赖氨酸特异性去甲基化酶1选择性失活剂：蛋白质靶向药物递送机制 - Suppr

Lysine-specific demethylase 1-selective inactivators: protein-targeted drug delivery mechanism.

作者信息

Ogasawara Daisuke, Itoh Yukihiro, Tsumoto Hiroki, Kakizawa Taeko, Mino Koshiki, Fukuhara Kiyoshi, Nakagawa Hidehiko, Hasegawa Makoto, Sasaki Ryuzo, Mizukami Tamio, Miyata Naoki, Suzuki Takayoshi

机构信息

Graduate School of Medical Science, Kyoto Prefectural University of Medicine, 13 Nishitakatsukasa-cho, Taishogun Kita-ku, Kyoto 603-8334, Japan.

出版信息

Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8620-4. doi: 10.1002/anie.201303999. Epub 2013 Jul 3.

DOI:10.1002/anie.201303999

PMID:23824985

Abstract

摘要

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Lysine-specific demethylase 1-selective inactivators: protein-targeted drug delivery mechanism.赖氨酸特异性去甲基化酶1选择性失活剂：蛋白质靶向药物递送机制

Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8620-4. doi: 10.1002/anie.201303999. Epub 2013 Jul 3.

Design, Synthesis, and In Vitro Evaluation of Novel Histone H3 Peptide-Based LSD1 Inactivators Incorporating α,α-Disubstituted Amino Acids with γ-Turn-Inducing Structures.新型组蛋白 H3 肽基 LSD1 失活剂的设计、合成及体外评价，其中包含具有 γ-转角诱导结构的α,α-二取代氨基酸。

Molecules. 2018 May 6;23(5):1099. doi: 10.3390/molecules23051099.

cis-Cyclopropylamines as mechanism-based inhibitors of monoamine oxidases.顺式环丙胺作为单胺氧化酶的基于机制的抑制剂。

FEBS J. 2015 Aug;282(16):3190-8. doi: 10.1111/febs.13260. Epub 2015 Mar 27.

Identification of cell-active lysine specific demethylase 1-selective inhibitors.鉴定细胞活性赖氨酸特异性去甲基化酶 1 选择性抑制剂。

J Am Chem Soc. 2009 Dec 9;131(48):17536-7. doi: 10.1021/ja907055q.

Structural insight into inhibitors of flavin adenine dinucleotide-dependent lysine demethylases.黄素腺嘌呤二核苷酸依赖性赖氨酸去甲基化酶抑制剂的结构洞察

Epigenetics. 2017 May 4;12(5):340-352. doi: 10.1080/15592294.2017.1290032. Epub 2017 Feb 10.

Identification of Novel Selective Lysine-Specific Demethylase 1 (LSD1) Inhibitors Using a Pharmacophore-Based Virtual Screening Combined with Docking.基于药效团的虚拟筛选结合对接技术鉴定新型选择性赖氨酸特异性去甲基化酶1（LSD1）抑制剂

Chem Biol Drug Des. 2015 Jun;85(6):659-71. doi: 10.1111/cbdd.12461. Epub 2014 Dec 22.

Irreversible LSD1 Inhibitors: Application of Tranylcypromine and Its Derivatives in Cancer Treatment.不可逆 LSD1 抑制剂：反苯环丙胺及其衍生物在癌症治疗中的应用。

Curr Top Med Chem. 2016;16(19):2179-88. doi: 10.2174/1568026616666160216154042.

trans-2-Phenylcyclopropylamine is a mechanism-based inactivator of the histone demethylase LSD1.反式-2-苯基环丙胺是一种基于机制的组蛋白去甲基化酶LSD1失活剂。

Biochemistry. 2007 Apr 10;46(14):4408-16. doi: 10.1021/bi0618621. Epub 2007 Mar 17.

Synthesis, biological activity and mechanistic insights of 1-substituted cyclopropylamine derivatives: a novel class of irreversible inhibitors of histone demethylase KDM1A.1-取代环丙胺衍生物的合成、生物活性及作用机制研究：一类新型组蛋白去甲基化酶KDM1A不可逆抑制剂

Eur J Med Chem. 2014 Oct 30;86:352-63. doi: 10.1016/j.ejmech.2014.08.068. Epub 2014 Aug 27.

