ArticlePloS one2014
Novel small molecule XPO1/CRM1 inhibitors induce nuclear accumulation of TP53, phosphorylated MAPK and apoptosis in human melanoma cells.
Article in PloS one, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers.
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Who cites it
33 citing papers in PubMed, 52 citations in OpenAlex.
- Cracking melanoma's armor: Supramolecular dual-strike on XPO1 and β-catenin to overcome resistance.Journal of advanced research · 2025Article
- Exportin 1 (XPO1) Expression and Effectiveness of XPO1 Inhibitor Against Canine Lymphoma Cell Lines.Veterinary sciences · 2025Article
- Analysis of exportins expression unveils their prognostic significance in colon adenocarcinoma: insights from public databases.Discover oncology · 2025Article
- The nuclear export protein exportin-1 in solid malignant tumours: From biology to clinical trials.Clinical and translational medicine · 2024Review
- Genomic and global gene expression profiling in pediatric and young adult acute leukemia with PICALM::MLLT10 Fusion.Leukemia · 2024Article
- Selective nuclear export inhibitor KPT‑330 enhances the radiosensitivity of esophageal carcinoma cells.Experimental and therapeutic medicine · 2023Article
- Therapeutic Targeting of Exportin-1 in Childhood Cancer.Cancers · 2021Review
- Pan-cancer analysis reveals the roles of XPO1 in predicting prognosis and tumorigenesis.Translational cancer research · 2021Article
- XPO1/CRM1 is a promising prognostic indicator for neuroblastoma and represented a therapeutic target by selective inhibitor verdinexor.Journal of experimental & clinical cancer research : CR · 2021Article
- The Second-Generation XPO1 Inhibitor Eltanexor Inhibits Human Cytomegalovirus (HCMV) Replication and Promotes Type I Interferon Response.Frontiers in microbiology · 2021Article
- Quantitative expression of Ikaros, IRF4, and PSMD10 proteins predicts survival in VRD-treated patients with multiple myeloma.Blood advances · 2020Article
- Targeted CRM1-inhibition perturbs leukemogenic NUP214 fusion proteins and exerts anti-cancer effects in leukemia cell lines withOncotarget · 2020Article
- Exportin 1 Inhibition Induces Nerve Growth Factor Receptor Expression to Inhibit the NF-κB Pathway in Preclinical Models of Pediatric High-Grade Glioma.Molecular cancer therapeutics · 2020Article
- A Radiosensitivity Gene Signature and XPO1 Predict Clinical Outcomes for Glioma Patients.Frontiers in oncology · 2020Article
- Molecular profiling of anastatic cancer cells: potential role of the nuclear export pathway.Cellular oncology (Dordrecht, Netherlands) · 2019Article
- Targeting Translation of mRNA as a Therapeutic Strategy in Cancer.Current hematologic malignancy reports · 2019Review
- The roles of p53 and XPO1 on colorectal cancer progression in Yemeni patients.Journal of gastrointestinal oncology · 2019Article
- The past, present, and future of CRM1/XPO1 inhibitors.Stem cell investigation · 2019Review
- Article
- Selinexor (KPT-330) demonstrates anti-tumor efficacy in preclinical models of triple-negative breast cancer.Breast cancer research : BCR · 2017Article
Corrections and comments
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Authors and funding
12 authors at 2 institutions in 1 country.
Funding
Abstract
XPO1/CRM1 is a key nuclear exporter protein that mediates translocation of numerous cellular regulatory proteins. We investigated whether XPO1 is a potential therapeutic target in melanoma using novel selective inhibitors of nuclear export (SINE). In vitro effects of SINE on cell growth and apoptosis were measured by MTS assay and flow cytometry [Annexin V/propidium iodide (PI)], respectively in human metastatic melanoma cell lines. Immunoblot analysis was used to measure nuclear localization of key cellular proteins. The in vivo activity of oral SINE was evaluated in NOD/SCID mice bearing A375 or CHL-1 human melanoma xenografts. SINE compounds induced cytostatic and pro-apoptotic effects in both BRAF wild type and mutant (V600E) cell lines at nanomolar concentrations. The cytostatic and pro-apoptotic effects of XPO1 inhibition were associated with nuclear accumulation of TP53, and CDKN1A induction in the A375 cell line with wild type TP53, while pMAPK accumulated in the nucleus regardless of TP53 status. The orally bioavailable KPT-276 and KPT-330 compounds significantly inhibited growth of A375 (p<0.0001) and CHL-1 (p = 0.0087) human melanoma cell lines in vivo at well tolerated doses. Inhibition of XPO1 using SINE represents a potential therapeutic approach for melanoma across cells with diverse molecular phenotypes by promoting growth inhibition and apoptosis.
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