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)
Potassium Channel(0)
Proton Pump(38)
Sodium Channel(147)
TRP/TRPV Channel(115)
URAT1(1)
CRM1
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CBS9106
产品货号 : M33306
cas no: 1076235-04-5
CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activity.CBS9106 inhibits CRM1-dependent nuclear export and reduces CRM1 protein levels.CBS9106 inhibits tumor growth and prolongs the survival of mice bearing tumor xenografts.CBS9106 is an inhibitor of CRM1-dependent nuclear export and reduces CRM1 protein levels. -
Leptomycin B
产品货号 : M24883
cas no: 87081-35-4
Leptomycin B 是一种有效的蛋白质核输出抑制剂,也是一种有效的抗真菌抗生素,可阻断真核细胞周期。 Leptomycin B 通过半胱氨酸残基的共价修饰使 CRM1/exportin 1 失活。 -
KPT276
产品货号 : M19411
cas no: 1421919-75-6
KPT-276 是一种口服生物可利用的选择性核输出抑制剂 (SINE),它不可逆地与 CRM1 结合并阻断 CRM1 的功能。 -
KPT-330
产品货号 : M11769
cas no: 1421923-86-5
KPT-330 在 11 种 NSCLC 细胞系中抑制增殖并诱导细胞周期停滞和凋亡相关蛋白。 -
KPT-185
产品货号 : M11326
cas no: 1333151-73-7
KPT-185 是一种选择性 CRM1 抑制剂。