Discovery of an Indirubin Derivative as a Novel c-Met Kinase Inhibitor with In Vitro Anti-Tumor Effects.
作者： Karyn Muzinga Ndolo , Su Jin An , Kyeong Ryang Park , Hyo Jeong Lee , Kyoung Bin Yoon
DOI: 10.4062/BIOMOLTHER.2018.091
关键词:
摘要: The c-Met protein is a receptor tyrosine kinase involved in cell growth, proliferation, survival, and angiogenesis of several human tumors. Overexpression has been found gastric cancers correlated with poor prognosis. Indirubin the active component Danggui Longhui Wan, which traditional Chinese antileukemic recipe. In present study, we tested anti-cancer effects an indirubin derivative, LDD-1937, on cancer cells SNU-638. When performed vitro assay against activity, LDD-1937 inhibited activity c-Met. This result was confirmed by immunoblot immunofluorescence phosphorylated Immunoblot analysis showed that decreased expression Erk1/2, STAT3, STAT5, Akt, downstream proteins addition, reduced viability suppressed colony formation migration SNU-638 cells. Furthermore, induced G2/M phase arrest decreasing levels cyclin B1 CDC2. Cleaved-PARP, apoptosis-related protein, up-regulated treated LDD-1937. Overall, this study suggests may be novel small-molecule therapeutic potential for selectively inhibiting pathways overexpressing
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