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Title 

Cis-fumagillin, a new methionine aminopeptidase(yp 2) inhibitor produced by Penicillium sp. F2757

Authors 

Ju Young KwonHa Won JeongHyae Kyeong KimKui Hyun KangYie Hwa ChangKyung Sook BaeJung Do ChoiUn Chul LeeKwang Hee SonByoung-Mog Kwon

Publisher 

Nature Publishing Group

Issue Date 

2000

Citation 

Journal of Antibiotics, vol. 53, no. 8, pp. 799-806

Keywords 

aminopeptidaseangiogenesis inhibitorfumagillinmethionine aminopeptidase iimethionine aminopeptidase ii inhibitorunclassified drugdrug activitydrug isolationfermentationfungus mutant

Abstract 

Selective inhibition against the yeast MetAP2 (methionine aminopeptidase type 2) was detected in the fermentation broth of a fungus F2757 that was later identified as Penicillium janczewskii. A new compound cis-fumagillin methyl ester (1) was isolated from the diazomethane treated fermentation extracts together with the known compound fumagillin methyl ester (2). The cis-fumagillin methyl ester, a stereoisomer of fumagillin methyl ester at the C2'-C3' position of the aliphatic side chain, selectively inhibited growth of the map 1 mutant yeast strain (MetAP1 deletion strain) at a concentration as low as 1 ng. However, the wild type yeast w303 and the mutant map2 (MetAP2 deleted) strains were resistant up to 10 μg of the compound. In enzyme experiments, compound 1 inhibited the MetAP2 with an IC50 value of 6.3 nM, but it did not inhibit the MetAP1 (IC50 >200 μM). Compound 2 also inhibited the MetAP2 with an IC50 value of 9.2 nM and 105 μM against MetAP1.

ISSN 

0021-8820

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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