Results 71 to 80 of about 22,216 (225)

Targeting class I histone deacetylases by the novel small molecule inhibitor 4SC-202 blocks oncogenic hedgehog-GLI signaling and overcomes smoothened inhibitor resistance [PDF]

, 2017
Aberrant activation of Hedgehog (HH)/GLI signaling is causally involved in numerous human malignancies, including basal cell carcinoma (BCC) and medulloblastoma. HH pathway antagonists targeting smoothened (SMO), an essential effector of canonical HH/GLI
Aberger, Fritz, Bartz, René, Canettieri, Gianluca, Coni, Sonia, Del Burgo, Pedro, Elmer, Dominik P, Gruber, Wolfgang, Kohlhof, Hella, Neureiter, Daniel, Peer, Elisabeth, Sternberg, Christina, Tesanovic, Suzana, Vitt, Daniel   +12 more
core   +1 more source

Protein degradation of Lsd1 is mediated by Bre1 yet opposed by Lsd1-interacting lncRNAs during fly follicle development

iScience
Summary: Tissue development, homeostasis, and repair all require efficient progenitor expansion. Lysine-specific demethylase 1 (Lsd1) maintains plastic epigenetic states to promote progenitor proliferation while overexpressed Lsd1 protein causes ...
Chun Ting Lin, Ruei-Teng Ting, Yang-Hsuan Ou, Tzu-Ling Shao, Ming-Chia Lee   +4 more
doaj   +1 more source

Silencing Lysine-Specific Histone Demethylase 1 (LSD1) Causes Increased HP1-Positive Chromatin, Stimulation of DNA Repair Processes, and Dysregulation of Proliferation by Chk1 Phosphorylation in Human Endothelial Cells

Cells, 2019
The methylation of histone lysine residues modifies chromatin conformation and regulates the expression of genes implicated in cell metabolism. Lysine-specific demethylase 1 (LSD1) is a flavin-dependent monoamine oxidase that can demethylate mono- and ...
Martyna Wojtala, Arkadiusz Dąbek, Dorota Rybaczek, Agnieszka Śliwińska, Ewa Świderska, Katarzyna Słapek, Assam El-Osta, Aneta Balcerczyk   +7 more
doaj   +1 more source

β‐Aminoisobutyric Acid Alleviates Cisplatin‐Induced Muscle Atrophy by Regulating E3 Ubiquitin Ligases, Apoptosis, Amino Acid Metabolism, Autophagy, and Ferroptosis

Medicine Bulletin, EarlyView.
ABSTRACT Background Cisplatin (CIS) is a widely used broad‐spectrum anticancer agent, but its clinical application is often limited by severe adverse effects, including skeletal muscle atrophy, which compromises patients' quality of life and treatment efficacy.
Hao‐Zhe Wang, Wen‐Bi He, Huan Wang, Hao Wang, Wen‐Jun Fang, Meng‐Qian Li, Jiong‐Xing Huang, Fei‐Peng Chen, Hui‐Guo Wang, Lin Zhu, Xiao‐Guang Liu   +10 more
wiley   +1 more source

Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors [PDF]

, 2018
Here we report corin, a synthetic hybrid agent derived from the class I HDAC inhibitor (entinostat) and an LSD1 inhibitor (tranylcypromine analog). Enzymologic analysis reveals that corin potently targets the CoREST complex and shows more sustained ...
A Laugesen, B Al-Lazikani, B Apsel, B Oronsky, BM Bolstad, C Binda, CA Lipinski, CH Arrowsmith, CM Johannessen, D Hayward, D Zingg, F Forneris, G Yan, HP Mohammad, J Bostrom, JC Culhane, JC Culhane, JE Bradner, JM Erikson, K Inui, K Luger, K Piotukh, K Yamanaka, KJ Falkenberg, L Jin, LM Szewczuk, M Yu, MA Dawson, MC Alley, MP Martin, N Portolano, P Prusevich, PH Huang, PJ Watson, PN Dyer, R Breslow, R Brown, R Li, RA Copeland, RA Copeland, RA Irizarry, RH Shoemaker, S Mimasu, SN Vasilatos, T Beckers, T Itoh, YC Duan   +46 more
core   +4 more sources

The dual role of LSD1 and HDAC3 in STAT5-dependent transcription is determined by protein interactions, binding affinities, motifs and genomic positions [PDF]

, 2016
STAT5 interacts with other factors to control transcription, and the mechanism of regulation is of interest as constitutive active STAT5 has been reported in malignancies. Here, LSD1 and HDAC3 were identified as novel STAT5a interacting partners in pro-B
Demmers, J.A.A. (Jeroen), Katsantoni, E. (Eleni), Lavigne, M.D. (Matthieu D.), Lazou, V. (Vassiliki), Nanou, A. (Aikaterini), Paparountas, T. (Triantafillos), Thanos, D. (Dimitris), Toumpeki, C. (Chrisavgi)   +7 more
core   +3 more sources

CRISPR‐Cas9 Genome‐Wide Screening in Paediatric Cancer: Functional Genomics for Target Discovery and the Improvement of Existing Therapies

Medicinal Research Reviews, EarlyView.
ABSTRACT CRISPR‐Cas9 genome‐wide screening has been instrumental towards identifying novel targets for drug discovery in cancer research. However, much of this research has centred specifically on adult cancers, with paediatric cancers being underserviced by current research and screening.
Steven He, Patrick Connerty, Antoine de Weck   +2 more
wiley   +1 more source

Homologous recombination mutants cause differing lethality between h− and h+ Schizosaccharomyces pombe strains due to mat1 heterochromatin

The FEBS Journal, EarlyView.
Homologous recombination (HR) in Schizosaccharomyces pombe is essential when mating‐type switching–induced double‐strand breaks (DSBs) form at the mat1 locus. In h90 and h− strains, efficient mat1 DSB formation renders HR indispensable unless suppressors block these breaks.
Peter Kolesar, Siarhei Paliavoi, Barbora Stefanovie, Jan Josef Palecek   +3 more
wiley   +1 more source

SIB1‐SEC23A undergo ER to chloroplast relocalization to mediate immunity in Arabidopsis thaliana

Journal of Integrative Plant Biology, EarlyView.
SEC23A mediates membrane trafficking between the endoplasmic reticulum (ER) and Golgi apparatus and interacts with the immunity protein SIGMA FACTOR‐BINDING PROTEIN1 in Arabidopsis. Under stress, both proteins relocate from the ER to chloroplasts, suppressing photosynthesis genes and enhancing defense genes.
Jialin Peng, Huan Zhong, Jianan Zhang, Hailei Zhang, Wuzhen Liu, Yonglun Zeng, Liwen Jiang, Yiji Xia   +7 more
wiley   +1 more source

Targeting histone methyltransferases and demethylases in clinical trials for cancer therapy [PDF]

, 2016
Drawing of Object No ...
Ludovica Morera, Michael Lübbert, Manfred Jung   +2 more
core   +1 more source