87081-36-5

Leptomycin 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 (Item No. 10004976) 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.

Leptomycin 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.

ChEBI: A leptomycin having all-trans double bonds and a seventh methyl substituent at position 17.

HIV-1

[1] NOBUAKI KUDO . Leptomycin B Inhibition of Signal-Mediated Nuclear Export by Direct Binding to CRM1[J]. Experimental cell research, 1998, 242 2: Pages 540-547. DOI: 10.1006/excr.1998.4136
[2] YING WANG. Novel leptomycins from a streptomyces strain A92-308902: Inhibitors of the Nucleo-cytoplasmic translocation of the HIV-1 regulatory protein Rev[J]. Helvetica Chimica Acta, 2004, 80 7: 2157-2167. DOI: 10.1002/hlca.19970800715