Histone H3 lysine 4 demethylation is a target of nonselective antidepressive medications.组蛋白H3赖氨酸4去甲基化是非选择性抗抑郁药物的作用靶点。

Chem Biol. 2006 Jun;13(6):563-7. doi: 10.1016/j.chembiol.2006.05.004.

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Effect of a Novel Antidepressant and Anticancer Nuc01 on Depression in Cancer Survivors.新型抗抑郁和抗癌药物Nuc01对癌症幸存者抑郁的影响。

Curr Issues Mol Biol. 2025 Jul 24;47(8):587. doi: 10.3390/cimb47080587.

The roles of histone modifications in tumorigenesis and associated inhibitors in cancer therapy.组蛋白修饰在肿瘤发生中的作用以及癌症治疗中的相关抑制剂。

J Natl Cancer Cent. 2022 Sep 28;2(4):277-290. doi: 10.1016/j.jncc.2022.09.002. eCollection 2022 Dec.

KDM1A/LSD1 inhibition enhances chemotherapy response in ovarian cancer.KDM1A/LSD1抑制作用增强卵巢癌化疗反应。

Mol Carcinog. 2024 Oct;63(10):2026-2039. doi: 10.1002/mc.23792. Epub 2024 Jul 11.

Pharmacological inhibition of KDM1A/LSD1 enhances estrogen receptor beta-mediated tumor suppression in ovarian cancer.KDM1A/LSD1的药理学抑制增强了雌激素受体β介导的卵巢癌肿瘤抑制作用。

Cancer Lett. 2023 Oct 28;575:216383. doi: 10.1016/j.canlet.2023.216383. Epub 2023 Sep 14.

LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials.用于癌症治疗的 LSD1 抑制剂：聚焦于多靶点药物及临床试验中的化合物。

Front Pharmacol. 2023 Feb 2;14:1120911. doi: 10.3389/fphar.2023.1120911. eCollection 2023.

Lysine-specific histone demethylase 1A (KDM1A/LSD1) inhibition attenuates DNA double-strand break repair and augments the efficacy of temozolomide in glioblastoma.赖氨酸特异性组蛋白去甲基化酶 1A（KDM1A/LSD1）抑制减弱了 DNA 双链断裂修复，并增强了替莫唑胺在胶质母细胞瘤中的疗效。

Neuro Oncol. 2023 Jul 6;25(7):1249-1261. doi: 10.1093/neuonc/noad018.

Cancer-Cell-Selective Targeting by Arylcyclopropylamine-Vorinostat Conjugates.芳基环丙胺-伏立诺他缀合物对癌细胞的选择性靶向作用。

ACS Med Chem Lett. 2022 Sep 12;13(10):1568-1573. doi: 10.1021/acsmedchemlett.2c00126. eCollection 2022 Oct 13.

KDM1A inhibition augments the efficacy of rapamycin for the treatment of endometrial cancer.KDM1A 抑制增强了雷帕霉素治疗子宫内膜癌的疗效。

Cancer Lett. 2022 Jan 1;524:219-231. doi: 10.1016/j.canlet.2021.10.019. Epub 2021 Oct 18.

KDM1A inhibition is effective in reducing stemness and treating triple negative breast cancer.抑制 KDM1A 可有效降低三阴性乳腺癌的干性并进行治疗。

Breast Cancer Res Treat. 2021 Jan;185(2):343-357. doi: 10.1007/s10549-020-05963-1. Epub 2020 Oct 14.

Synthesis of artificial substrate based on inhibitor for detecting LSD1 activity.基于抑制剂的用于检测LSD1活性的人工底物的合成。

J Clin Biochem Nutr. 2020 Sep;67(2):153-158. doi: 10.3164/jcbn.20-9. Epub 2020 May 15.

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Lysine-specific demethylase 1-selective inactivators: protein-targeted drug delivery mechanism.

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