Cytoplasmic translocation of nuclear LSD1 (
            <i>KDM1A</i>
            ) in human hepatoma cells is induced by its inhibitors

Yabuta, Suemi; Shidoji, Yoshihiro

doi:10.2217/hep-2018-0008

Cited by 7 publications

(6 citation statements)

References 41 publications

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“…It is a critical factor for mammalian development and many cellular processes (Shi et al, 2004). KDM1A constitutes a potential epigenetic target for drug therapy as suggested by its homology with MAOB in structure (Yabuta & Shidoji, 2019). An increasing number of researches have validated that the high expression levels of KDM1A is related to the poor prognosis of multiple cancers (Huang et al, 2017; Maiques‐Diaz & Somervaille, 2016).…”

Section: Discussionmentioning

confidence: 99%

ORY‐1001, a KDM1A inhibitor, inhibits proliferation, and promotes apoptosis of triple negative breast cancer cells by inactivating androgen receptor

Zhang

Sun

2021

Drug Development Research

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Breast cancer (BC), which is widely considered as the most common cancer in women around the world, evokes ~1.7 million new BC cases and 522,000 BC‐related deaths each year. Triple negative breast cancer (TNBC) is clinically confirmed as one of the most aggressive subtypes of BC. ORY‐1001, a clinically used lysine specific demethylase 1 (LSD1/KDM1A) inhibitor, was investigated herein to confirm its role in the progression of TNBC and reveal the potential mechanism. After treatment with ORY‐1001 in MDA‐MB‐231 and BT549 cells, the cell proliferation and apoptosis were respectively measured by CCK‐8 and TUNEL assays. The expression of proliferation‐ and apoptosis‐associated proteins was tested by means of western blot analysis. Then, R1881, an androgen receptor (AR) agonist, was used to evaluate whether the effects of ORY‐1001 on proliferation and apoptosis of TNBC cells was mediated by regulating AR. Results indicated that ORY‐1001 treatment restrained the proliferation while enhanced the apoptosis of BC cells, accompanied by the change of proliferation‐ and apoptosis‐related proteins expression. Furthermore, ORY‐1001 reduced the level of AR in BC cells. After the activation of AR by R1881, the decreased proliferation and enhanced apoptosis of BC cells triggered by ORY‐1001 intervention were partially abolished. In conclusion, this paper has presented the first evidence to suggest that ORY‐1001 inhibits proliferation and promotes apoptosis of TNBC cells by suppressing AR expression, which may constitute the theoretical basis for the clinical use of ORY‐1001 in the treatment of this disease.

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Section: Discussionmentioning

confidence: 99%

ORY‐1001, a KDM1A inhibitor, inhibits proliferation, and promotes apoptosis of triple negative breast cancer cells by inactivating androgen receptor

Zhang

Sun

2021

Drug Development Research

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“…GGA [XI] and several of its dihydro derivatives inhibited active recombinant human LSD1 ( 100 ). Furthermore, GGA treatment of HuH-7 cells resulted in rapid migration of nuclear-localized LSD1 to the cytoplasm ( 101 ), indicating that GGA [XI] may have epigenetic effects on cells.…”

Section: Other Biological Functions Of Ggamentioning

confidence: 99%

Geranylgeranoic acid, a bioactive and endogenous fatty acid in mammals: a review

Shidoji

2023

Journal of Lipid Research

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“…LSD1 is mainly localized in the nucleus, while pharmacological intervention could cause a translocation of LSD1 from the nucleus to the cytoplasm ( Yabuta and Shidoji, 2019 ). In tau pathology, Christopher et al (2017) found LSD1 is localized to tau aggregates and sequestered in the cytoplasm, and proposed that the reduction of LSD1 in nucleus impairs the survival of hippocampal and cortical.…”

Section: Lysine-specific Demethylase 1 and Tau Proteinmentioning

confidence: 99%

Biological and therapeutic role of LSD1 in Alzheimer’s diseases

Zhao

et al. 2022

Front. Pharmacol.

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Alzheimer’s disease (AD) is a common chronic neurodegenerative disease characterized by cognitive learning and memory impairments, however, current treatments only provide symptomatic relief. Lysine-specific demethylase 1 (LSD1), regulating the homeostasis of histone methylation, plays an important role in the pathogenesis of many neurodegenerative disorders. LSD1 functions in regulating gene expression via transcriptional repression or activation, and is involved in initiation and progression of AD. Pharmacological inhibition of LSD1 has shown promising therapeutic benefits for AD treatment. In this review, we attempt to elaborate on the role of LSD1 in some aspects of AD including neuroinflammation, autophagy, neurotransmitters, ferroptosis, tau protein, as well as LSD1 inhibitors under clinical assessments for AD treatment.

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Cytoplasmic translocation of nuclear LSD1 ( KDM1A ) in human hepatoma cells is induced by its inhibitors

Cited by 7 publications

References 41 publications

ORY‐1001, a KDM1A inhibitor, inhibits proliferation, and promotes apoptosis of triple negative breast cancer cells by inactivating androgen receptor

ORY‐1001, a KDM1A inhibitor, inhibits proliferation, and promotes apoptosis of triple negative breast cancer cells by inactivating androgen receptor

Geranylgeranoic acid, a bioactive and endogenous fatty acid in mammals: a review

Biological and therapeutic role of LSD1 in Alzheimer’s diseases

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