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Research progress in histone lysine demethylases inhibitors
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Bo YANG1, 2, *, Yan-qing CHEN1, Liang-ming ZHANG1, Sheng-yong YANG2, Lin-li LI2
Acta Pharmaceutica Sinica | 2017, 52(7) : 1102 - 1109
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Acta Pharmaceutica Sinica | 2017, 52(7): 1102-1109
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Research progress in histone lysine demethylases inhibitors
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Bo YANG1, 2, *, Yan-qing CHEN1, Liang-ming ZHANG1, Sheng-yong YANG2, Lin-li LI2
Affiliations
  • 1. Panzhihua Central Hospital, Panzihua 617067, China
  • 2. West China Center of Medical Sciences, Sichuan University, Chengdu 610041, China
Published: 2017-07-12 doi: 10.16438/j.0513-4870.2017-0012
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The methylation of histone lysine plays a pivotal role in epigenetic regulation of gene expression. Histone lysine methylation modifications have 5 sites within histone H3(K4, K9, K27, K36, K79) and 1 site within histone H4(K20). Methylation at various sites has been shown to lead to transcriptional activation or silencing. Histone lysine methyltransferases(HKMTs)and histone lysine demethylases(HKDMs)collectively regulate the methylation modification state of histone lysine. It was reported that the mis-regulation of HKDMs is associated with the occurring and resistance of numerous malignant tumors, so more and more attention are received to HKDMs. Therefore, it is great significant in the study and development of HKDMs inhibitors. The inhibitors could be served not only as a tool in the investigation of the biological function, but also could be used as novel anti-cancer agents in the anticancer therapy. In this review, we provide a short summary of the HKDMs inhibitors recently reported and their potential in the treatment of diseases.

epigenetics  /  histone lysine demethylases  /  inhibitor  /  anticancer therapy
Bo YANG, Yan-qing CHEN, Liang-ming ZHANG, Sheng-yong YANG, Lin-li LI. Research progress in histone lysine demethylases inhibitors[J]. Acta Pharmaceutica Sinica, 2017 , 52 (7) : 1102 -1109 . DOI: 10.16438/j.0513-4870.2017-0012
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Article Info
doi: 10.16438/j.0513-4870.2017-0012
  • Receive Date：2017-01-04
  • Online Date：2026-01-14
  • Published：2017-07-12
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  • Received：2017-01-04
  • Revised：2017-01-24
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    1. Panzhihua Central Hospital, Panzihua 617067, China
    2. West China Center of Medical Sciences, Sichuan University, Chengdu 610041, China
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多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
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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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