(2E,10E,12E,16E,18E)-6-hydroxy-3,5,7,9,11,15,17-heptamethyl-19-(3-methyl-6-oxo-2,3-dihydropyran-2-yl)-8-oxononadeca-2,10,12,16,18-pentaenoic acid

개요Leptomycin A is an inhibitor of CRM1 (exportin 1) that blocks CRM1 interaction with nuclear export signals, preventing the nuclear export of a broad range of proteins. Leptomycin A inhibits Rev translocation, though less potently than leptomycin B with IC50 values of 0.8 and 0.1 nM, respectively after 7 hours. Rev export to the cytoplasm is required for HIV-1 replication. Leptomycin A was originally identified as an antifungal agent.

용도Leptomycin A, a methyl analogue of leptomycin B, is a minor component of the leptomycin complex produced by selected Streptomyces species. Leptomycin B is a potent inhibitor of the nuclear transport receptor CRM1. Leptomycin A is also likely to inhibit nuclear transport and may offer differences in exporter selectivity. Leptomycin A shows antimicrobial activity against Schizosaccaromyces pombe and Mucor rouxianus.