Taipei Medical University

A B C D E F G H I J K L M N O P Q R S T U V W X Y Z
Lin CP
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------>insert_date=20061213
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------>ISSN=0959-4973
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------>journal_name=Anticancer Drugs
------>paper_name=Small molecule c-Myc inhibitor, 10058-F4, inhibits proliferation and downregulates human telomerase reverse transcriptase and enhances chemosensitivity in human hepatocellular carcinoma
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------>fullAbstract=c-Myc oncogene is critical for the development of hepatocellular carcinoma. Given the successful use of small-molecule inhibitors on cancers, targeting c-Myc with small-molecule inhibitors represents a promising approach. The potential of using small-molecule c-Myc inhibitor, 10058-F4, was evaluated on hepatocellular carcinoma cell lines, HepG2 and Hep3B cells. HepG2 cells were more sensitive to 10058-F4 than Hep3B cells, as demonstrated by reduced cell viability, marked morphological changes and decreased c-Myc levels. 10058-F4 arrested the cell cycle (at G0/G1 phase) and induced apoptosis upon extended treatment. These observations might be attributable to the increased cyclin-dependent kinase inhibitor, p21, and decreased cyclin D3 levels. Besides, 10058-F4 also significantly decreased the alpha-fetoprotein levels, an indicator for hepatocellular carcinoma differentiation. We further found that 10058-F4 inhibited the transactivation of human telomerase reverse transcriptase, downregulated human telomerase reverse transcriptase expression and abrogated telomerase activity. In addition, pretreatment with 10058-F4 increased the chemosensitivity of HepG2 cells to low-dose doxorubicin, 5-fluorouracil and cisplatin. Therefore, small-molecule c-Myc inhibitors might represent a novel agent, alone or in combination with conventional chemotherapeutic agents, for anti-hepatocellular carcinoma therapy.
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------>authors2=Liu JD
------>authors3=Chow JM
------>authors4=Liu CR
------>authors5=Liu HE
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------>authors=Lin CP
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------>updateTitle=Small-molecule c-Myc inhibitor, 10058-F4, inhibits proliferation, downregulates human telomerase reverse transcriptase and enhances chemosensitivity in human hepatocellular carcinoma cells.
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------>no=2
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------>publish_year=2007
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A B C D E F G H I J K L M N O P Q R S T U V W X Y Z