دورية أكاديمية
Proteasome inhibitors suppress MYB oncogenic activity in a p300-dependent manner.
العنوان: | Proteasome inhibitors suppress MYB oncogenic activity in a p300-dependent manner. |
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المؤلفون: | Yusenko MV; Institute for Biochemistry, Westfälische-Wilhelms-Universität, Münster, Germany., Biyanee A; Institute for Biochemistry, Westfälische-Wilhelms-Universität, Münster, Germany., Andersson MK; Sahlgrenska Cancer Center, Department of Pathology, University of Gothenburg, Gothenburg, Sweden., Radetzki S; Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), Berlin, Germany., von Kries JP; Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), Berlin, Germany., Stenman G; Sahlgrenska Cancer Center, Department of Pathology, University of Gothenburg, Gothenburg, Sweden., Klempnauer KH; Institute for Biochemistry, Westfälische-Wilhelms-Universität, Münster, Germany. Electronic address: klempna@uni.muenster.de. |
المصدر: | Cancer letters [Cancer Lett] 2021 Nov 01; Vol. 520, pp. 132-142. Date of Electronic Publication: 2021 Jul 10. |
نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't |
اللغة: | English |
بيانات الدورية: | Publisher: Elsevier Science Ireland Country of Publication: Ireland NLM ID: 7600053 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1872-7980 (Electronic) Linking ISSN: 03043835 NLM ISO Abbreviation: Cancer Lett Subsets: MEDLINE |
أسماء مطبوعة: | Publication: Limerick : Elsevier Science Ireland Original Publication: Amsterdam, Elsevier/North-Holland. |
مواضيع طبية MeSH: | Carcinoma, Adenoid Cystic/*drug therapy , E1A-Associated p300 Protein/*genetics , Leukemia, Myeloid, Acute/*drug therapy , Proto-Oncogene Proteins c-myb/*genetics, Carcinoma, Adenoid Cystic/genetics ; Carcinoma, Adenoid Cystic/pathology ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Humans ; Leukemia, Myeloid, Acute/genetics ; Leukemia, Myeloid, Acute/pathology ; Molecular Targeted Therapy ; Proteasome Endopeptidase Complex/drug effects ; Proteasome Endopeptidase Complex/genetics ; Proteasome Inhibitors/pharmacology |
مستخلص: | Studies of the role of MYB in human malignancies have highlighted MYB as a potential drug target for acute myeloid leukemia (AML) and adenoid cystic carcinoma (ACC). Although transcription factors are often considered un-druggable, recent work has demonstrated successful targeting of MYB by low molecular weight compounds. This has fueled the notion that inhibition of MYB has potential as a therapeutic approach against MYB-driven malignancies. Here, we have used a MYB reporter cell line to screen a library of FDA-approved drugs for novel MYB inhibitors. We demonstrate that proteasome inhibitors have significant MYB-inhibitory activity, prompting us to characterize the proteasome inhibitor oprozomib in more detail. Oprozomib was shown to interfere with the ability of the co-activator p300 to stimulate MYB activity and to exert anti-proliferative effects on human AML and ACC cells. Overall, our work demonstrated suppression of oncogenic MYB activity as a novel result of proteasome inhibition. (Copyright © 2021 Elsevier B.V. All rights reserved.) |
فهرسة مساهمة: | Keywords: Adenoid cystic carcinoma; Inhibitor; MYB; Myeloid leukemia; Proteasome inhibitor |
المشرفين على المادة: | 0 (MYB protein, human) 0 (Proteasome Inhibitors) 0 (Proto-Oncogene Proteins c-myb) EC 2.3.1.48 (E1A-Associated p300 Protein) EC 2.3.1.48 (EP300 protein, human) EC 3.4.25.1 (Proteasome Endopeptidase Complex) |
تواريخ الأحداث: | Date Created: 20210713 Date Completed: 20220107 Latest Revision: 20220107 |
رمز التحديث: | 20231215 |
DOI: | 10.1016/j.canlet.2021.07.010 |
PMID: | 34256093 |
قاعدة البيانات: | MEDLINE |
تدمد: | 1872-7980 |
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DOI: | 10.1016/j.canlet.2021.07.010 |