Results 41 to 50 of about 12,929 (212)

SYNTHESIS, LSD1 INHIBITORY ACTIVITY, AND LSD1 BINDING MODEL OF OPTICALLY PURE LYSINE-PCPA CONJUGATES

Computational and Structural Biotechnology Journal, 2014
Compounds that inhibit the catalytic function of lysine-specific demethylase 1 (LSD1) are interesting as therapeutic agents. Recently, we identified three lysine-phenylcyclopropylamine conjugates, NCD18, NCD25, and NCD41, which are potent LSD1 inactivators.
Takayoshi Suzuki, Yosuke Ota, Yukihiro Itoh, Tamio Mizukami, Daisuke Ogasawara   +4 more
openaire   +4 more sources

Biological and therapeutic role of LSD1 in Alzheimer’s diseases

Frontiers in Pharmacology, 2022
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 ...
Yu Li, Yuanyuan Zhao, Xiaona Li, Liuqun Zhai, Hua Zheng, Ying Yan, Qiang Fu, Jinlian Ma, Haier Fu, Zhenqiang Zhang, Zhonghua Li   +10 more
openaire   +3 more sources

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 ...
Yadi Wu, Binhua P. Zhou
openaire   +3 more sources

Histone demethylase LSD1 restricts influenza A virus infection by erasing IFITM3-K88 monomethylation. [PDF]

PLoS Pathogens, 2017
The histone demethylase LSD1 has been known as a key transcriptional coactivator for DNA viruses such as herpes virus. Inhibition of LSD1 was found to block viral genome transcription and lytic replication of DNA viruses.
Jiaoyu Shan, Binbin Zhao, Zhao Shan, Jia Nie, Rong Deng, Rui Xiong, Andy Tsun, Weiqi Pan, Hanzhi Zhao, Ling Chen, Ying Jin, Zhikang Qian, Kawing Lui, Rui Liang, Dan Li, Bing Sun, Dimitri Lavillette, Ke Xu, Bin Li   +18 more
doaj   +1 more source

Lsd1 as a therapeutic target in Gfi1-activated medulloblastoma [PDF]

Nature Communications, 2019
AbstractDrugs that modify the epigenome are powerful tools for treating cancer, but these drugs often have pleiotropic effects, and identifying patients who will benefit from them remains a major clinical challenge. Here we show that medulloblastomas driven by the transcription factor Gfi1 are exquisitely dependent on the enzyme lysine demethylase 1 ...
Jianxun Wang, Serap Erkek, Serap Erkek, Lianne Q. Chau, Paul A. Northcott, Alexandra Garancher, Jessica M. Rusert, Vasilisa A. Rudneva, Robert J. Wechsler-Reya, Robert J. Wechsler-Reya, Helai P. Mohammad, Catherine A. Lee, Catherine A. Lee, Ozlem Aksoy, Robin Lea, Stefan M. Pfister, Silvia K. Tacheva-Grigorova, Marc Zapatka, H. Leighton Grimes, William A. Weiss   +19 more
openaire   +5 more sources

Natural products as LSD1 inhibitors for cancer therapy

Acta Pharmaceutica Sinica B, 2021
Natural products generally fall into the biologically relevant chemical space and always possess novel biological activities, thus making them a rich source of lead compounds for new drug discovery. With the recent technological advances, natural product-based drug discovery is now reaching a new era.
Xiaochuan Li, Zhiqiang Yu, Yuan Fang, Guochao Liao, Chao Yang, Qingchun Mu, Bin Yu, Bin Yu   +7 more
openaire   +4 more sources

Possible role of human ribonuclease dicer in the regulation of R loops

FEBS Open Bio, EarlyView.
R loops play an important role in regulating key cellular processes such as replication, transcription, centromere stabilization, or control of telomere length. However, the unscheduled accumulation of R loops can cause many diseases, including cancer, and neurodegenerative or inflammatory disorders. Interestingly, accumulating data indicate a possible
Klaudia Wojcik, Paulina Krzeminska, Anna Kurzynska‐Kokorniak   +2 more
wiley   +1 more source

Targeting Nuclear LSD1 to Reprogram Cancer Cells and Reinvigorate Exhausted T Cells via a Novel LSD1-EOMES Switch [PDF]

Frontiers in Immunology, 2020
Lysine specific demethylase 1 (LSD1) is a key epigenetic eraser enzyme implicated in cancer metastases and recurrence. Nuclear LSD1 phosphorylated at serine 111 (nLSD1p) has been shown to be critical for the development of breast cancer stem cells.
Wen Juan Tu, Wen Juan Tu, Robert D. McCuaig, Robert D. McCuaig, Abel H. Y. Tan, Kristine Hardy, Nabila Seddiki, Nabila Seddiki, Nabila Seddiki, Sayed Ali, Jane E. Dahlstrom, Jane E. Dahlstrom, Jane E. Dahlstrom, Elaine G. Bean, Jenny Dunn, Jade Forwood, Sofia Tsimbalyuk, Kate Smith, Kate Smith, Desmond Yip, Desmond Yip, Laeeq Malik, Laeeq Malik, Thiru Prasanna, Thiru Prasanna, Peter Milburn, Sudha Rao, Sudha Rao   +27 more
openaire   +4 more sources

Long non‐coding RNAs as therapeutic targets in head and neck squamous cell carcinoma and clinical application

FEBS Open Bio, EarlyView.
Long non‐coding RNAs (lncRNAs) occupy an abundant fraction of the eukaryotic transcriptome and an emerging area in cancer research. Regulation by lncRNAs is based on their subcellular localization in HNSCC. This cartoon shows the various functions of lncRNAs in HNSCC discussed in this review.
Ellen T. Tran, Ruchi A. Patel, Amogh Chariyamane, Ratna B. Ray   +3 more
wiley   +1 more source

LSD1: more than demethylation of histone lysine residues [PDF]

Experimental & Molecular Medicine, 2020
AbstractLysine-specific histone demethylase 1 (LSD1) represents the first example of an identified nuclear protein with histone demethylase activity. In particular, it plays a special role in the epigenetic regulation of gene expression, as it removes methyl groups from mono- and dimethylated lysine 4 and/or lysine 9 on histone H3 (H3K4me1/2 and ...
Perillo Bruno, Tramontano Alfonso, Pezone Antonio, Migliaccio Antimo   +3 more
openaire   +6 more sources