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New Stem Cells Findings from N. Weygant et al Outlined (Small molecule kinase inhibitor LRRK2-IN-1 demonstrates potent activity against colorectal...

August 5, 2014



New Stem Cells Findings from N. Weygant et al Outlined (Small molecule kinase inhibitor LRRK2-IN-1 demonstrates potent activity against colorectal and pancreatic cancer through inhibition of doublecortin-like kinase 1)

By a News Reporter-Staff News Editor at Cancer Weekly -- Fresh data on Stem Cell Research are presented in a new report. According to news reporting out of Oklahoma City, Oklahoma, by NewsRx editors, research stated, "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."

Our news journalists obtained a quote from the research, "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. Here we report that LRRK2-IN-1 demonstrates potent anti-cancer activity including inhibition of cancer cell proliferation, migration, and invasion as well as induction of apoptosis and cell cycle arrest. Additionally we found that it regulates stemness, epithelial-mesenchymal transition, and oncogenic targets on the molecular level. Moreover, we show that LRRK2-IN-1 suppresses DCLK1 kinase activity and downstream DCLK1 effector c-MYC, and demonstrate that DCLK1 kinase activity is a significant factor in resistance to LRRK2-IN-1. Given DCLK1's tumor stem cell marker status, a strong understanding of its biological role and interactions in gastrointestinal tumors may lead to discoveries that improve patient outcomes."

According to the news editors, the research concluded: "The results of this study suggest that small molecule inhibitors of DCLK1 kinase should be further investigated as they may hold promise as anti-tumor stem cell drugs."

For more information on this research see: Small molecule kinase inhibitor LRRK2-IN-1 demonstrates potent activity against colorectal and pancreatic cancer through inhibition of doublecortin-like kinase 1. Molecular Cancer, 2014;13():1-14. Molecular Cancer can be contacted at: Biomed Central Ltd, 236 Grays Inn Rd, Floor 6, London WC1X 8HL, England. (BioMed Central - www.biomedcentral.com/; Molecular Cancer - www.molecular-cancer.com)

Our news journalists report that additional information may be obtained by contacting N. Weygant, COARE Biotechnol, Oklahoma City, OK, United States. Additional authors for this research include D.F. Qu, W.L. Berry, R. May, P. Chandrakesan, D.B. Owen, S.M. Sureban, N. Ali, R. Janknecht and C.W. Houchen (see also Stem Cell Research).

Keywords for this news article include: Genetics, Oncology, Colorectal, Oklahoma City, United States, Nanotechnology, Gastroenterology, Pancreatic Cancer, Stem Cell Research, Pancreatic Neoplasms, Emerging Technologies, Enzymes and Coenzymes, North and Central America, Small Molecule Kinase Inhibitors

Our reports deliver fact-based news of research and discoveries from around the world. Copyright 2014, NewsRx LLC


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Source: Cancer Weekly


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