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TMC-52A to D, novel cysteine proteinase inhibitors, produced by Gliocladium sp
K Isshiki1, M Nishio, N Sakurai
1Lead Generation Research Laboratory at Toda, Tanabe Seiyaku Co., Ltd., Saitama, Japan.
The Journal of Antibiotics
|September 4, 1998
Abstract:
New cysteine proteinase inhibitors, TMC-52A, B, C, and D, were isolated from the fungal fermentation broth. On the basis of a taxonomical study, the producing strain, F-2665, was characterized as Gliocladium sp. Spectroscopic analyses and chemical degradation have shown TMC-52A to D to be epoxysuccinyl peptides. TMC-52A to D strongly inhibited cysteine proteinases, in particular, cathepsin L with IC50 values of 13 nM, 10nM, 10nM, and 6nM, respectively.