Title |
Small molecule kinase inhibitor LRRK2-IN-1 demonstrates potent activity against colorectal and pancreatic cancer through inhibition of doublecortin-like kinase 1
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Published in |
Molecular Cancer, May 2014
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DOI | 10.1186/1476-4598-13-103 |
Pubmed ID | |
Authors |
Nathaniel Weygant, Dongfeng Qu, William L Berry, Randal May, Parthasarathy Chandrakesan, Daniel B Owen, Sripathi M Sureban, Naushad Ali, Ralf Janknecht, Courtney W Houchen |
Abstract |
Doublecortin-like kinase 1 (DCLK1) is emerging as a tumor specific stem cell marker in colorectal and pancreatic cancer. Previous in vitro and in vivo studies have demonstrated the therapeutic effects of inhibiting DCLK1 with small interfering RNA (siRNA) as well as genetically targeting the DCLK1+ cell for deletion. However, the effects of inhibiting DCLK1 kinase activity have not been studied directly. Therefore, we assessed the effects of inhibiting DCLK1 kinase activity using the novel small molecule kinase inhibitor, LRRK2-IN-1, which demonstrates significant affinity for DCLK1. |
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