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Development of the First-in-Class FEM1B-Recruiting Histone Deacetylase Degraders.
J Med Chem
January 2025
Department of Pharmaceutical and Cell Biological Chemistry, Pharmaceutical Institute, University of Bonn institution, An der Immenburg 4, Bonn 53121, Germany.
Targeted protein degradation (TPD) represents a promising alternative to conventional occupancy-driven protein inhibition. Despite the existence of more than 600 E3 ligases in the human proteome, so far only a few have been utilized for TPD of histone deacetylases (HDACs), which represent important epigenetic anticancer drug targets. In this study, we disclose the first-in-class Fem-1 homologue B (FEM1B)-recruiting HDAC degraders.
View Article and Find Full Text PDFKMT2A degradation is observed in decitabine-responsive acute lymphoblastic leukemia cells.
Mol Oncol
January 2025
Department of Medicine, Clinic III - Hematology, Oncology, Palliative Medicine, Rostock University Medical Center, Germany.
Hypermethylation of tumor suppressor genes is a hallmark of leukemia. The hypomethylating agent decitabine covalently binds, and degrades DNA (cytosine-5)-methyltransferase 1 (DNMT1). Structural similarities within DNA-binding domains of DNMT1, and the leukemic driver histone-lysine N-methyltransferase 2A (KMT2A) suggest that decitabine might also affect the latter.
View Article and Find Full Text PDFPhosphorylation of the prokaryotic histone-like protein H-NS modulates bacterial virulence in Salmonella Typhimurium.
Microbiol Res
December 2024
Department of Microbiology and Infectious Disease Center, NHC Key Laboratory of Medical Immunology, School of Basic Medical Sciences, Peking University Health Science Center, Beijing 100191, China; Department of Infectious Diseases, Peking University Third Hospital, Beijing, 100191, China. Electronic address:
H-NS is a prokaryotic histone-like protein that binds to bacterial chromosomal DNA with important regulatory roles in gene expression. Unlike histone proteins, hitherto post-translational modifications of H-NS are still largely uncharacterized, especially in bacterial pathogens. Salmonella Typhimurium is a primary enteric pathogen and its virulence is mainly dependent on specialized type III secretion systems (T3SSs), which were evolutionarily acquired via horizontal gene transfer.
View Article and Find Full Text PDFSlow-Binding and Covalent HDAC Inhibition: A New Paradigm?
JACS Au
November 2024
Laboratory of Chemistry and Biophysics of Macromolecules (LCBM), Institute of Chemical Sciences and Engineering (ISIC), School of Basic Sciences, École Polytechnique Fédérale de Lausanne (EPFL), CH-1015 Lausanne, Switzerland.
The dysregulated post-translational modification of proteins is an established hallmark of human disease. Through Zn-dependent hydrolysis of acyl-lysine modifications, histone deacetylases (HDACs) are key regulators of disease-implicated signaling pathways and tractable drug targets in the clinic. Early targeting of this family of 11 enzymes (HDAC1-11) afforded a first generation of broadly acting inhibitors with medicinal applications in oncology, specifically in cutaneous and peripheral T-cell lymphomas and in multiple myeloma.
View Article and Find Full Text PDFContribution of the paternal histone epigenome to the preimplantation embryo.
Front Cell Dev Biol
November 2024
Department of Animal Science, Texas A&M University, College Station, TX, United States.
The paternal germline contains a plethora of information that extends beyond DNA. Packaged within the sperm cell is a wealth of epigenetic information, including DNA methylation, small RNAs, and chromatin associated histone proteins and their covalently attached post-translational modifications. Paternal chromatin is particularly unique, as during the process of spermatogenesis, nearly all histones are evicted from the genome with only a small percentage retained in the mature sperm cell.
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