Art

J-GLOBAL ID：200902245328660401   Reference number：05A0816283

Synthesis and Activity of Tyropeptin A Derivatives as Potent and Selective Inhibitors of Mammalian 20S Proteasome

ほ乳動物20Sプロテアソームの強力で選択的な阻害剤としてのチロペプチンA誘導体の合成および活性

Author (6)： MOMOSE Isao (Numazu Bio-Medical Res. Inst., Microbial Chemistry Res. Center) ,  UMEZAWA Yoji (Microbial Chemistry Res. Center) ,  HIROSAWA Sehei (Hiyoshi Medicinal Chemistry Res. Inst., Microbial Chemistry Res. Center) ,  IIJIMA Masatomi (Numazu Bio-Medical Res. Inst., Microbial Chemistry Res. Center) ,  IINUMA Hironobu (Microbial Chemistry Res. Center) ,  IKEDA Daishiro (Numazu Bio-Medical Res. Inst., Microbial Chemistry Res. Center)
Material： Bioscience, Biotechnology, and Biochemistry  (Bioscience Biotechnology & Biochemistry)
Volume： 69  Issue： 9  Page： 1733-1742 (J-STAGE)  Publication year： 2005 
JST Material Number： G0021A  ISSN： 0916-8451  CODEN： BBBIEJ  Document type： Article
Article type： 原著論文  Country of issue： Japan (JPN)  Language： ENGLISH (EN)

Thesaurus term： proteasome ,...

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JST classification (1)： Enzyme in general  (EB09010D)

Substance index (12)： Tyropeptin A ,  rac-(R^*)-2-[[N-(Cyclohexylacetyl)-L-Tyr-L-Val-]amino]-3-(4-hydroxyphenyl)propanal ,  rac-(R^*)-2-[[N-(Phenylacetyl)-L-Tyr-L-Val-]amino]-3-(4-hydroxyphenyl)propanal ,  rac-(R^*)-2-[[N-(2-Naphthylacetyl)-L-Tyr-L-Val-]amino]-3-(4-hydroxyphenyl)propanal ,  rac-(R^*)-2-[[N-(1-Naphthylacetyl)-L-Tyr-L-Val-]amino]-3-(4-hydroxyphenyl)propanal ,  rac-(R^*)-2-[(N-Heptanoyl-L-Tyr-L-Val-)amino]-3-(4-hydroxyphenyl)propanal ,  rac-(R^*)-2-[(N-Isovaleryl-L-Tyr-L-Val-)amino]-3-(4-methoxyphenyl)propanal ,  rac-(R^*)-2-[(N-Isovaleryl-O-methyl-L-Tyr-L-Val-)amino]-3-(4-methoxyphenyl)propanal ,  rac-(R^*)-2-[[N-(1-Naphthylacetyl)-L-Tyr-L-Val-]amino]-3-(4-methoxyphenyl)propanal ,  rac-(R^*)-2-[[N-(1-Naphthylacetyl)-O-methyl-L-Tyr-L-Val-]amino]-3-(4-hydroxyphenyl)propanal ,  rac-(R^*)-2-[[N-(1-Naphthylacetyl)-O-methyl-L-Tyr-L-Val-]amino]-3-(4-methoxyphenyl)propanal ,  rac-(R^*)-2-[[N-(Dimethylaminoacetyl)-L-Tyr-L-Val-]amino]-3-(4-hydroxyphenyl)propanal

Reference (13)：

• 1) Coux, O., Tanaka, K., and Goldberg, A. L., Structure and functions of the 20S and 26S proteasomes. Annu. Rev. Biochem., 65, 801–847 (1996).
• 2) Voges, D., Zwickl, P., and Baumeister, W., The 26S proteasome: A molecular machine designed for controlled proteolysis. Annu. Rev. Biochem., 68, 1015–1068 (1999).
• 3) Maki, C. G., and Howley, P. N., Ubiquitination of p53 and p21 is differentially affected by ionizing and UV radiation. Mol. Cell. Biol., 17, 355–363 (1997).
• 4) Pagano, M., Tam, S. W., Theodoras, A. M., Beer-Romero, P., Del Sal, G., Chau, V., Yew, P. R., Draetta, G. F., and Rolfe, M., Role of the ubiquitin-proteasome pathway in regulating abundance of the cyclin-dependent kinase inhibitor p27. Science, 269, 682–685 (1995).
• 5) Ciechanover, A., DiGiuseppe, J. A., Bercovich, B., Orian, A., Richter, J. D., Schwartz, A. L., and Brodeur, G. M., Degradation of nuclear oncoproteins by the ubiquitin system in vitro. Proc. Natl. Acad. Sci. U.S.A., 88, 139–143 (1991).

Terms in the title (5)： ほ乳動物 ,  20Sプロテアソーム ,  阻害剤 ,  誘導体 ,  活性