Please use this identifier to cite or link to this item: https://hdl.handle.net/10356/85086
Title: Investigation of human flap structure-specific endonuclease 1 (FEN1) activity on primer-template models and exploration of a substrate-based FEN1 inhibitor
Authors: Wu, Haixia
Ye, Ruijuan
Huang, Dejian
Li, Tianhu
Ba, Sai
Zhang, Hao
Lee, Jasmine Yiqin
Keywords: FEN1
Phosphorothioate
Issue Date: 2016
Source: Ba, S., Zhang, H., Lee, J. Y., Wu, H., Ye, R., Huang, D., et al. (2016). Investigation of human flap structure-specific endonuclease 1 (FEN1) activity on primer-template models and exploration of a substrate-based FEN1 inhibitor. Bioorganic & Medicinal Chemistry, 24(9), 1988-1992.
Series/Report no.: Bioorganic & Medicinal Chemistry
Abstract: Flap structure-specific endonuclease 1 (FEN1) is one of the enzymes that involve in Eukaryotic DNA replication and repair. Recent studies have proved that FEN1 is highly over-expressed in various types of cancer cells and is a drug target. However, a limited number of FEN1 inhibitors has been identified and approved. Herein, we investigate the catalytic activity of FEN1, and propose a substrate-based inhibitor. As a consequence, one of the phosphorothioate-modified substrates is proved to exhibit the most efficient inhibitory effect in our in vitro examinations. A novelly-designed substrate-based FEN1 inhibitor was accordingly constructed and determined a remarkable IC50 value.
URI: https://hdl.handle.net/10356/85086
http://hdl.handle.net/10220/43624
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2016.03.025
Rights: © 2016 Elsevier. This is the author created version of a work that has been peer reviewed and accepted for publication by Bioorganic & Medicinal Chemistry, Elsevier. It incorporates referee’s comments but changes resulting from the publishing process, such as copyediting, structural formatting, may not be reflected in this document. The published version is available at: [http://dx.doi.org/10.1016/j.bmc.2016.03.025].
Fulltext Permission: open
Fulltext Availability: With Fulltext
Appears in Collections:SPMS Journal Articles

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