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Recent advances in novel anticancer agents targeting β-catenin/TCF4 interaction for molecular cancer therapeutics
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Zheng-hao FU, Gan-gan YAN, Hai-yan QI, Xiao-ping LIU, Yun-yu CHEN*
Acta Pharmaceutica Sinica | 2021, 56(5) : 1238 - 1245
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Acta Pharmaceutica Sinica | 2021, 56(5): 1238-1245
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Recent advances in novel anticancer agents targeting β-catenin/TCF4 interaction for molecular cancer therapeutics
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Zheng-hao FU, Gan-gan YAN, Hai-yan QI, Xiao-ping LIU, Yun-yu CHEN*
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  • Institute for Drug Screening and Evaluation, Wannan Medical College, Wuhu 241002, China
Published: 2021-05-12 doi: 10.16438/j.0513-4870.2021-0018
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Wnt/β-catenin signaling pathway plays an important role in the proliferation, growth, invasion, and metastasis of human cancers. Moreover, β-catenin/T-cell factor 4 (TCF4) interaction regulates the transcription of the key oncogenes in Wnt/β-catenin signaling pathway. Therefore, β-catenin/TCF4 interaction would be a promising therapeutic target for the development of highly selective anticancer agents. At present, most ongoing small-molecule inhibitors targeting β-catenin/TCF4 interaction, including PKF222-815, iCRT3/5/14, LF3, and sanguinarine, have been developed in preclinical studies for human cancer therapeutics. In this review, we summarized the research advances of up-to date inhibitors targeting β-catenin/TCF4 interaction, including the molecular structure and cellular functions of β-catenin in canonical Wnt signaling pathway. This review holds a hopeful avenue for the development of novel and highly selective Wnt inhibitors targeting β-catenin/TCF4 interaction for future anticancer strategy.

Wnt inhibitor  /  β-catenin/TCF4 interaction  /  β-catenin/LEF1 interaction  /  protein-protein interaction  /  anticancer activity
Zheng-hao FU, Gan-gan YAN, Hai-yan QI, Xiao-ping LIU, Yun-yu CHEN. Recent advances in novel anticancer agents targeting β-catenin/TCF4 interaction for molecular cancer therapeutics[J]. Acta Pharmaceutica Sinica, 2021 , 56 (5) : 1238 -1245 . DOI: 10.16438/j.0513-4870.2021-0018
Year 2021 volume 56 Issue 5
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doi: 10.16438/j.0513-4870.2021-0018
  • Receive Date:2021-01-05
  • Online Date:2025-12-18
  • Published:2021-05-12
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  • Received:2021-01-05
  • Revised:2021-01-26
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    Institute for Drug Screening and Evaluation, Wannan Medical College, Wuhu 241002, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
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Genus
种数
Number of
species
占总种数比例
Percentage of total
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鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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