- •Individual treatments with RG-7388 and Selinexor are able to reduce the viability of ovarian cancer cells.
- •The ovarian cancer cells (A2780) treated with the drug combination produced higher levels of apoptosis.
- •The combination treatments with RG-7388 and Selinexor are involved in the induction of caspase-mediated apoptotic mechanism via up-regulation of MDM2, p53, phospho-p53, and p21.
- •The combination treatments enhanced the Inhibitory effects of MDM2 through blocking nuclear export mechanisms in A2780 Ovarian Cancer Cells.
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- Cancer Statistics 2021.CA Cancer J Clin. 2021; 71: 7-33
CDC. 03/15/2021 [cited 2022 04/04], Division of cancer prevention and control, 2020, Centers for Disease Control and Prevention. https://www.cdc.gov/cancer/ovarian/basic_info/index.htm.
- Chromosome region maintenance 1 expression and its association with clinical pathological features in primary carcinoma of the liver.Exp Ther Med. 2016; 12: 59-68
- KPT-330 has antitumour activity against non-small cell lung cancer.Br J Cancer. 2014; 111: 281-291
- CRM1 is an export receptor for leucine-rich nuclear export signals.Cell. 1997; 90: 1051-1060
- p53 SUMOylation promotes its nuclear export by facilitating its release from the nuclear export receptor CRM1.Mol Biol Cell. 2013; 24: 2739-2752
- Characterization of BRCA1 protein targeting, dynamics, and function at the centrosome: a role for the nuclear export signal, CRM1, and Aurora A kinase.J Biol Chem. 2012; 287: 7701-7716
- Nuclear export of proteins and drug resistance in cancer.Biochem Pharmacol. 2012; 83: 1021-1032
- Expression, function, and targeting of the nuclear exporter chromosome region maintenance 1 (CRM1) protein.Pharmacol Ther. 2015; 153: 25-35
- NESdb: a database of NES-containing CRM1 cargoes.Mol Biol Cell. 2012; 23: 3673-3676
- Human multiple myeloma cells are sensitized to topoisomerase II inhibitors by CRM1 inhibition.Cancer Res. 2009; 69: 6899-6905
- Prognostic impact and targeting of CRM1 in acute myeloid leukemia.Blood. 2013; 121: 4166-4174
- CRM1 inhibition induces tumor cell cytotoxicity and impairs osteoclastogenesis in multiple myeloma: molecular mechanisms and therapeutic implications.Leukemia. 2014; 28: 155-165
- Dysregulation of apoptosis in hepatocellular carcinoma cells.World J Gastroenterol. 2009; 15: 513
- Cell proliferation and death: forgotten features of chronic lymphocytic leukemia B cells.Best Pract Res Clin Haematol. 2007; 20: 399-413
- Death receptor signaling in cancer therapy.Curr Med Chem Anticancer Agents. 2003; 3: 253-262
- Nucleo-cytoplasmic transport as a therapeutic target of cancer.J Hematol Oncol. 2014; 7: 85
- Prognostic value of CRM1 in pancreas cancer.Clin Invest Med. 2009; 32: e315
- Antitumor effects of a novel chromosome region maintenance 1 (CRM1) inhibitor on non-small cell lung cancer cells in vitro and in mouse tumor xenografts.PLoS One. 2014; 9: e89848
- Expression of the nuclear export protein chromosomal region maintenance/exportin 1/Xpo1 is a prognostic factor in human ovarian cancer.Cancer. 2008; 112: 1733-1743
- The Karyopherin proteins, Crm1 and Karyopherin beta1, are overexpressed in cervical cancer and are critical for cancer cell survival and proliferation.Int J Cancer. 2009; 124: 1829-1840
- CRM1 is a novel independent prognostic factor for the poor prognosis of gastric carcinomas.Med Oncol. 2013; 30: 726
- The expression of CRM1 is associated with prognosis in human osteosarcoma.Oncol Rep. 2009; 21: 229-235
- Gain in the short arm of chromosome 2 (2p+) induces gene overexpression and drug resistance in chronic lymphocytic leukemia: analysis of the central role of XPO1.Leukemia. 2017; 31: 1625-1629
- Restoring the tumour suppressive function of p53 as a parallel strategy in melanoma therapy.FEBS Lett. 2014; 588: 2616-2621
- Genome-wide studies in multiple myeloma identify XPO1/CRM1 as a critical target validated using the selective nuclear export inhibitor KPT-276.Leukemia. 2013; 27: 2357-2365
- Cell cycle arrest and cytotoxic effects of SAHA and RG7388 mediated through p21(WAF1/CIP1) and p27(KIP1) in cancer cells.Medicina. 2019; 55 (Kaunas)
- Differential mechanisms involved in RG-7388 and Nutlin-3 induced cell death in SJSA-1 osteosarcoma cells.Cell Signal. 2020; 75109742
- Ovarian cancer.Lancet North Am Ed. 2014; 384: 1376-1388
- Selinexor is effective in acquired resistance to ibrutinib and synergizes with ibrutinib in chronic lymphocytic leukemia.Blood. 2015; 125: 3128-3132
- Combination treatment with rucaparib (Rubraca) and MDM2 inhibitors, Nutlin-3 and RG7388, has synergistic and dose reduction potential in ovarian cancer.Oncotarget. 2017; 8: 69779-69796
- Molecular mechanism and therapeutic implications of selinexor (KPT-330) in liposarcoma.Oncotarget. 2017; 8: 7521-7532
- MDM2 inhibition: an important step forward in cancer therapy.Leukemia. 2020; 34: 2858-2874
- Combination of metformin and RG7388 enhances inhibition of growth and induction of apoptosis of ovarian cancer cells through the PI3K/AKT/mTOR pathway.Biochem Biophys Res Commun. 2020; 533: 665-671
- Differential mechanisms of cell death induced by HDAC inhibitor SAHA and MDM2 inhibitor RG7388 in MCF-7 cells.Cells. 2018; 8
- A phase 1 clinical trial of single-agent selinexor in acute myeloid leukemia.Blood. 2017; 129: 3165-3174
- CBS9106 is a novel reversible oral CRM1 inhibitor with CRM1 degrading activity.Blood. 2011; 118: 3922-3931
- Nuclear export inhibition through covalent conjugation and hydrolysis of Leptomycin B by CRM1.Proc Natl Acad Sci U S A. 2013; 110: 1303-1308
- First-in-class, first-in-human phase i study of selinexor, a selective inhibitor of nuclear export, in patients with advanced solid tumors.J Clin Oncol. 2016; 34: 4142-4150
- Phase IB study of selinexor, a first-in-class inhibitor of nuclear export, in patients with advanced refractory bone or soft tissue sarcoma.J Clin Oncol. 2016; 34: 3166-3174
- Phase I study of selinexor, a selective inhibitor of nuclear export, in combination with fludarabine and cytarabine, in pediatric relapsed or refractory acute Leukemia.J Clin Oncol. 2016; 34: 4094-4101
- KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia.Br J Haematol. 2013; 161: 117-127
- Identification of nuclear export inhibitors with potent anticancer activity in vivo.Cancer Res. 2009; 69: 510-517
- p21Cip1/Waf1 protein and its function based on a subcellular localization [corrected].J Cell Biochem. 2011; 112: 3502-3506
- Pharmacodynamic and genomic markers associated with response to the XPO1/CRM1 inhibitor selinexor (KPT-330): a report from the pediatric preclinical testing program.Pediatr Blood Cancer. 2016; 63: 276-286