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BIOMARKER:

RXRA overexpression

i
Other names: RXRA, Retinoid X Receptor Alpha, NR2B1, Nuclear Receptor Subfamily 2 Group B Member 1, RXR-Alpha, RXRalpha, Retinoic Acid Receptor RXR-Alpha, Retinoid X Nuclear Receptor Alpha, Retinoid X Receptor, Alpha
Entrez ID:
21d
CALR but Not JAK2 Mutations Are Associated with an Overexpression of Retinoid X Receptor Alpha in Essential Thrombocythemia. (PubMed, Cancers (Basel))
The use of drugs targeting the activation or blockade of this target in the analyzed cell lines did not result in changes in cell viability. However, RXRA might be relevant in the disease, pointing to the need for future research testing retinoids and other drugs targeting RXRα for the treatment of ET patients.
Journal
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JAK2 (Janus kinase 2) • CALR (Calreticulin) • RXRA (Retinoid X Receptor Alpha)
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JAK2 mutation • CALR mutation • RXRA overexpression
5ms
Clinical • P1 data • Metastases
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FGFR3 (Fibroblast growth factor receptor 3) • PPARG (Peroxisome Proliferator Activated Receptor Gamma)
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RXRA overexpression
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FX-909
5ms
Novel phloretin-based combinations targeting glucose metabolism in hepatocellular carcinoma through GLUT2/PEPCK axis of action: in silico molecular modelling and in vivo studies. (PubMed, Med Oncol)
We investigated novel anti-HCC treatments through either the simultaneous inhibition of glycolysis and gluconeogenesis by "phloretin" and "sodium meta-arsenite", respectively (Combination 1); or the concurrent inhibition of glycolysis and induction of gluconeogenesis by phloretin and dexamethasone, respectively, (combination 2). Biochemically, both combinations caused a significant reduction in ATP levels, ALT, and AST activity compared to the other groups. In conclusion, we propose two novel phloretin-based combinations that can be used in treating HCC through the regulation of glucose metabolism and ATP production.
Preclinical • Journal
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CCND1 (Cyclin D1) • CASP3 (Caspase 3) • BECN1 (Beclin 1)
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CCND1 expression • RXRA overexpression
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Kominox (sodium metaarsenite)
8ms
Nuclear receptor RXRα binds the precursor of miR-103 to inhibit its maturation. (PubMed, BMC Biol)
Our findings unravel an unexpected role of transcription factor RXRα in specific miRNA maturation at post-transcriptional level through pre-miRNA binding, and present a mechanistic insight regarding RXRα role in breast cancer progression.
Journal
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RXRA overexpression
9ms
Vitamin D Receptor and Retinoid X Receptor Alpha in Melanocytic Benign Lesions and Melanoma. (PubMed, Am J Dermatopathol)
RXRα inversely correlated with mitosis, indicating that RXRα can have a role in proliferation control. VDR and RXRα may participate in the development of melanocytic lesions and be a future target of new studies and directed therapies.
Journal
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VDR (Vitamin D Receptor)
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RXRA overexpression
11ms
Modulating retinoid-X-receptor alpha (RXRA) expression sensitizes chronic myeloid leukemia cells to imatinib in vitro and reduces disease burden in vivo. (PubMed, Front Pharmacol)
Importantly, RXRA OE also led to the disruption of the oxidative capacity of these cells. Combining IM with clinically available RXRA ligands could form an alternative treatment strategy in CML patients with suboptimal response to IM.
Preclinical • Journal
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ABL1 (ABL proto-oncogene 1) • RARA (Retinoic Acid Receptor Alpha) • CD34 (CD34 molecule) • RXRA (Retinoid X Receptor Alpha)
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RXRA overexpression
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imatinib
over1year
Rxra Overexpression Improves the Sensitivity to Imatinib In-Vitro/in-Vivo By Disrupting the Oxidative Capacity of Chronic Myeloid Leukemia Cells (ASH 2022)
We then assessed the sensitivity to other TKIs nilotinib and dasatinib in the RXRA OE cells and found increased sensitivity...Next we assessed the effect of clinically available ligands specific to RXRA (Acitretin,Bexarotene and 9-cis-Retinoic acid) on CML CD34+ cells in combination with IM...Interestingly RXRA OE reduced the engraftment potential of CML cells in-vivo, indicating a mechanism for altering the stemness capacity of CML cells. Further work is ongoing to elucidate the molecular mechanisms orchestrated by RXRA in CML cells.
Preclinical
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase) • CD34 (CD34 molecule) • CRKL (CRK Like Proto-Oncogene, Adaptor Protein) • RXRA (Retinoid X Receptor Alpha)
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RXRA overexpression
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dasatinib • imatinib • Tasigna (nilotinib) • Targretin oral (bexarotene oral)