Inhibition of USP10 induces degradation of oncogenic FLT3

An inhibitor of the deubiquitinase (DUB) USP10 regulates the degradation of oncogenic FLT3, thus defining USP10 as a DUB for FLT3 and providing a therapeutic approach for human acute myeloid leukemia in which FLT3 activation is dysregulated. Oncogenic forms of the kinase FLT3 are important therapeut...

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Veröffentlicht in:	Nature chemical biology Jg. 13; H. 12; S. 1207 - 1215
Hauptverfasser:	Weisberg, Ellen L, Schauer, Nathan J, Yang, Jing, Lamberto, Ilaria, Doherty, Laura, Bhatt, Shruti, Nonami, Atsushi, Meng, Chengcheng, Letai, Anthony, Wright, Renee, Tiv, Hong, Gokhale, Prafulla C, Ritorto, Maria Stella, De Cesare, Virginia, Trost, Matthias, Christodoulou, Alexandra, Christie, Amanda, Weinstock, David M, Adamia, Sophia, Stone, Richard, Chauhan, Dharminder, Anderson, Kenneth C, Seo, Hyuk-Soo, Dhe-Paganon, Sirano, Sattler, Martin, Gray, Nathanael S, Griffin, James D, Buhrlage, Sara J
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	New York Nature Publishing Group US 01.12.2017 Nature Publishing Group
Schlagworte:	13 13/1 13/106 13/109 13/31 13/95 49/98 59/5 631/67/1059 631/92/468 631/92/555 82/80 82/83 Acute myeloid leukemia Animal models Animals Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Biochemical Engineering Biochemistry Bioorganic Chemistry Cell Biology Cell Proliferation - drug effects Cell Survival - drug effects Chemistry Chemistry/Food Science Degradation Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Female fms-Like Tyrosine Kinase 3 - genetics fms-Like Tyrosine Kinase 3 - metabolism Humans Inhibitors Kinases Leukemia Leukemia, Myeloid, Acute - drug therapy Leukemia, Myeloid, Acute - metabolism Leukemia, Myeloid, Acute - pathology Mice Mice, Inbred NOD Molecular Structure Mutation Myeloid leukemia Neoplasms, Experimental - drug therapy Neoplasms, Experimental - metabolism Neoplasms, Experimental - pathology Pharmacology Proteasomes Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Rodents Small Molecule Libraries - chemistry Small Molecule Libraries - pharmacology Structure-Activity Relationship Thiophenes - chemistry Thiophenes - pharmacology Tumor Cells, Cultured Ubiquitin Ubiquitin - metabolism Ubiquitin Thiolesterase - antagonists & inhibitors Ubiquitin Thiolesterase - genetics Ubiquitin Thiolesterase - metabolism
ISSN:	1552-4450, 1552-4469, 1552-4469
Online-Zugang:	Volltext
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