دورية أكاديمية
Preclinical testing of the glycogen synthase kinase-3β inhibitor tideglusib for rhabdomyosarcoma.
| العنوان: | Preclinical testing of the glycogen synthase kinase-3β inhibitor tideglusib for rhabdomyosarcoma. |
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| المؤلفون: | Bharathy N; Children's Cancer Therapy Development Institute, Beaverton, OR 97005, USA., Svalina MN; Children's Cancer Therapy Development Institute, Beaverton, OR 97005, USA., Settelmeyer TP; Children's Cancer Therapy Development Institute, Beaverton, OR 97005, USA., Cleary MM; Children's Cancer Therapy Development Institute, Beaverton, OR 97005, USA., Berlow NE; Children's Cancer Therapy Development Institute, Beaverton, OR 97005, USA., Airhart SD; The Jackson Laboratory, Sacramento, CA 95838, USA., Xiang S; The Jackson Laboratory, Sacramento, CA 95838, USA., Keck J; The Jackson Laboratory, Sacramento, CA 95838, USA., Hayden JB; Department of Orthopedics and Rehabilitation, Oregon Health & Science University, Portland, OR 97239, USA., Shern JF; Genetics Branch, Oncogenomics Section, Center for Cancer Research, National Institutes of Health, Bethesda, MD 20892, USA.; Pediatric Oncology Branch, Center for Cancer Research, National Institutes of Health, Bethesda, MD 20892, USA., Mansoor A; Department of Pathology, Oregon Health & Science University, Portland, OR 97239, USA., Lathara M; Omics Data Automation, Beaverton, OR 97005, USA., Srinivasa G; Omics Data Automation, Beaverton, OR 97005, USA., Langenau DM; Molecular Pathology, Cancer Center, and Regenerative Medicine, Massachusetts General Hospital, Boston, MA 02114, USA.; Harvard Stem Cell Institute, Cambridge, MA 02129, USA., Keller C; Children's Cancer Therapy Development Institute, Beaverton, OR 97005, USA. |
| المصدر: | Oncotarget [Oncotarget] 2017 Jun 16; Vol. 8 (38), pp. 62976-62983. Date of Electronic Publication: 2017 Jun 16 (Print Publication: 2017). |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Impact Journals Country of Publication: United States NLM ID: 101532965 Publication Model: eCollection Cited Medium: Internet ISSN: 1949-2553 (Electronic) Linking ISSN: 19492553 NLM ISO Abbreviation: Oncotarget Subsets: PubMed not MEDLINE |
| أسماء مطبوعة: | Original Publication: Albany, N.Y. : Impact Journals |
| مستخلص: | Rhabdomyosarcoma (RMS) is the most common childhood soft tissue sarcoma. RMS often arise from myogenic precursors and displays a poorly differentiated skeletal muscle phenotype most closely resembling regenerating muscle. GSK3β is a ubiquitously expressed serine-threonine kinase capable of repressing the terminal myogenic differentiation program in cardiac and skeletal muscle. Recent unbiased chemical screening efforts have prioritized GSK3β inhibitors as inducers of myodifferentiation in RMS, suggesting efficacy as single agents in suppressing growth and promoting self-renewal in zebrafish transgenic embryonal RMS (eRMS) models in vivo . In this study, we tested the irreversible GSK3β-inhibitor, tideglusib for in vivo efficacy in patient-derived xenograft models of both alveolar rhabdomyosarcoma (aRMS) and eRMS. Tideglusib had effective on-target pharmacodynamic efficacy, but as a single agent had no effect on tumor progression or myodifferentiation. These results suggest that as monotherapy, GSK3β inhibitors may not be a viable treatment for aRMS or eRMS. Competing Interests: CONFLICTS OF INTEREST The authors declare that they have no conflicts of interest. |
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| فهرسة مساهمة: | Keywords: GSK3β; myodifferentiation; patient-derived xenograft; preclinical testing; rhabdomyosarcoma |
| تواريخ الأحداث: | Date Created: 20171004 Latest Revision: 20220410 |
| رمز التحديث: | 20240829 |
| مُعرف محوري في PubMed: | PMC5609896 |
| DOI: | 10.18632/oncotarget.18520 |
| PMID: | 28968964 |
| قاعدة البيانات: | MEDLINE |
| تدمد: | 1949-2553 |
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| DOI: | 10.18632/oncotarget.18520 |