Leptomycin B is a potent inhibitor of the nuclear export of proteins. It directly blocks the interaction of CRM1 (exportin 1) with nuclear export signals (NES), preventing the export of a broad range of proteins.1 Leptomycin B will also indirectly inhibit the export of mRNA from the nucleus by blocking the nuclear export of mRNA-binding proteins (export factors).2 By blocking the nuclear export of p53, leptomycin B prevents entry of human normal fibroblasts into the S phase of the cell cycle, thus inhibiting proliferation.3 Leptomycin B was originally identified as an antifungal agent and is isolated from Streptomyces sp..
1
Kudo, N., Wolff, B., Sekimoto, T., et al. Leptomycin B inhibition of signal-mediated nuclear export by direct binding to CRM1. Exp Cell Res242540-547(1998).
2
Nishi, K., Yoshida, M., Fujiwara, D., et al. Leptomycin B targets a regulatory cascade of crm1, a fission yeast nuclear protein, involved in control of higher order chromosome structure and gene expression. J Biol Chem269(9)6320-6324(1994).
3
Smart, P., Lane, E.B., Lane, D.P., et al. Effects on normal fibroblasts and neuroblastoma cells of the activation of the p53 response by the nuclear export inhibitor leptomycin B. Oncogene187378-7386(1999).
Kudo, N., Wolff, B., Sekimoto, T., et al. Leptomycin B inhibition of signal-mediated nuclear export by direct binding to CRM1. Exp Cell Res242540-547(1998).
Nishi, K., Yoshida, M., Fujiwara, D., et al. Leptomycin B targets a regulatory cascade of crm1, a fission yeast nuclear protein, involved in control of higher order chromosome structure and gene expression. J Biol Chem269(9)6320-6324(1994).
Smart, P., Lane, E.B., Lane, D.P., et al. Effects on normal fibroblasts and neuroblastoma cells of the activation of the p53 response by the nuclear export inhibitor leptomycin B. Oncogene187378-7386(1999).
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