RNA Polymerase I Inhibition with CX-5461 as a Novel Therapeutic Strategy to TargetMYCin Multiple Myeloma

التفاصيل البيبلوغرافية
العنوان: RNA Polymerase I Inhibition with CX-5461 as a Novel Therapeutic Strategy to TargetMYCin Multiple Myeloma
المؤلفون: Jonathan J Keats, John Soon Yew Lim, Veerabhadran Baladandayuthapani, Hua Wang, Wencai Ma, Dongmin Gu, Isere Kuiatse, Jin He, Jing Yang, Zhiqiang Wang, Richard J. Jones, Robert Z. Orlowski, Sean O'Brien, Richard E. Davis, Hans C. Lee, Heather Lin
المصدر: British Journal of Haematology. 177:80-94
بيانات النشر: Wiley, 2017.
سنة النشر: 2017
مصطلحات موضوعية: 0301 basic medicine, Myeloma protein, Gene Expression, Antineoplastic Agents, Article, Proto-Oncogene Proteins c-myc, Mice, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, RNA Polymerase I, Ribosomal protein, Cell Line, Tumor, RNA polymerase, RNA polymerase I, Animals, Humans, Gene silencing, Benzothiazoles, Molecular Targeted Therapy, Naphthyridines, Messenger RNA, Gene Expression Profiling, Translation (biology), Hematology, Xenograft Model Antitumor Assays, Tumor Burden, Disease Models, Animal, 030104 developmental biology, chemistry, Drug Resistance, Neoplasm, 030220 oncology & carcinogenesis, Mutation, Cancer research, Tumor Suppressor Protein p53, Growth inhibition, Multiple Myeloma
الوصف: Dysregulation of MYC is frequently implicated in both early and late myeloma progression events, yet its therapeutic targeting has remained a challenge. Among key MYC downstream targets is ribosomal biogenesis, enabling increases in protein translational capacity necessary to support the growth and self-renewal programmes of malignant cells. We therefore explored the selective targeting of ribosomal biogenesis with the small molecule RNA polymerase (pol) I inhibitor CX-5461 in myeloma. CX-5461 induced significant growth inhibition in wild-type (WT) and mutant TP53 myeloma cell lines and primary samples, in association with increases in downstream markers of apoptosis. Moreover, Pol I inhibition overcame adhesion-mediated drug resistance and resistance to conventional and novel agents. To probe the TP53-independent mechanisms of CX-5461, gene expression profiling was performed on isogenic TP53 WT and knockout cell lines and revealed reduction of MYC downstream targets. Mechanistic studies confirmed that CX-5461 rapidly suppressed both MYC protein and MYC mRNA levels. The latter was associated with an increased binding of the RNA-induced silencing complex (RISC) subunits TARBP2 and AGO2, the ribosomal protein RPL5, and MYC mRNA, resulting in increased MYC transcript degradation. Collectively, these studies provide a rationale for the clinical translation of CX-5461 as a novel therapeutic approach to target MYC in myeloma.
تدمد: 0007-1048
DOI: 10.1111/bjh.14525
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::31461a52ac2f9f98ff245fdfa05ddabc
https://doi.org/10.1111/bjh.14525
Rights: OPEN
رقم الانضمام: edsair.doi.dedup.....31461a52ac2f9f98ff245fdfa05ddabc
قاعدة البيانات: OpenAIRE
الوصف
تدمد:00071048
DOI:10.1111/bjh.14525