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The export pump that carries tumour suppressor proteins such as p53 out of the nucleus, where they cannot act. Selinexor blocks it so those brakes stay in the nucleus and cancer cells die.
Exportin-1, also called CRM1, shuttles more than 200 cargo proteins from the nucleus to the cytoplasm, including p53, p21, FOXO, IkB and the eIF4E-bound oncogene messenger RNAs. Many cancers overexpress it, keeping tumour suppressors out of the nucleus. Selinexor binds covalently to cysteine 528 of XPO1, trapping the suppressors inside the nucleus; it is approved for relapsed multiple myeloma and diffuse large B-cell lymphoma, and is under study in TP53 wild-type endometrial cancer. Nausea, anorexia, weight loss and thrombocytopenia are its main side effects.
In plain words · The export pump that carries tumour suppressor proteins such as p53 out of the nucleus, where they cannot act. Selinexor blocks it so those brakes stay in the nucleus and cancer cells die.
The export pump that carries tumour suppressor proteins such as p53 out of the nucleus, where they cannot act. Selinexor blocks it so those brakes stay in the nucleus and cancer cells die.
Karyopherin that exports nuclear export signal-bearing proteins and some RNAs; inhibited covalently by selinexor at Cys528.
No product in this corpus aims at Exportin-1 (XPO1) yet. Drugs bind the molecule precisely: to switch it off, flag the cell for the immune system, or deliver a payload.
Broadly expressed or essential: HPA lists XPO1 among essential proteins and finds the RNA at low tissue specificity; the 1 medicine aimed at it (Selinexor) act on the wild-type protein, so normal tissue is exposed and the therapeutic window comes from the tumour's faster division or its dependence on the protein. HPA XPO1: RNA low tissue specificity; high antibody staining in 29 normal tissues; highest cancer staining urothelial cancer (8 of 12 high). Distribution: 3 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Lymphoma, Multiple myeloma, Endometrial cancer); Open Targets associates it with 3 specific cancer types at or above 0.5 (plasma cell myeloma, B-cell chronic lymphocytic leukemia, diffuse large B-cell lymphoma). (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas XPO1 tissue; Open Targets ENSG00000082898 associations
First described 1997. Earliest sequence paper UniProt cites for the protein: Fornerod et al, EMBO J, 1997, "The human homologue of yeast CRM1 is in a dynamic subcomplex with CAN/Nup214 and the novel nuclear pore component Nup88". Source.
Karyopherin that exports nuclear export signal-bearing proteins and some RNAs; inhibited covalently by selinexor at Cys528.
RNA: low tissue specificity, detected in all normal tissues.
Medium: Adipose tissue, Breast, Caudate, Cerebellum, Cerebral cortex, Gallbladder, Hippocampus, Kidney.
Medium only: cervical cancer, endometrial cancer, head and neck cancer, liver cancer.
HPA XPO1 tissue · HPA XPO1 pathology · HPA protein class: Essential proteins, FDA approved drug targets
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Hodgkin lymphoma | 26% | XPO1 mutation (mostly E571K), sequencing, 5 of 19 cases | Small series; the same study found XPO1 mutations in 24% of primary mediastinal B-cell lymphoma (28 of 117) and in under 2% of other diffuse large B-cell lymphoma | doi.org |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Query for this target: (TITLE:"Exportin-1" OR ABSTRACT:"Exportin-1" OR TITLE:"XPO1" OR ABSTRACT:"XPO1") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Exportin-1 (XPO1), not a curated reading list.
Shares Selinexor, Relapsed or refractory multiple myeloma, Multiple myeloma.
Shares Selinexor, Diffuse large B-cell lymphoma.
Shares Selinexor, Relapsed or refractory multiple myeloma, Multiple myeloma.
Shares Relapsed or refractory multiple myeloma, Multiple myeloma.
Shares Relapsed or refractory multiple myeloma, Multiple myeloma.
Shares Relapsed or refractory multiple myeloma, Multiple myeloma.
Shares Relapsed or refractory multiple myeloma, Multiple myeloma.
Shares Relapsed or refractory multiple myeloma, Multiple myeloma.