CRM1
CRM1 is present in all eukaryotic cells and was initially identified as a chromosomal mutation in the yeast schizosaccharomyces pombe. Also known as exportin 1 or XPO1, it is responsible for the transport of over 200 proteins, which include many tumor suppressor proteins (TSP) and oncoproteins. CRM1 plays an essential role in mitosis through (I) binding and targeting key mitotic proteins to specific areas of the mitotic spindle; and (II) stabilizing the microtubule kinetochore to promote proper chromosomal segregation. Inhibition of RCC1, which regulates CRM1, by actinomycin D resulted in severe spindle assembly defects and mitotic catastrophe. Among the list of CRM1-mediated proteins are p53, FOXOs, p27, nucleophosmin, BCR-ABL, p21, PI3K/AKT, Wnt/β-catenin, NF-kB, APC, and Rb, all of which are significant targets in oncogenesis. Dysregulation of this transport process has been implicated in cancer, in addition to wound healing, inflammation, and viral infections. CRM1 overexpression has been demonstrated in both solid tumors and hematologic malignancies, and this overexpression is associated with a poorer prognosis and drug resistance. The exact mechanism by which this occurs remains unclear but is thought to involve altered transport mechanisms in favor of cytoplasmic localization and the modification of nuclear proteins to reveal their LR-NES enabling them to bind CRM1.
References
1.Amy Y. Wang,et al. Stem Cell Investig. 2019; 6: 6.
References
1.Amy Y. Wang,et al. Stem Cell Investig. 2019; 6: 6.
Membrane Transporter/Ion Channel
AMPK(58)
ASBT Transporter(6)
BCRP(10)
Beta Amyloid(69)
Carbonic Anhydrase(40)
Chloride Channel(34)
CRAC Channel(0)
CRM1(5)
Exportin-1(5)
FABP(6)
GAT(63)
GLUT(5)
Glutamate Transporter(1)
GlyT(13)
HCN Channel(5)
iGluR(52)
Monoamine Transporter(26)
Monocarboxylate Transporter(12)
MTP(1)
nAChR(5)
NADPH(35)
Na-K-ATPase(2)
NKCC(4)
NMDAR(65)
OCT(4)
Other Targets(13)
P2X Receptor(23)
P-glycoprotein(14)
Proton Pump(38)
Sodium Channel(147)
TRP/TRPV Channel(115)
URAT1(1)
CRM1
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CBS9106
catalog no : M33306
cas no: 1076235-04-5
CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activity. -
Leptomycin B
catalog no : M24883
cas no: 87081-35-4
Leptomycin B is a potent inhibitor of the nuclear export of proteins and is a potent antifungal antibiotic blocking the eukaryotic cell cycle. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. -
KPT276
catalog no : M19411
cas no: 1421919-75-6
KPT-276 is an orally bioavailable selective inhibitor of nuclear export (SINE) that irreversibly bind to CRM1 and block the function of CRM1. -
KPT-330
catalog no : M11769
cas no: 1421923-86-5
KPT-330 inhibited proliferation and induced cell cycle arrest and apoptosis-related proteins in 11 NSCLC cells lines. -
KPT-185
catalog no : M11326
cas no: 1333151-73-7
KPT-185 is a selective CRM1 inhibitor.