YQ36: A Novel Bisindolylmaleimide Analogue Induces KBVCR Cell Death
Joint Authors
Zhou, Xinglu
Cao, Ji
Zhu, Difeng
Hu, Yongzhou
He, Qiaojun
Lou, Jianshu
Zhang, Lei
Yang, Bo
Ye, Qing
Source
Issue
Vol. 2009, Issue 2009 (31 Dec. 2009), pp.1-11, 11 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2009-12-06
Country of Publication
Egypt
No. of Pages
11
Main Subjects
Abstract EN
Overexpression of multidrug resistance proteins P-glycoprotein (P-gp, MDR1) causes resistance of the tumor cells against a variety of chemotherapeutic agents.
3-(1-methyl-1H-indol-3-yl)-1-phenyl-4-(1-(3-(piperidin-1-yl)propyl)-1H-pyrazolo[3,4-b]pyridine-3-yl)-1H-pyrrole-2,5-dione (YQ36) is a novel analogue of bisindolylmaleimide, which has been reported to overcome multidrug resistance.
Here, we dedicated to investigate the anticancer activity of YQ36 on KB/VCR cells.
The results revealed that YQ36 exhibited great antiproliferative activity on three parental cell lines and MDR1 overexpressed cell lines.
Moreover, the hypersensitivity of YQ36 was confirmed on the base of great apoptosis induction and unaltered intracellular drug accumulation in KB/VCR cells.
Further results suggested that YQ36 could not be considered as a substrate of P-gp, which contributed to its successfully escaping from the efflux mediated by P-gp.
Interestingly, we observed that YQ36 could accumulate in nucleus and induce DNA damage.
YQ36 could also induce the activation of caspase-3, imposing effects on the mitochondrial function.
Collectively, our data demonstrated that YQ36 exhibited potent activities against MDR cells, inducing DNA damage and triggering subsequent apoptosis via mitochondrial pathway.
American Psychological Association (APA)
Cao, Ji& Zhang, Lei& Ye, Qing& Zhou, Xinglu& Lou, Jianshu& Zhu, Difeng…[et al.]. 2009. YQ36: A Novel Bisindolylmaleimide Analogue Induces KBVCR Cell Death. BioMed Research International،Vol. 2009, no. 2009, pp.1-11.
https://search.emarefa.net/detail/BIM-988388
Modern Language Association (MLA)
Cao, Ji…[et al.]. YQ36: A Novel Bisindolylmaleimide Analogue Induces KBVCR Cell Death. BioMed Research International No. 2009 (2009), pp.1-11.
https://search.emarefa.net/detail/BIM-988388
American Medical Association (AMA)
Cao, Ji& Zhang, Lei& Ye, Qing& Zhou, Xinglu& Lou, Jianshu& Zhu, Difeng…[et al.]. YQ36: A Novel Bisindolylmaleimide Analogue Induces KBVCR Cell Death. BioMed Research International. 2009. Vol. 2009, no. 2009, pp.1-11.
https://search.emarefa.net/detail/BIM-988388
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-988388