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1
Facile synthesis of substituted trans-2-arylcyclopropylamine inhibitors of the human histone demethylase LSD1 and monoamine oxidases A and B.
Bioorg Med Chem Lett. 2008 May 15;18(10):3047-51. doi: 10.1016/j.bmcl.2008.01.003. Epub 2008 Jan 8.
2
trans-2-Phenylcyclopropylamine is a mechanism-based inactivator of the histone demethylase LSD1.
Biochemistry. 2007 Apr 10;46(14):4408-16. doi: 10.1021/bi0618621. Epub 2007 Mar 17.
3
Structural basis for the inhibition of the LSD1 histone demethylase by the antidepressant trans-2-phenylcyclopropylamine.
Biochemistry. 2007 Jul 10;46(27):8058-65. doi: 10.1021/bi700664y. Epub 2007 Jun 15.
5
Tying up tranylcypromine: Novel selective histone lysine specific demethylase 1 (LSD1) inhibitors.
Eur J Med Chem. 2017 Dec 1;141:101-112. doi: 10.1016/j.ejmech.2017.09.073. Epub 2017 Oct 3.
7
Development and Structural Evaluation of N-Alkylated trans-2-Phenylcyclopropylamine-Based LSD1 Inhibitors.
ChemMedChem. 2020 May 6;15(9):787-793. doi: 10.1002/cmdc.202000014. Epub 2020 Mar 30.
8
Crystal structure of histone demethylase LSD1 and tranylcypromine at 2.25 A.
Biochem Biophys Res Commun. 2008 Feb 1;366(1):15-22. doi: 10.1016/j.bbrc.2007.11.066. Epub 2007 Nov 26.
9
Towards the development of activity-based probes for detection of lysine-specific demethylase-1 activity.
Bioorg Med Chem. 2017 Feb 1;25(3):847-856. doi: 10.1016/j.bmc.2016.11.043. Epub 2016 Dec 1.
10
Fluorinated tranylcypromine analogues as inhibitors of lysine-specific demethylase 1 (LSD1, KDM1A).
Bioorg Med Chem Lett. 2017 May 15;27(10):2099-2101. doi: 10.1016/j.bmcl.2017.03.081. Epub 2017 Mar 29.

引用本文的文献

1
Discovery of novel dual-target inhibitors of LSD1/EGFR for non-small cell lung cancer therapy.
Acta Pharmacol Sin. 2025 Apr;46(4):1030-1044. doi: 10.1038/s41401-024-01439-w. Epub 2025 Jan 3.
4
Targeting the LSD1/KDM1 Family of Lysine Demethylases in Cancer and Other Human Diseases.
Adv Exp Med Biol. 2023;1433:15-49. doi: 10.1007/978-3-031-38176-8_2.
5
Inhibition of FAD-dependent lysine-specific demethylases by chiral polyamine analogues.
RSC Adv. 2018 Oct 31;8(64):36895-36902. doi: 10.1039/c8ra07879c. eCollection 2018 Oct 26.
6
Machine-Learning-Enabled Virtual Screening for Inhibitors of Lysine-Specific Histone Demethylase 1.
Molecules. 2021 Dec 10;26(24):7492. doi: 10.3390/molecules26247492.
8
New histone demethylase LSD1 inhibitor selectively targets teratocarcinoma and embryonic carcinoma cells.
Bioorg Med Chem. 2018 May 1;26(8):1523-1537. doi: 10.1016/j.bmc.2018.01.031. Epub 2018 Feb 7.
9
Inhibitors of Protein Methyltransferases and Demethylases.
Chem Rev. 2018 Feb 14;118(3):989-1068. doi: 10.1021/acs.chemrev.6b00801. Epub 2017 Mar 24.
10
Structural insight into inhibitors of flavin adenine dinucleotide-dependent lysine demethylases.
Epigenetics. 2017 May 4;12(5):340-352. doi: 10.1080/15592294.2017.1290032. Epub 2017 Feb 10.

本文引用的文献

1
Structural basis for the inhibition of the LSD1 histone demethylase by the antidepressant trans-2-phenylcyclopropylamine.
Biochemistry. 2007 Jul 10;46(27):8058-65. doi: 10.1021/bi700664y. Epub 2007 Jun 15.
2
trans-2-Phenylcyclopropylamine is a mechanism-based inactivator of the histone demethylase LSD1.
Biochemistry. 2007 Apr 10;46(14):4408-16. doi: 10.1021/bi0618621. Epub 2007 Mar 17.
3
The putative oncogene GASC1 demethylates tri- and dimethylated lysine 9 on histone H3.
Nature. 2006 Jul 20;442(7100):307-11. doi: 10.1038/nature04837. Epub 2006 May 28.
4
The transcriptional repressor JHDM3A demethylates trimethyl histone H3 lysine 9 and lysine 36.
Nature. 2006 Jul 20;442(7100):312-6. doi: 10.1038/nature04853. Epub 2006 May 28.
5
Reversal of histone lysine trimethylation by the JMJD2 family of histone demethylases.
Cell. 2006 May 5;125(3):467-81. doi: 10.1016/j.cell.2006.03.028. Epub 2006 Apr 6.
6
JHDM2A, a JmjC-containing H3K9 demethylase, facilitates transcription activation by androgen receptor.
Cell. 2006 May 5;125(3):483-95. doi: 10.1016/j.cell.2006.03.027. Epub 2006 Apr 6.
7
Histone demethylation by a family of JmjC domain-containing proteins.
Nature. 2006 Feb 16;439(7078):811-6. doi: 10.1038/nature04433. Epub 2005 Dec 18.
8
Histone demethylation catalysed by LSD1 is a flavin-dependent oxidative process.
FEBS Lett. 2005 Apr 11;579(10):2203-7. doi: 10.1016/j.febslet.2005.03.015.
9
Histone demethylation mediated by the nuclear amine oxidase homolog LSD1.
Cell. 2004 Dec 29;119(7):941-53. doi: 10.1016/j.cell.2004.12.012.

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