Isshiki K, Nishio M, Sakurai N, Uchida T, Okuda T, Komatsubara S
Lead Generation Research Laboratory at Toda, Tanabe Seiyaku Co., Ltd., Saitama, Japan.
J Antibiot (Tokyo). 1998 Jul;51(7):629-34. doi: 10.7164/antibiotics.51.629.
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.
新型半胱氨酸蛋白酶抑制剂TMC - 52A、B、C和D是从真菌发酵液中分离得到的。基于分类学研究，产生菌株F - 2665被鉴定为粘帚霉属。光谱分析和化学降解表明TMC - 52A至D为环氧琥珀酰肽。TMC - 52A至D强烈抑制半胱氨酸蛋白酶，尤其是组织蛋白酶L，其IC50值分别为13 nM、10 nM、10 nM和6 nM。
