Covalent inhibition of NSD1 histone methyltransferase

The nuclear receptor-binding SET domain (NSD) family of histone methyltransferases is associated with various malignancies, including aggressive acute leukemia with NUP98-NSD1 translocation. While NSD proteins represent attractive drug targets, their catalytic SET domains exist in autoinhibited conf...

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Veröffentlicht in:	Nat. Chem. Biol 2020-12, Vol.16 (12), p.1403-1410
Hauptverfasser:	Huang, Huang, Howard, Christina A., Zari, Sergei, Cho, Hyo Je, Shukla, Shirish, Li, Hao, Ndoj, Juliano, González-Alonso, Paula, Nikolaidis, Caroline, Abbott, Joshua, Rogawski, David S., Potopnyk, Mykhaylo A., Kempinska, Katarzyna, Miao, Hongzhi, Purohit, Trupta, Henderson, Andrew, Mapp, Anna, Sulis, Maria Luisa, Ferrando, Adolfo, Grembecka, Jolanta, Cierpicki, Tomasz
Format:	Artikel
Sprache:	eng
Schlagworte:	631/92/458 631/92/607 631/92/613 Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Binding Binding Sites Biochemical Engineering Biochemistry Bioorganic Chemistry Cell Biology Chemistry Chemistry and Materials Science Chemistry/Food Science Coordination compounds Covalence Crystal structure Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Gene expression Gene Expression Regulation, Leukemic Histone H3 Histone methyltransferase Histone-Lysine N-Methyltransferase - antagonists & inhibitors Histone-Lysine N-Methyltransferase - genetics Histone-Lysine N-Methyltransferase - metabolism Histones Homeodomain Proteins - genetics Homeodomain Proteins - metabolism Humans Inhibitors Kinases Kinetics Leukemia Leukemia - drug therapy Leukemia - enzymology Leukemia - genetics Leukemia - pathology Leukocytes - drug effects Leukocytes - enzymology Leukocytes - pathology Lysine Models, Molecular Myeloid Ecotropic Viral Integration Site 1 Protein - genetics Myeloid Ecotropic Viral Integration Site 1 Protein - metabolism Nuclear Pore Complex Proteins - genetics Nuclear Pore Complex Proteins - metabolism Oncogene Proteins, Fusion - antagonists & inhibitors Oncogene Proteins, Fusion - genetics Oncogene Proteins, Fusion - metabolism Optimization Protein Binding Protein Conformation, alpha-Helical Protein Conformation, beta-Strand Protein Interaction Domains and Motifs Proteins Receptors Signal Transduction Substrate Specificity Therapeutic targets Translocation Tumor Cells, Cultured
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