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A robust photoluminescence screening assay identifies uracil-DNA glycosylase inhibitors against prostate cancer
Li,Guodong1; Henry,Stuart Adam2; Liu,Hao3; Kang,Tian Shu1; Nao,Sang Cuo1; Zhao,Yichao4; Wu,Chun3; Jin,Jianwen4; Zhang,Jia Tong1; Leung,Chung Hang1; Wai Hong Chan,Philip2,4; Ma,Dik Lung3
2020-02-21
Source PublicationChemical Science
ISSN2041-6520
Volume11Issue:7Pages:1750-1760
Abstract

Many cancers have developed resistance to 5-FU, due to removal by the enzyme uracil-DNA glycosylase (UDG), a type of base excision repair enzyme (BER) that can excise uracil and 5-fluorouracil (5-FU) from DNA. However, the development of UDG inhibitor screening methods, especially for the rapid and efficient screening of natural product/natural product-like compounds, is still limited so far. We developed herein a robust time-resolved photoluminescence method for screening UDG inhibitors, which could significantly improve sensitivity over the screening method based on the conventional steady-state spectroscopy, reducing the substantial fluorescence background interference. As a proof-of-concept, two potential UDG inhibitors were identified from a database of natural products and approved drugs. Co-treatment of these two compounds with 5-FU showed synergistic cytotoxicity, providing the basis for treating drug-resistant cancers. Overall, this method provides an avenue for the rapid screening of small molecule regulators of other BER enzyme activities that can avoid false negatives arising from the background fluorescence.

DOI10.1039/c9sc05623h
URLView the original
Indexed BySCIE
Language英語English
WOS Research AreaChemistry
WOS SubjectChemistry, Multidisciplinary
WOS IDWOS:000515704400027
Scopus ID2-s2.0-85081080567
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Cited Times [WOS]:9   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Corresponding AuthorLeung,Chung Hang; Wai Hong Chan,Philip; Ma,Dik Lung
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine,Institute of Chinese Medical Sciences,University of Macau,Macao
2.Department of Chemistry,University of Warwick,Coventry,CV4 7AL,United Kingdom
3.Department of Chemistry,Hong Kong Baptist University,Kowloon Tong,Hong Kong
4.School of Chemistry,Monash University,Clayton,3800,Australia
First Author AffilicationInstitute of Chinese Medical Sciences
Corresponding Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Li,Guodong,Henry,Stuart Adam,Liu,Hao,et al. A robust photoluminescence screening assay identifies uracil-DNA glycosylase inhibitors against prostate cancer[J]. Chemical Science,2020,11(7):1750-1760.
APA Li,Guodong,Henry,Stuart Adam,Liu,Hao,Kang,Tian Shu,Nao,Sang Cuo,Zhao,Yichao,Wu,Chun,Jin,Jianwen,Zhang,Jia Tong,Leung,Chung Hang,Wai Hong Chan,Philip,&Ma,Dik Lung.(2020).A robust photoluminescence screening assay identifies uracil-DNA glycosylase inhibitors against prostate cancer.Chemical Science,11(7),1750-1760.
MLA Li,Guodong,et al."A robust photoluminescence screening assay identifies uracil-DNA glycosylase inhibitors against prostate cancer".Chemical Science 11.7(2020):1750-1760.
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