutic drugs.

First Author  Sun SY Year  2013
Journal  Cancer Lett Volume  340
Issue  1 Pages  1-8
PubMed ID  23792225 Mgi Jnum  J:204216
Mgi Id  MGI:5529853 Doi  10.1016/j.canlet.2013.06.017
Citation  Sun SY (2013) mTOR kinase inhibitors as potential cancer therapeutic drugs. Cancer Lett 340(1):1-8
abstractText  The mammalian target of rapamycin (mTOR) plays a critical role in the positive regulation of cell growth and survival primarily through direct interaction with raptor (forming mTORC complex 1; mTORC1) or rictor (forming mTOR complex 2; mTORC2). The mTOR axis is often activated in many types of cancer and thus has become an attractive cancer therapeutic target. The modest clinical anticancer activity of conventional mTOR allosteric inhibitors, rapamycin and its analogs (rapalogs), which preferentially inhibit mTORC1, in most types of cancer, has encouraged great efforts to develop mTOR kinase inhibitors (TORKinibs) that inhibit both mTORC1 and mTORC2, in the hope of developing a novel generation of mTOR inhibitors with better therapeutic efficacy than rapalogs. Several TORKinibs have been developed and actively studied pre-clinically and clinically. This review will highlight recent advances in the development and research of TORKinibs and discuss some potential issues or challenges in this area.
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