Leptomycins are antifungal antibiotics with unique unsaturated, branched-chain fatty acid structures. The physiochemical and biological properties of Leptomycins A and B are very similar. Both are considered to be specific inhibitors of nuclear export. The suggested inhibition mechanism involves the direct binding of leptomycins to CRM1 (Exportin-1), which is the main nuclear export protein. This blocks the binding of CRM1 to proteins containing a nuclear export signal (NES), and therefore prevents their export from the nucleus. Although more research on nuclear export inhibition has been performed using Leptomycin B, it has been shown that Leptomycin A has similar effects and can induce, for example, nuclear accumulation of wild-type ERK5.
Leptomycin A is also active against Schizosaccaromyces pombe and Mucor rouxianus.
| Molecular Weight | 526.7 |
| Formula | C32H46O6 |
| CAS Number | 87081-36-5 |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] M Yoshida, et al. Leptomycin: a specific inhibitor of protein nuclear export
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