Results 11 to 20 of about 11,397 (98)

Epigenetic regulation of LSD1 during mammary carcinogenesis [PDF]

Molecular & Cellular Oncology, 2014
Inheritable epigenetic regulation is integral to the dynamic control of gene expression under different stimuli for cellular homeostasis and disease progression. Histone methylation is a common and important type of chromatin modification. LSD1, the first known histone lysine-specific demethylase, operates as a key component of several corepressor ...
Wu, Yadi, Zhou, Binhua P
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Dual inhibitors of LSD1 and spermine oxidase [PDF]

MedChemComm, 2019
Dual inhibitors of LSD1 and SMOX, with no activity against N1-acetylpolyamine oxidase (PAOX).
Steven Holshouser, Matthew Dunworth, Tracy Murray-Stewart, Yuri K. Peterson, Pieter Burger, Joy Kirkpatrick, Huan-Huan Chen, Robert A. Casero, Patrick M. Woster   +8 more
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LSD1 and the chemistry of histone demethylation [PDF]

Current Opinion in Chemical Biology, 2007
The recent discovery that histone demethylation can be catalyzed by the flavin-dependent amine oxidase LSD1 has ushered in a new chapter in the chromatin-remodeling community. Herein, we discuss the rapid progress of the histone demethylase field including the recent identification of the non-heme iron-dependent histone demethylases (JmjC family), the ...
Jeffrey C, Culhane, Philip A, Cole
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Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors

ACS Medicinal Chemistry Letters, 2020
Leveraging the catalytic machinery of LSD1 (KDM1A), a series of covalent styrenylcyclopropane LSD1 inhibitors were identified. These inhibitors represent a new class of mechanism-based inhibitors that target and covalently label the FAD cofactor of LSD1.
Victor S. Gehling, John P. McGrath, Martin Duplessis, Avinash Khanna, Francois Brucelle, Rishi G. Vaswani, Alexandre Côté, Jacob Stuckey, Venita Watson, Richard T. Cummings, Srividya Balasubramanian, Priyadarshini Iyer, Priyanka Sawant, Andrew C. Good, Brian K. Albrecht, Jean-Christophe Harmange, James E. Audia, Steven F. Bellon, Patrick Trojer, Julian R. Levell   +19 more
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LSD1 demethylates histone and non-histone proteins [PDF]

Epigenetics, 2009
One of the key breakthroughs in the epigenetics/chromatin field in the last several years was the identification of enzymes capable of removing the methyl group from methylated lysines in histone proteins. Lysine-specific demethylase 1 (LSD1) was the first such enzyme identified, which has been shown to demethylate histone H3 on lysine 4 (H3K4) and ...
Thomas B, Nicholson, Taiping, Chen
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LSD1 protects against hippocampal and cortical neurodegeneration [PDF]

Nature Communications, 2017
AbstractTo investigate the mechanisms that maintain differentiated cells, here we inducibly delete the histone demethylase LSD1/KDM1A in adult mice. Loss of LSD1 leads to paralysis, along with widespread hippocampus and cortex neurodegeneration, and learning and memory defects.
Michael A. Christopher, Dexter A. Myrick, Benjamin G. Barwick, Amanda K. Engstrom, Kirsten A. Porter-Stransky, Jeremy M. Boss, David Weinshenker, Allan I. Levey, David J. Katz   +8 more
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Human Histone Demethylase LSD1 Reads the Histone Code [PDF]

Journal of Biological Chemistry, 2005
Human histone demethylase LSD1 is a flavin-dependent amine oxidase that catalyzes the specific removal of methyl groups from mono- and dimethylated Lys4 of histone H3. The N-terminal tail of H3 is subject to various covalent modifications, and a fundamental question in LSD1 biology is how these epigenetic marks affect the demethylase activity.
F. Forneris, C. Binda, M.A. Vanoni, E. Battaglioli, A. Mattevi   +4 more
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Targeting LSD1 and FOXA1 in prostate cancer

Nature Genetics, 2020
FOXA1 is a key pioneer factor in androgen-receptor activity but has been an elusive drug target. A new study shows that inhibition of the associated cofactor LSD1 modifies the methylation state of FOXA1, thus resulting in chromatin dissociation and tumor inhibition, even in models of treatment-resistant prostate cancer.
Omarjee, Soleilmane, Carroll, Jason S
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Discovery of an LSD1 PROTAC degrader

Proceedings of the National Academy of Sciences
Aberrant expression of lysine-specific demethylase 1 (LSD1) has been implicated in various cancers, including acute myeloid leukemia (AML). Recent studies have revealed both catalytic and noncatalytic oncogenic functions of LSD1, which cannot be effectively addressed by traditional small-molecule inhibitors.
Amir Hosseini, Xing Qiu, Yan Xiong, Ki Him Nicholas Chiang, Jerrel Catlett, Ines Kaltheuner, Zhijie Deng, Sudipta Ghosh, Yang Shi, Jian Jin   +9 more
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Pharmacological Inhibition of LSD1 for Cancer Treatment

Molecules, 2018
Lysine-specific demethylase 1A (LSD1, also named KDM1A) is a demethylase that can remove methyl groups from histones H3K4me1/2 and H3K9me1/2. It is aberrantly expressed in many cancers, where it impedes differentiation and contributes to cancer cell proliferation, cell metastasis and invasiveness, and is associated with inferior prognosis ...
Guan-Jun Yang, Pui-Man Lei, Suk-Yu Wong, Dik-Lung Ma, Chung-Hang Leung   +4 more
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