Synonyms: compound 70 [WO2013019561A1] | KPT-330 | KPT330 | Nexpovio® | Xpovio®
selinexor is an approved drug (FDA (2019), EMA (2021))
Compound class:
Synthetic organic
Comment: Selinexor (KPT-330) is an inhibitor of the nuclear export protein XPO1 (a.k.a. exportin 1) that is being developed as an anti-neoplastic agent by Karyopharm Therapeutics. It is a first-in-class inhibitor that exploits a novel mechanism of action compared to existing chemotherapeutics [2,7-8]. The chemical structure is claimed in patent WO2013019561A1 (as compound 70) [9].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Garg M, Kanojia D, Mayakonda A, Ganesan TS, Sadhanandhan B, Suresh S, S S, Nagare RP, Said JW, Doan NB et al.. (2017)
Selinexor (KPT-330) has antitumor activity against anaplastic thyroid carcinoma in vitro and in vivo and enhances sensitivity to doxorubicin. Sci Rep, 7 (1): 9749. [PMID:28852098] |
2. Gerecitano J. (2014)
SINE (selective inhibitor of nuclear export)--translational science in a new class of anti-cancer agents. J Hematol Oncol, 7: 67. [PMID:25281264] |
3. Gordon DE, Jang GM, Bouhaddou M, Xu J, Obernier K, White KM, O'Meara MJ, Rezelj VV, Guo JZ, Swaney DL et al.. (2020)
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. Nature, 583 (7816): 459-468. [PMID:32353859] |
4. Gravina GL, Mancini A, Colapietro A, Marampon F, Sferra R, Pompili S, Biordi LA, Iorio R, Flati V, Argueta C et al.. (2017)
Pharmacological treatment with inhibitors of nuclear export enhances the antitumor activity of docetaxel in human prostate cancer. Oncotarget, 8 (67): 111225-111245. [PMID:29340049] |
5. Kudo N, Khochbin S, Nishi K, Kitano K, Yanagida M, Yoshida M, Horinouchi S. (1997)
Molecular cloning and cell cycle-dependent expression of mammalian CRM1, a protein involved in nuclear export of proteins. J Biol Chem, 272 (47): 29742-51. [PMID:9368044] |
6. Nie D, Huang K, Yin S, Li Y, Xie S, Ma L, Wang X, Wu Y, Xiao J, Wang J et al.. (2018)
KPT-330 inhibition of chromosome region maintenance 1 is cytotoxic and sensitizes chronic myeloid leukemia to Imatinib. Cell Death Discov, 4: 48. [PMID:29707241] |
7. Pal I, Safari M, Jovanovic M, Bates SE, Deng C. (2019)
Targeting Translation of mRNA as a Therapeutic Strategy in Cancer. Curr Hematol Malig Rep, 14 (4): 219-227. [PMID:31231778] |
8. Parikh K, Cang S, Sekhri A, Liu D. (2014)
Selective inhibitors of nuclear export (SINE)--a novel class of anti-cancer agents. J Hematol Oncol, 7: 78. [PMID:25316614] |
9. Sandanayaka VP, Shacham S, Kauffman M, Schechter S, Mccauley D, Landesman Y, Senapedis W, Saint-Martin J-R. (2013)
Nuclear transport modulators and uses thereof. Patent number: WO2013019561A1. Assignee: Karyopharm Therapeutics, Inc.. Priority date: 29/07/2011. Publication date: 04/07/2013. |
10. Widman DG, Gornisiewicz S, Shacham S, Tamir S. (2018)
In vitro toxicity and efficacy of verdinexor, an exportin 1 inhibitor, on opportunistic viruses affecting immunocompromised individuals. PLoS ONE, 13 (10): e0200043. [PMID:30332435] |
11. Wu M, Gui H, Feng Z, Xu H, Li G, Li M, Chen T, Wu Y, Huang J, Bai Z et al.. (2018)
KPT-330, a potent and selective CRM1 inhibitor, exhibits anti-inflammation effects and protection against sepsis. Biochem Biophys Res Commun, 503 (3): 1773-1779. [PMID:30064906] |