A living cell-based fluorescent reporter for high-throughput screening of anti-tumor drugs
Suppression of cellular O-linked β-N-acetylglucosaminylation (O-GlcNAcylation) can repress proliferation and migration of various cancer cells, which opens a new avenue for cancer therapy. Based on the regulation of insulin gene transcription, we designed a cell-based fluorescent reporter capable of...
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| Main Authors: | , , , , , , , |
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| Format: | Book |
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Elsevier,
2021-12-01T00:00:00Z.
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|---|---|---|---|
| 001 | doaj_eadd0b976b1c4f58b91f973e48c44a0a | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Ningning Tang |e author |
| 700 | 1 | 0 | |a Ling Li |e author |
| 700 | 1 | 0 | |a Fei Xie |e author |
| 700 | 1 | 0 | |a Ying Lu |e author |
| 700 | 1 | 0 | |a Zifan Zuo |e author |
| 700 | 1 | 0 | |a Hao Shan |e author |
| 700 | 1 | 0 | |a Quan Zhang |e author |
| 700 | 1 | 0 | |a Lianwen Zhang |e author |
| 245 | 0 | 0 | |a A living cell-based fluorescent reporter for high-throughput screening of anti-tumor drugs |
| 260 | |b Elsevier, |c 2021-12-01T00:00:00Z. | ||
| 500 | |a 2095-1779 | ||
| 500 | |a 10.1016/j.jpha.2021.04.001 | ||
| 520 | |a Suppression of cellular O-linked β-N-acetylglucosaminylation (O-GlcNAcylation) can repress proliferation and migration of various cancer cells, which opens a new avenue for cancer therapy. Based on the regulation of insulin gene transcription, we designed a cell-based fluorescent reporter capable of sensing cellular O-GlcNAcylation in HEK293T cells. The fluorescent reporter mainly consists of a reporter (green fluorescent protein (GFP)), an internal reference (red fluorescent protein), and an operator (neuronal differentiation 1), which serves as a "sweet switch" to control GFP expression in response to cellular O-GlcNAcylation changes. The fluorescent reporter can efficiently sense reduced levels of cellular O-GlcNAcylation in several cell lines. Using the fluorescent reporter, we screened 120 natural products and obtained one compound, sesamin, which could markedly inhibit protein O-GlcNAcylation in HeLa and human colorectal carcinoma-116 cells and repress their migration in vitro. Altogether, the present study demonstrated the development of a novel strategy for anti-tumor drug screening, as well as for conducting gene transcription studies. | ||
| 546 | |a EN | ||
| 690 | |a Fluorescent reporter | ||
| 690 | |a High-throughput screening | ||
| 690 | |a O-linked β-N-acetylglucosaminylation | ||
| 690 | |a Anti-tumor drug | ||
| 690 | |a Gene transcriptional regulation | ||
| 690 | |a Therapeutics. Pharmacology | ||
| 690 | |a RM1-950 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Journal of Pharmaceutical Analysis, Vol 11, Iss 6, Pp 808-814 (2021) | |
| 787 | 0 | |n http://www.sciencedirect.com/science/article/pii/S2095177921000356 | |
| 787 | 0 | |n https://doaj.org/toc/2095-1779 | |
| 856 | 4 | 1 | |u https://doaj.org/article/eadd0b976b1c4f58b91f973e48c44a0a |z Connect to this object online. |